This document describes the design and evaluation of atenolol gastroretentive floating tablets using a 3^2 factorial design. Nine formulations were prepared using different concentrations of HPMC K15M and sodium bicarbonate as independent variables. The dependent variables measured were the time taken for 10%, 50%, 75%, and 90% drug dissolution. Formulation F8, containing 25% HPMC K15M and 3.75% sodium bicarbonate, showed prolonged drug release similar to the marketed product and followed Higuchi kinetics with non-Fickian diffusion-controlled drug release. Polynomial equations were developed relating the independent and dependent variables.
Abstract
The main objective of present research work is to formulate the floating tablets of atenolol using 32 factorial design. Atenolol, β-blocker belongs to Biopharmaceutical Classification System Class-III. The floating tablets of atenolol were prepared employing different concentrations of hydroxypropyl methylcellulose (HPMC) K15M and sodium bicarbonate in different combinations by direct compression technique using 32 factorial design. The concentration of HPMC K15M and sodium bicarbonate required to achieve desired drug release was selected as independent variables, X1 and X2, respectively, whereas time required for 10% of drug dissolution (t10%), 50% (t50%), 75% (t75%), and 90% (t90%) were selected as dependent variables. Totally, nine formulations were designed and are evaluated for hardness, friability, thickness, % drug content, floating lag time, in vitro drug release. From the results, concluded that all the formulation were found to be within the pharmacopoeial limits and the in vitro dissolution profiles of all formulations were fitted into different Kinetic models, the statistical parameters like intercept (a), slope (b) and regression coefficient (r) were calculated. Polynomial equations were developed for t10%, t50%, t75%, t90%. Validity of developed polynomial equations was verified by designing 2 checkpoint formulations (C1, C2). According to SUPAC guidelines the formulation (F8) containing combination of 25% HPMC K15M and 3.75% sodium bicarbonate, is the most similar formulation (similarity factor f2 = 87.797, dissimilarity factor f1 = 2.248 and no significant difference, t = 0.098) to marketed product (BETACARD). The selected formulation (F8) follows Higuchi’s kinetics, and the mechanism of drug release was found to be non-Fickian diffusion (n = 1.029, Super Case-II transport).
The main objective of present investigation is to formulate the floating tablets of
Ranitidine.HCl using 32 factorial design. Ranitidine.HCl, H2-receptor antagonist belongs to
BCS Class-III. The Floating tablets of Ranitidine.HCl were prepared employing different
concentrations of HPMCK4M and Guar Gum in different combinations as a release rate
modifiers by Direct Compression technique using 32 factorial design. The concentration of
Polymers , HPMCK4M and Guar Gum required to achieve desired drug release was selected
as independent variables, X1 and X2 respectively whereas, time required for 10% of drug
dissolution (t10%), 50% (t50%), 75% (t75%) and 90% (t90%) were selected as dependent variables.
Totally nine formulations were designed and are evaluated for hardness, friability, thickness,
% drug content, Floating Lag time, In-vitro drug release. From the Results concluded that all
the formulation were found to be within the Pharmacopoeial limits and the In-vitro
dissolution profiles of all formulations were fitted in to different Kinetic models, the
statistical parameters like intercept (a), slope (b) & regression coefficient (r) were calculated.
Polynomial equations were developed for t10%, t50%, t75%, t90%. Validity of developed
polynomial equations were verified by designing 2 check point formulations(C1, C2).
According to SUPAC guidelines the formulation (F5) containing combination of 22.5%
HPMCK4M and 22.5% Guar Gum, is the most similar formulation (similarity factor f2=85.01,
dissimilarity factor f1= 15.358 & No significant difference, t= 0.169) to marketed product
(ZANTAC). The selected formulation (F5) follows Higuchi’s kinetics, and the mechanism of
drug release was found to be Non-Fickian Diffusion (n= 0.922).
This document describes the development and evaluation of carvedilol phosphate gastroretentive floating tablets using a 32 factorial design. Carvedilol phosphate is a drug that belongs to BCS Class II and is indicated for hypertension and heart failure. Floating tablets were prepared using varying concentrations of guar gum and sodium bicarbonate as polymers to control the release of the water soluble drug. Nine formulations were designed and evaluated for properties like drug content, floating lag time, and in vitro drug release using kinetic models. The results showed that all formulations met pharmacopeial standards and formulation F8 containing 25% guar gum and 3.75% sodium bicarbonate best matched the marketed product with respect to drug release.
ABSTRACT
The main objective of present research work is to formulate the floating tablets of Carvedilol Phosphate using 32 factorial design. Carvedilol Phosphate, non-selective α1-β1-blocking agent belongs to BCS Class-II and Indicated for treatment of Hypertension/moderate Heart Failure. The Floating tablets of Carvedilol Phosphate were prepared employing different concentrations of HPMCK100M and Sodium bicarbonate in different combinations by Direct Compression technique using 32 factorial design. The concentration of HPMCK100M and Sodium bicarbonate required to achieve desired drug release was selected as independent variables, X1 and X2 respectively whereas, time required for 10% of drug dissolution (t10%), 50% (t50%), 75% (t75%) and 90% (t90%) were selected as dependent variables. Totally nine formulations were designed and are evaluated for hardness, friability, thickness, % drug content, Floating Lag time, In-vitro drug release. From the Results concluded that all the formulation were found to be with in the Pharmacopoeial limits and the In-vitro dissolution profiles of all formulations were fitted in to different Kinetic models, the statistical parameters like intercept (a), slope (b) & regression coefficient (r) were calculated. Polynomial equations were developed for t10%, t50%, t75%, t90%. Validity of developed polynomial equations were verified by designing 2 check point formulations (C1, C2). According to SUPAC guidelines the formulation (F8) containing combination of 25% HPMCK100M and 3.75% Sodium bicarbonate, is the most similar formulation (similarity factor f2=88.801, dissimilarity factor f1= 2.250 & No significant difference, t= 0.095) to marketed product (CARDIVAS). The selected formulation (F8) follows Higuchi’s kinetics, and the mechanism
ABSTRACT
The main objective of present research work is to formulate the of Domperidone Maleate floating tablets.
Domperidone Maleate, an antiemetic and a prokinetic agent belongs to BCS Class-II and Indicated for treatment of
upper gastrointestinal motility disorders by blocking the action of Dopamine. The Floating tablets of Domperidone
Maleate were prepared employing different concentrations of HPMCK4M and Guar Gum in different combinations
as a release rate modifiers by Direct Compression technique using 32 factorial design. The concentration of
HPMCK4M and Guar Gum was selected as independent variables, X1 and X2 respectively whereas, time required
for drug dissolution t10%, t50%,t75%,t90%were selected as dependent variables. Totally nine formulations were designed
and are evaluated for hardness, friability, thickness, Assay, Floating Lag time, In-vitro drug release. From the
Results concluded that all the formulation were found to be with in the Pharmacopoeial limits and the In-vitro
dissolution profiles of all formulations were fitted in to different Kinetic models, the statistical parameters like
intercept (a), slope (b) & regression coefficient (r) were calculated. Polynomial equations were developed for t10%,
t50%, t75%, t90%. Validity of developed polynomial equations were verified by designing 2 check point formulations(C1,
C2). According to SUPAC guidelines the formulation (F5) containing combination of 18.75% HPMCK4M and
18.75% Guar Gum, is the most similar formulation (similarity factor f2=89.03, dissimilarity factor f1= 11.539& No
significant difference, t= 0.169) to marketed product (DOMSTAL OD). The selected formulation (F5) follows
Higuchi’s kinetics, and the mechanism of drug release was found to be Non-Fickian Diffusion (n= 0.925).
Keywords: Domperidone Maleate, 32Factorial Design, Gastro retentive Floating Tablet, HPMCK100M, Sodium
bicarbonate, Floating Lag Time, SUPAC, Non-Fickian Diffusion Mechanism.
Abstract: The main objective of present investigation is to formulate the sustained release
tablet of Rosiglitazone Maleate using 32 factorial design. Rosiglitazone Maleate, an oral antidiabetic
agent. The SR tablets of Rosiglitazone Maleate were prepared employing different
concentrations of HPMCK15M and Carboplol934P in different combinations as a rate
retardants by Direct Compression technique using 32 factorial design. The quantity/
concentration of Polymers , HPMCK15M and Carboplol934P required to achieve the desired
drug release was selected as independent variables, X1 and X2 respectively whereas, time
required for 10% of drug dissolution (t10%), 50% (t50%), 75% (t75%) and 90% (t90%) were
selected as dependent variables. Totally nine formulations were designed and are evaluated
for hardness, friability, thickness, % drug content, In-vitro drug release. From the Results it
was concluded that all the formulation were found to be with in the Pharmacopoeial limits
and the In-vitro dissolution profiles of all formulations were fitted in to different Kinetic
models, the statistical parameters like intercept (a), slope (b) & regression coefficient (r)
were calculated. Polynomial equations were developed for t10%, t50%, t75%, t90%. Validity of
developed polynomial equations were verified by designing 2 check point formulations(C1,
C2). According to SUPAC guidelines the formulation (F5) containing combination of 25%
HPMCK15M and 20% Carboplol934P, is the most similar formulation (similarity factor
f2=93.1376, dissimilarity factor f1= 1.7642 & No significant difference, t= 0.06949) to
marketed product (AVANDIA). The selected formulation (F5) follows Higuchi’s kinetics,
and the mechanism of drug release was found to be Fickian Diffusion (n= 0.417).
ABSTRACT
The main objective of present investigation is to formulate the sustained release tablet of Metoprolol Succinate
using 32 factorial design. Metoprolol Succinate, is a selective β1blocker, to treat Hypertension & Heart Failure. The
SR tablets of Metoprolol Succinate were prepared employing different concentrations of HPMCK15M and
HPMCK100M in different combinations as a rate retardants by Direct Compression technique using 32 factorial
design. The quantity of rate retarders, HPMCK15M and HPMCK100M required to achieve the desired drug release
was selected as independent variables, X1 and X2 respectively whereas, time required for 10% of drug dissolution
(t10%), 50% (t50%), 75% (t75%) and 90% (t90%) were selected as dependent variables. Totally nine formulations were
designed and are evaluated for hardness, friability, thickness, % drug content, In-vitro drug release. From the
Results it was concluded that all the formulation were found to be with in the Pharmacopoeial limits and the Invitro
dissolution profiles of all formulations were fitted in to different Kinetic models, the statistical parameters like
intercept (a), slope (b) & regression coefficient (r) were calculated. Polynomial equations were developed for t10%,
t50%, t75%, t90%. Validity of developed polynomial equations were verified by designing 2 check point formulations(C1,
C2). According to SUPAC guidelines the formulation (F5) containing combination of 10% HPMCK15M and 10%
HPMCK100M, is the most similar formulation (f2=92.38 & No significant difference, t= 0.0216) to marketed
product (Metocard). The selected formulation (F5) follows Higuchi’s kinetics, the mechanism of drug release was
found to be Super case II transport (Non-Fickian, n= 0.981).
The main objective of present research investigation is to formulate
the sustained release tablet of Doxofylline using 32 factorial design.
Doxofylline, an anti-Asthmatic agent, belongs BCS class-III agent.
The SR tablets of Doxofylline were prepared employing different
concentrations of HPMC K100M and Chitosan in different
combinations by Direct Compression technique using 32 factorial
design. The concentration of Polymers, HPMC K100M and
Chitosan required to achieve the desired drug release was selected as
independent variables, X1 and X2 respectively whereas, time required
for 10% of drug dissolution (t10%), 50% (t50%), 75% (t75%) and 90%
(t90%) were selected as dependent variables. Totally nine formulations
were designed, Formulated and are evaluated for hardness, friability,
thickness, % drug content, In-vitro drug release. From the Results
it was concluded that all the formulation were found to be with
in the Pharmacopoeial limits and the In-vitro dissolution profiles
of all formulations were fitted in to different Kinetic models, the
statistical parameters like intercept, slope & regression coefficient
were calculated. Polynomial equations were developed for t10%,
t50%, t75%, t90%. Validity of developed polynomial equations were
verified by designing 2 check point formulations (C1, C2). According
to SUPAC guidelines the formulation (F4) containing combination
of 10% HPMC K100M and 15% Chitosan, is the most similar
formulation (similarity factor f2= 64.501, dissimilarity factor f1=
6.862 & No significant difference, t= 0.23001) to marketed product
(DOXOLIN). The selected formulation (F4) follows Zero order,
Higuchi’s kinetics, and the mechanism of drug release was found to be Non-Fickian Diffusion anomalous Super Case-II Transport (n= 0.963).
Abstract
The main objective of present research work is to formulate the floating tablets of atenolol using 32 factorial design. Atenolol, β-blocker belongs to Biopharmaceutical Classification System Class-III. The floating tablets of atenolol were prepared employing different concentrations of hydroxypropyl methylcellulose (HPMC) K15M and sodium bicarbonate in different combinations by direct compression technique using 32 factorial design. The concentration of HPMC K15M and sodium bicarbonate required to achieve desired drug release was selected as independent variables, X1 and X2, respectively, whereas time required for 10% of drug dissolution (t10%), 50% (t50%), 75% (t75%), and 90% (t90%) were selected as dependent variables. Totally, nine formulations were designed and are evaluated for hardness, friability, thickness, % drug content, floating lag time, in vitro drug release. From the results, concluded that all the formulation were found to be within the pharmacopoeial limits and the in vitro dissolution profiles of all formulations were fitted into different Kinetic models, the statistical parameters like intercept (a), slope (b) and regression coefficient (r) were calculated. Polynomial equations were developed for t10%, t50%, t75%, t90%. Validity of developed polynomial equations was verified by designing 2 checkpoint formulations (C1, C2). According to SUPAC guidelines the formulation (F8) containing combination of 25% HPMC K15M and 3.75% sodium bicarbonate, is the most similar formulation (similarity factor f2 = 87.797, dissimilarity factor f1 = 2.248 and no significant difference, t = 0.098) to marketed product (BETACARD). The selected formulation (F8) follows Higuchi’s kinetics, and the mechanism of drug release was found to be non-Fickian diffusion (n = 1.029, Super Case-II transport).
The main objective of present investigation is to formulate the floating tablets of
Ranitidine.HCl using 32 factorial design. Ranitidine.HCl, H2-receptor antagonist belongs to
BCS Class-III. The Floating tablets of Ranitidine.HCl were prepared employing different
concentrations of HPMCK4M and Guar Gum in different combinations as a release rate
modifiers by Direct Compression technique using 32 factorial design. The concentration of
Polymers , HPMCK4M and Guar Gum required to achieve desired drug release was selected
as independent variables, X1 and X2 respectively whereas, time required for 10% of drug
dissolution (t10%), 50% (t50%), 75% (t75%) and 90% (t90%) were selected as dependent variables.
Totally nine formulations were designed and are evaluated for hardness, friability, thickness,
% drug content, Floating Lag time, In-vitro drug release. From the Results concluded that all
the formulation were found to be within the Pharmacopoeial limits and the In-vitro
dissolution profiles of all formulations were fitted in to different Kinetic models, the
statistical parameters like intercept (a), slope (b) & regression coefficient (r) were calculated.
Polynomial equations were developed for t10%, t50%, t75%, t90%. Validity of developed
polynomial equations were verified by designing 2 check point formulations(C1, C2).
According to SUPAC guidelines the formulation (F5) containing combination of 22.5%
HPMCK4M and 22.5% Guar Gum, is the most similar formulation (similarity factor f2=85.01,
dissimilarity factor f1= 15.358 & No significant difference, t= 0.169) to marketed product
(ZANTAC). The selected formulation (F5) follows Higuchi’s kinetics, and the mechanism of
drug release was found to be Non-Fickian Diffusion (n= 0.922).
This document describes the development and evaluation of carvedilol phosphate gastroretentive floating tablets using a 32 factorial design. Carvedilol phosphate is a drug that belongs to BCS Class II and is indicated for hypertension and heart failure. Floating tablets were prepared using varying concentrations of guar gum and sodium bicarbonate as polymers to control the release of the water soluble drug. Nine formulations were designed and evaluated for properties like drug content, floating lag time, and in vitro drug release using kinetic models. The results showed that all formulations met pharmacopeial standards and formulation F8 containing 25% guar gum and 3.75% sodium bicarbonate best matched the marketed product with respect to drug release.
ABSTRACT
The main objective of present research work is to formulate the floating tablets of Carvedilol Phosphate using 32 factorial design. Carvedilol Phosphate, non-selective α1-β1-blocking agent belongs to BCS Class-II and Indicated for treatment of Hypertension/moderate Heart Failure. The Floating tablets of Carvedilol Phosphate were prepared employing different concentrations of HPMCK100M and Sodium bicarbonate in different combinations by Direct Compression technique using 32 factorial design. The concentration of HPMCK100M and Sodium bicarbonate required to achieve desired drug release was selected as independent variables, X1 and X2 respectively whereas, time required for 10% of drug dissolution (t10%), 50% (t50%), 75% (t75%) and 90% (t90%) were selected as dependent variables. Totally nine formulations were designed and are evaluated for hardness, friability, thickness, % drug content, Floating Lag time, In-vitro drug release. From the Results concluded that all the formulation were found to be with in the Pharmacopoeial limits and the In-vitro dissolution profiles of all formulations were fitted in to different Kinetic models, the statistical parameters like intercept (a), slope (b) & regression coefficient (r) were calculated. Polynomial equations were developed for t10%, t50%, t75%, t90%. Validity of developed polynomial equations were verified by designing 2 check point formulations (C1, C2). According to SUPAC guidelines the formulation (F8) containing combination of 25% HPMCK100M and 3.75% Sodium bicarbonate, is the most similar formulation (similarity factor f2=88.801, dissimilarity factor f1= 2.250 & No significant difference, t= 0.095) to marketed product (CARDIVAS). The selected formulation (F8) follows Higuchi’s kinetics, and the mechanism
ABSTRACT
The main objective of present research work is to formulate the of Domperidone Maleate floating tablets.
Domperidone Maleate, an antiemetic and a prokinetic agent belongs to BCS Class-II and Indicated for treatment of
upper gastrointestinal motility disorders by blocking the action of Dopamine. The Floating tablets of Domperidone
Maleate were prepared employing different concentrations of HPMCK4M and Guar Gum in different combinations
as a release rate modifiers by Direct Compression technique using 32 factorial design. The concentration of
HPMCK4M and Guar Gum was selected as independent variables, X1 and X2 respectively whereas, time required
for drug dissolution t10%, t50%,t75%,t90%were selected as dependent variables. Totally nine formulations were designed
and are evaluated for hardness, friability, thickness, Assay, Floating Lag time, In-vitro drug release. From the
Results concluded that all the formulation were found to be with in the Pharmacopoeial limits and the In-vitro
dissolution profiles of all formulations were fitted in to different Kinetic models, the statistical parameters like
intercept (a), slope (b) & regression coefficient (r) were calculated. Polynomial equations were developed for t10%,
t50%, t75%, t90%. Validity of developed polynomial equations were verified by designing 2 check point formulations(C1,
C2). According to SUPAC guidelines the formulation (F5) containing combination of 18.75% HPMCK4M and
18.75% Guar Gum, is the most similar formulation (similarity factor f2=89.03, dissimilarity factor f1= 11.539& No
significant difference, t= 0.169) to marketed product (DOMSTAL OD). The selected formulation (F5) follows
Higuchi’s kinetics, and the mechanism of drug release was found to be Non-Fickian Diffusion (n= 0.925).
Keywords: Domperidone Maleate, 32Factorial Design, Gastro retentive Floating Tablet, HPMCK100M, Sodium
bicarbonate, Floating Lag Time, SUPAC, Non-Fickian Diffusion Mechanism.
Abstract: The main objective of present investigation is to formulate the sustained release
tablet of Rosiglitazone Maleate using 32 factorial design. Rosiglitazone Maleate, an oral antidiabetic
agent. The SR tablets of Rosiglitazone Maleate were prepared employing different
concentrations of HPMCK15M and Carboplol934P in different combinations as a rate
retardants by Direct Compression technique using 32 factorial design. The quantity/
concentration of Polymers , HPMCK15M and Carboplol934P required to achieve the desired
drug release was selected as independent variables, X1 and X2 respectively whereas, time
required for 10% of drug dissolution (t10%), 50% (t50%), 75% (t75%) and 90% (t90%) were
selected as dependent variables. Totally nine formulations were designed and are evaluated
for hardness, friability, thickness, % drug content, In-vitro drug release. From the Results it
was concluded that all the formulation were found to be with in the Pharmacopoeial limits
and the In-vitro dissolution profiles of all formulations were fitted in to different Kinetic
models, the statistical parameters like intercept (a), slope (b) & regression coefficient (r)
were calculated. Polynomial equations were developed for t10%, t50%, t75%, t90%. Validity of
developed polynomial equations were verified by designing 2 check point formulations(C1,
C2). According to SUPAC guidelines the formulation (F5) containing combination of 25%
HPMCK15M and 20% Carboplol934P, is the most similar formulation (similarity factor
f2=93.1376, dissimilarity factor f1= 1.7642 & No significant difference, t= 0.06949) to
marketed product (AVANDIA). The selected formulation (F5) follows Higuchi’s kinetics,
and the mechanism of drug release was found to be Fickian Diffusion (n= 0.417).
ABSTRACT
The main objective of present investigation is to formulate the sustained release tablet of Metoprolol Succinate
using 32 factorial design. Metoprolol Succinate, is a selective β1blocker, to treat Hypertension & Heart Failure. The
SR tablets of Metoprolol Succinate were prepared employing different concentrations of HPMCK15M and
HPMCK100M in different combinations as a rate retardants by Direct Compression technique using 32 factorial
design. The quantity of rate retarders, HPMCK15M and HPMCK100M required to achieve the desired drug release
was selected as independent variables, X1 and X2 respectively whereas, time required for 10% of drug dissolution
(t10%), 50% (t50%), 75% (t75%) and 90% (t90%) were selected as dependent variables. Totally nine formulations were
designed and are evaluated for hardness, friability, thickness, % drug content, In-vitro drug release. From the
Results it was concluded that all the formulation were found to be with in the Pharmacopoeial limits and the Invitro
dissolution profiles of all formulations were fitted in to different Kinetic models, the statistical parameters like
intercept (a), slope (b) & regression coefficient (r) were calculated. Polynomial equations were developed for t10%,
t50%, t75%, t90%. Validity of developed polynomial equations were verified by designing 2 check point formulations(C1,
C2). According to SUPAC guidelines the formulation (F5) containing combination of 10% HPMCK15M and 10%
HPMCK100M, is the most similar formulation (f2=92.38 & No significant difference, t= 0.0216) to marketed
product (Metocard). The selected formulation (F5) follows Higuchi’s kinetics, the mechanism of drug release was
found to be Super case II transport (Non-Fickian, n= 0.981).
The main objective of present research investigation is to formulate
the sustained release tablet of Doxofylline using 32 factorial design.
Doxofylline, an anti-Asthmatic agent, belongs BCS class-III agent.
The SR tablets of Doxofylline were prepared employing different
concentrations of HPMC K100M and Chitosan in different
combinations by Direct Compression technique using 32 factorial
design. The concentration of Polymers, HPMC K100M and
Chitosan required to achieve the desired drug release was selected as
independent variables, X1 and X2 respectively whereas, time required
for 10% of drug dissolution (t10%), 50% (t50%), 75% (t75%) and 90%
(t90%) were selected as dependent variables. Totally nine formulations
were designed, Formulated and are evaluated for hardness, friability,
thickness, % drug content, In-vitro drug release. From the Results
it was concluded that all the formulation were found to be with
in the Pharmacopoeial limits and the In-vitro dissolution profiles
of all formulations were fitted in to different Kinetic models, the
statistical parameters like intercept, slope & regression coefficient
were calculated. Polynomial equations were developed for t10%,
t50%, t75%, t90%. Validity of developed polynomial equations were
verified by designing 2 check point formulations (C1, C2). According
to SUPAC guidelines the formulation (F4) containing combination
of 10% HPMC K100M and 15% Chitosan, is the most similar
formulation (similarity factor f2= 64.501, dissimilarity factor f1=
6.862 & No significant difference, t= 0.23001) to marketed product
(DOXOLIN). The selected formulation (F4) follows Zero order,
Higuchi’s kinetics, and the mechanism of drug release was found to be Non-Fickian Diffusion anomalous Super Case-II Transport (n= 0.963).
Formulation and evaluation of matrix type rosuvastatin sustained release tabletspharmaindexing
This document describes the formulation and evaluation of matrix-type sustained release tablets of rosuvastatin. Tablets were prepared using polymers like HPMC K15M, HPMC K50M, and ethylcellulose by direct compression technique. The tablets were evaluated for characteristics like hardness, thickness, friability, weight variation, drug content, and floating properties. The best formulation was subjected to kinetic treatment and was found to follow zero order, first order, Peppas, Higuchi, and Hixson-Crowell kinetics. The optimized batches were stable for 2 months at 40°C/75% RH conditions. The document provides details on various sustained release drug delivery systems, techniques for tablet formulation like direct compression
Matrix dosage forms in pharmaceutics (pharmaceutical dosage forms)YashYuvaraj
various sources from#detail of matrix dosage forms!!
1formulative pharmacy and biopharmaceutics
@pharmaceutical dosage forms
department of pharmaceutics
This document describes the formulation development and evaluation of simvastatin sustained release tablets. A 32 full factorial design was used to investigate the effect of two polymers, HPMCK4M and SCMC, on drug release times (t10%, t50%, t75%, t90%). Nine formulations were prepared according to the design and evaluated for properties like hardness, friability, thickness, drug content, and in-vitro drug release. Polynomial equations were developed relating the polymer concentrations to drug release times. The formulation containing 17.5% HPMCK4M and 30% SCMC (F4) showed drug release most similar to the marketed product and followed zero-order kinetics and non-Fickian diffusion mechanisms.
Formulation And Evaluation of Mucoadhesive Tablets of Carvedilol Using Natura...Nausheen Fatima
This document summarizes the formulation and evaluation of mucoadhesive tablets containing carvedilol using natural binders such as chitosan and guar gum. Eight formulations of carvedilol mucoadhesive tablets were prepared using different polymer ratios and evaluated for properties such as drug release, swelling, mucoadhesion and compatibility. The optimized formulation F4 containing carvedilol, Carbopol 940P, chitosan in a 3:1 ratio showed maximum drug release of 92% over 7 hours, highest swelling of 62% after 6 hours, and greatest mucoadhesive strength of 0.95N. The results suggest this optimized formulation can prolong drug release and potentially enhance bioavailability by adhering to the bucc
Formulation and Evaluation of Enalapril Maleate SR Matrix TabletsBhaswat Chakraborty
1. The study developed and evaluated sustained release matrix tablets of enalapril maleate using HPMC KM and HPMC K15 M polymers by wet granulation.
2. In vitro drug release studies showed that formulations F9 and F10 best matched the target release profile, releasing drug over 5 hours.
3. Kinetic modeling showed that drug release from the HPMC matrices followed Higuchi kinetics, indicating that the release mechanism involved both diffusion and erosion of the polymer matrices.
The document discusses novel drug delivery systems. It describes various targeted, controlled, and modulated drug delivery systems. It discusses different routes of administration including oral, pulmonary, injectable, infusion, ocular, nasal, topical, implantable, transmucosal, transdermal, and others. It also describes carrier types such as nanoparticles, liposomes, microspheres, and monoclonal antibodies. Finally, it provides details on some specific delivery methods and technologies.
ABSTRACT
Hyperglycemia is the technical term for high blood glucose (sugar). It
happens when the body has too little or not enough insulin or when the
body can‘t use insulin properly. The main objective of the present
research work was to develop a bilayer tablet of immediate release
Pioglitazone and controlled release Metformin Hydrochloride, which is
used as an Anti-hyperglycemic agent. Metformin Hydrochloride has
biological half-life nearly about 6 hours, so, an attempt was made in
the direction of preparation and optimization of a combination of
sustained release and immediate release in a single tablet. In controlled
release layer natural gums like xanthum gum, gum trgacanth and guar
gum were used as retarding materials and in immediate release laye
croscarmellose sodium was used as a superdisintegrent to give the faster release of
pioglitazone. The tablets were prepared by wet granulation method and by direct
compression. Granules were evaluated for precompression parameters and the tablets were
evaluated for post compression parameters.
Key Words: Bilayer tablets, Metformin Hydrochloride, pioglitazone, xanthum gum, guar
gum, gum tragacanth and crosscarmellose sodium.
Objective: The purpose of the present research investigation was to formulate sustained release (SR) formulations for
losartan potassium using 32
factorial designs. Methods: Losartan potassium is an antihypertensive agent, non-peptide
angiotensin-II receptor (type AT1) blocker, and BCS class-III agent. SR tablet formulations of losartan potassium were
formulated using variable quantities of hydroxymethyl propyl cellulose (HPMC) K100M and xanthan gum in combinations
by direct compression technique. The amount of polymers, HPMC K100M, and xanthan gum required to achieve the drug
release was selected as independent variables, X1
and X2
, respectively, whereas time required to release 10% (t10%), 50%
(t50%), 75% (t75%), and 90% (t90%) of drug from formulation was selected as dependent variables. Nine formulations were
prepared and evaluated for various pharmacopoeial tests. Results: The results reveal that all formulations were found to be
with in the pharmacopoeial limits and in vitro drug release profiles of all formulations were subjected to kinetic modeling.
The statistical parameters such as intercept, slope, and correlation coefficient were determined. Polynomial equations were
developed for dependent variables. Validity of developed polynomial equations was checked by designing two checkpoint
formulations (C1
and C2
). According to SUPAC guidelines, formulation (F4
) containing mixture of 15% HPMC K100M
and 20% xanthan gum is the most identical formulation (similarity factor f2 = 86.747, dissimilarity factor f1 = 1.760, and no
significant difference, t = 0.0477) to marketed product (LOSACAR). Conclusion: Best Formulation F4 follows the first-order,
Higuchi kinetics, and the mechanism of drug release was found to be non-Fickian diffusion anomalous transport (n = 0.825).
KEY WORDS: 32 factorial design, First-order kinetics, Hydroxymethyl propyl cellulose K100M, Losartan potassium,
Non-fickian diffusion mechanism, Sustained release tablet, Xanthan gum
Formulation and Evaluation of Gabapentin Mucoadhesive Gastro Retentive Tablets.pharmaindexing
This document describes the formulation and evaluation of gabapentin mucoadhesive gastroretentive tablets. Various tablet formulations were prepared using different concentrations of mucoadhesive polymers like carbopol 934P, sodium CMC, and sodium alginate. The tablets were evaluated for parameters like thickness, weight variation, hardness, drug content, swelling index, and mucoadhesive strength. In vitro drug release studies showed that a formulation containing 0.5% carbopol 934P (F-IV) exhibited slowest drug release over 12 hours compared to other formulations. Stability studies of F-IV showed no significant changes in properties after 3 months of storage. The study concluded that mucoadhesive polymers can help
Formulation development and evalution of matrix tablet ofGajanan Ingole
The document describes the development of a matrix tablet for oral delivery of an antihypertensive drug (NSL) using pH dependent and independent polymers. It includes sections on introduction, literature review, drug and excipient profiles, aim and objectives, rationale, materials and equipment, experimental work, results, discussion, and references. The key steps involved preformulation studies, formulation of matrix tablets, optimization studies to match the in vitro dissolution profile of a marketed reference product, and stability studies. The optimized formulation was found to release the drug in a controlled manner for 24 hours.
Formulation and Development of Matrix tablet In Drug Delivery SystemSayan Pramanik
Formulation and Development of Matrix tablet In Drug Delivery System | What is matrix tablet | merits & demerits | Classification | formulation | Evaluation |
ABSTRACT
The main objective of present investigation is to formulate the sustained release tablet of Zidovudine using 32
factorial design. Zidovudine, antiretroviral drug belongs to BCS Class I. The SR tablets of Zidovudine were
prepared employing different concentrations of Carboplol974P and Xanthan gum in different combinations as a
rate retardants by Direct Compression technique using 32 factorial design. The quantity of rate retarders,
Carboplol974P and Xanthan gum required to achieve the desired drug release was selected as independent
variables, X1 and X2 respectively whereas, time required for 10% of drug dissolution (t10%), 50% (t50%), 75% (t75%)
and 90% (t90%) were selected as dependent variables. Totally nine formulations were designed and are evaluated
for hardness, friability, thickness, % drug content, In-vitro drug release. From the Results it was concluded that all
the formulation were found to be with in the Pharmacopoeial limits and the In-vitro dissolution profiles of all
formulations were fitted in to different Kinetic models, the statistical parameters like intercept (a), slope (b) &
regression coefficient (r) were calculated. Polynomial equations were developed for t10%, t50%, t75%, t90%. Validity of
developed polynomial equations were verified by designing 2 check point formulations(C1, C2). According to
SUPAC guidelines the formulation (F5) containing combination of 5% Carboplol974P and 5% Xanthan gum, is the
most similar formulation (f2=85.04 & No significant difference, t= 0.20046) to marketed product (Retrovir). The
selected formulation (F5) follows Higuchi’s kinetics, the mechanism of drug release was found to be Case-II
transport or typical Zero order release (Non-Fickian, n= 0.915).
Advance Techniques of Bilayer tablet: A Reviewpharmaindexing
This document discusses bilayer tablets, which provide controlled release of two drugs or different release profiles of a single drug. It describes several techniques for developing bilayer tablets, including OROS push-pull technology, L-OROS technology, ENSO TROL technology, and DUROS technology. It also discusses Elan Drug Technologies' DUREDAS bilayer tablet technology, which can provide immediate or sustained release from two layers in a single dosage form for tailored drug release. Bilayer tablets offer advantages like separating incompatible drugs, modifying drug release surfaces, and administering fixed-dose drug combinations.
ABSTRACT
Objective: The main objective of present investigation is to formulate the controlled release tablet of Lamivudine using 3² factorial design. Lamivudine, a basic molecule and antiretroviral drug belongs to BCS Class III, having low permeability and high solubility. Methods: The controlled release tablets of lamivudine were prepared employing different concentrations of Carboplol974P and Xanthan gum in different combinations as a rate retarding agent by Direct Compression technique using 32 factorial design. The quantity/ concentration of rate retarders, Carboplol974P and Xanthan gum required to achieve the desired drug release was selected as independent variables, X1 and X2 respectively whereas, time required for 10% of drug dissolution t10%, t50%, t75%,t90% were selected as dependent variables. Results: Totally nine formulations were designed and are evaluated for hardness, friability, thickness, % drug content, in-vitro drug release. From the results it was concluded that all the formulation were found to be with in the pharmacopoeial limits and the in-vitro dissolution profiles of all formulations were fitted in to different Kinetic models, the statistical parameters like intercept (a), slope (b) & regression coefficient (r) were calculated. Polynomial equations were developed for t10%, t50%, t75%,t90%. Conclusions: According to SUPAC guidelines the formulation (F5) containing combination of 10% Carboplol974P and 10% Xanthan gum, is the most similar formulation (similarity factor f2=85.04 & No significant difference, t= 0.20046) to Innovator product (Lamivir). The selected formulation (F5) follows Higuchi’s kinetics, and the mechanism of drug release was found to be Case-II transport or typical Zero order release (Non-Fickian, n= 0.915).
Objective: The purpose of present research work is to develop the sustained release formulation for Telmisartan using 32 factorial design. Telmisartan an Antihypertensive agent, nonpeptide angiotensin-II receptor (type AT1) antagonist and BCS class-II agent. Methods: Sustained Release tablet formulations of Telmisartan were prepared using different quantities of HPMCK100M and Xanthan Gum in combinations by direct compression technique. The concentration of Polymers, HPMCK100M and Xanthan gum required to achieve the drug release was selected as independent variables, X1 and X2 respectively whereas, time required for 10% of drug release (t10%), 50% (t50%), 75% (t75%) and 90% (t90%) were selected as dependent variables. Nine formulations were prepared and are evaluated for various pharmacopoeial tests. Results: The results reveals that all formulations were found to be with in the pharmacopoeial limits and In vitro drug release profiles of all formulations were fitted in to various Kinetic models. The statistical parameters like intercept, slope & correlation coefficient were calculated. Polynomial equations were developed for dependent variables. Validity of developed polynomial equations were checked by designing 2 check point formulations (C1, C2). Conclusion: According to SUPAC guidelines formulation (F5) containing combination of 15% HPMCK100M and 15% Xanthan gum, is the most identical formulation (similarity factor f2= 90.863, dissimilarity factor f1= 1.665 & No significant difference, t= 0.03379) to marketed product (TELVAS). Best Formulation F5 follows First order, Higuchi’s kinetics, and the mechanism of drug release was found to be Non-Fickian Diffusion Anomalous Transport. (n= 0.828).
Formulation, Development and Evaluation of Uncoated Bi-layer Tablet of Anti-H...Mohanish Shah
This document presents work on developing a bilayer tablet containing metoprolol succinate and hydrochlorothiazide for the treatment of hypertension. The bilayer tablet uses Dual Release Drug Absorption System (DUREDAS) technology to provide sustained release of metoprolol from one layer and immediate release of hydrochlorothiazide from the other layer. Preliminary studies were conducted to select polymers for the sustained release layer and superdisintegrants for the immediate release layer. Calibration curves were developed for both drugs alone and in combination. Materials and equipment used in the experimental work are listed.
Fundamental concept of modified drug releaseAbhinayJha3
Different Terminologies used in a modified release
1. Sustained release
2. Delayed release
3. Prolonged release
4. Extended-release
5. Controlled release
6. Site-specific targeting and receptor targeting
SELECTION OF DRUG CANDIDATE FOR ORAL SUSTAINED RELEASE SYSTEMS, BIOPHARMACEUTICAL CLASSIFICATION SYSTEM.
Cuento metafórico de Isabelle Carrier, que a través de palabras e ilustraciones simples, habla de la superación de un niño con dificultades para sobrellevar el día a día.
El documento resume las posiciones del PP y PSOE sobre posibles sanciones a sus militantes implicados en el caso de las tarjetas opacas de Caja Madrid, incluyendo la posible expulsión de Rodrigo Rato del PP. El PP ha abierto expedientes a todos los afiliados implicados y no descarta expulsar a Rato. El PSOE anuncia una decisión "inminente y contundente" sobre sus militantes. Ambos partidos sienten la indignación pública y prometen ir hasta las últimas consecuencias.
Formulation and evaluation of matrix type rosuvastatin sustained release tabletspharmaindexing
This document describes the formulation and evaluation of matrix-type sustained release tablets of rosuvastatin. Tablets were prepared using polymers like HPMC K15M, HPMC K50M, and ethylcellulose by direct compression technique. The tablets were evaluated for characteristics like hardness, thickness, friability, weight variation, drug content, and floating properties. The best formulation was subjected to kinetic treatment and was found to follow zero order, first order, Peppas, Higuchi, and Hixson-Crowell kinetics. The optimized batches were stable for 2 months at 40°C/75% RH conditions. The document provides details on various sustained release drug delivery systems, techniques for tablet formulation like direct compression
Matrix dosage forms in pharmaceutics (pharmaceutical dosage forms)YashYuvaraj
various sources from#detail of matrix dosage forms!!
1formulative pharmacy and biopharmaceutics
@pharmaceutical dosage forms
department of pharmaceutics
This document describes the formulation development and evaluation of simvastatin sustained release tablets. A 32 full factorial design was used to investigate the effect of two polymers, HPMCK4M and SCMC, on drug release times (t10%, t50%, t75%, t90%). Nine formulations were prepared according to the design and evaluated for properties like hardness, friability, thickness, drug content, and in-vitro drug release. Polynomial equations were developed relating the polymer concentrations to drug release times. The formulation containing 17.5% HPMCK4M and 30% SCMC (F4) showed drug release most similar to the marketed product and followed zero-order kinetics and non-Fickian diffusion mechanisms.
Formulation And Evaluation of Mucoadhesive Tablets of Carvedilol Using Natura...Nausheen Fatima
This document summarizes the formulation and evaluation of mucoadhesive tablets containing carvedilol using natural binders such as chitosan and guar gum. Eight formulations of carvedilol mucoadhesive tablets were prepared using different polymer ratios and evaluated for properties such as drug release, swelling, mucoadhesion and compatibility. The optimized formulation F4 containing carvedilol, Carbopol 940P, chitosan in a 3:1 ratio showed maximum drug release of 92% over 7 hours, highest swelling of 62% after 6 hours, and greatest mucoadhesive strength of 0.95N. The results suggest this optimized formulation can prolong drug release and potentially enhance bioavailability by adhering to the bucc
Formulation and Evaluation of Enalapril Maleate SR Matrix TabletsBhaswat Chakraborty
1. The study developed and evaluated sustained release matrix tablets of enalapril maleate using HPMC KM and HPMC K15 M polymers by wet granulation.
2. In vitro drug release studies showed that formulations F9 and F10 best matched the target release profile, releasing drug over 5 hours.
3. Kinetic modeling showed that drug release from the HPMC matrices followed Higuchi kinetics, indicating that the release mechanism involved both diffusion and erosion of the polymer matrices.
The document discusses novel drug delivery systems. It describes various targeted, controlled, and modulated drug delivery systems. It discusses different routes of administration including oral, pulmonary, injectable, infusion, ocular, nasal, topical, implantable, transmucosal, transdermal, and others. It also describes carrier types such as nanoparticles, liposomes, microspheres, and monoclonal antibodies. Finally, it provides details on some specific delivery methods and technologies.
ABSTRACT
Hyperglycemia is the technical term for high blood glucose (sugar). It
happens when the body has too little or not enough insulin or when the
body can‘t use insulin properly. The main objective of the present
research work was to develop a bilayer tablet of immediate release
Pioglitazone and controlled release Metformin Hydrochloride, which is
used as an Anti-hyperglycemic agent. Metformin Hydrochloride has
biological half-life nearly about 6 hours, so, an attempt was made in
the direction of preparation and optimization of a combination of
sustained release and immediate release in a single tablet. In controlled
release layer natural gums like xanthum gum, gum trgacanth and guar
gum were used as retarding materials and in immediate release laye
croscarmellose sodium was used as a superdisintegrent to give the faster release of
pioglitazone. The tablets were prepared by wet granulation method and by direct
compression. Granules were evaluated for precompression parameters and the tablets were
evaluated for post compression parameters.
Key Words: Bilayer tablets, Metformin Hydrochloride, pioglitazone, xanthum gum, guar
gum, gum tragacanth and crosscarmellose sodium.
Objective: The purpose of the present research investigation was to formulate sustained release (SR) formulations for
losartan potassium using 32
factorial designs. Methods: Losartan potassium is an antihypertensive agent, non-peptide
angiotensin-II receptor (type AT1) blocker, and BCS class-III agent. SR tablet formulations of losartan potassium were
formulated using variable quantities of hydroxymethyl propyl cellulose (HPMC) K100M and xanthan gum in combinations
by direct compression technique. The amount of polymers, HPMC K100M, and xanthan gum required to achieve the drug
release was selected as independent variables, X1
and X2
, respectively, whereas time required to release 10% (t10%), 50%
(t50%), 75% (t75%), and 90% (t90%) of drug from formulation was selected as dependent variables. Nine formulations were
prepared and evaluated for various pharmacopoeial tests. Results: The results reveal that all formulations were found to be
with in the pharmacopoeial limits and in vitro drug release profiles of all formulations were subjected to kinetic modeling.
The statistical parameters such as intercept, slope, and correlation coefficient were determined. Polynomial equations were
developed for dependent variables. Validity of developed polynomial equations was checked by designing two checkpoint
formulations (C1
and C2
). According to SUPAC guidelines, formulation (F4
) containing mixture of 15% HPMC K100M
and 20% xanthan gum is the most identical formulation (similarity factor f2 = 86.747, dissimilarity factor f1 = 1.760, and no
significant difference, t = 0.0477) to marketed product (LOSACAR). Conclusion: Best Formulation F4 follows the first-order,
Higuchi kinetics, and the mechanism of drug release was found to be non-Fickian diffusion anomalous transport (n = 0.825).
KEY WORDS: 32 factorial design, First-order kinetics, Hydroxymethyl propyl cellulose K100M, Losartan potassium,
Non-fickian diffusion mechanism, Sustained release tablet, Xanthan gum
Formulation and Evaluation of Gabapentin Mucoadhesive Gastro Retentive Tablets.pharmaindexing
This document describes the formulation and evaluation of gabapentin mucoadhesive gastroretentive tablets. Various tablet formulations were prepared using different concentrations of mucoadhesive polymers like carbopol 934P, sodium CMC, and sodium alginate. The tablets were evaluated for parameters like thickness, weight variation, hardness, drug content, swelling index, and mucoadhesive strength. In vitro drug release studies showed that a formulation containing 0.5% carbopol 934P (F-IV) exhibited slowest drug release over 12 hours compared to other formulations. Stability studies of F-IV showed no significant changes in properties after 3 months of storage. The study concluded that mucoadhesive polymers can help
Formulation development and evalution of matrix tablet ofGajanan Ingole
The document describes the development of a matrix tablet for oral delivery of an antihypertensive drug (NSL) using pH dependent and independent polymers. It includes sections on introduction, literature review, drug and excipient profiles, aim and objectives, rationale, materials and equipment, experimental work, results, discussion, and references. The key steps involved preformulation studies, formulation of matrix tablets, optimization studies to match the in vitro dissolution profile of a marketed reference product, and stability studies. The optimized formulation was found to release the drug in a controlled manner for 24 hours.
Formulation and Development of Matrix tablet In Drug Delivery SystemSayan Pramanik
Formulation and Development of Matrix tablet In Drug Delivery System | What is matrix tablet | merits & demerits | Classification | formulation | Evaluation |
ABSTRACT
The main objective of present investigation is to formulate the sustained release tablet of Zidovudine using 32
factorial design. Zidovudine, antiretroviral drug belongs to BCS Class I. The SR tablets of Zidovudine were
prepared employing different concentrations of Carboplol974P and Xanthan gum in different combinations as a
rate retardants by Direct Compression technique using 32 factorial design. The quantity of rate retarders,
Carboplol974P and Xanthan gum required to achieve the desired drug release was selected as independent
variables, X1 and X2 respectively whereas, time required for 10% of drug dissolution (t10%), 50% (t50%), 75% (t75%)
and 90% (t90%) were selected as dependent variables. Totally nine formulations were designed and are evaluated
for hardness, friability, thickness, % drug content, In-vitro drug release. From the Results it was concluded that all
the formulation were found to be with in the Pharmacopoeial limits and the In-vitro dissolution profiles of all
formulations were fitted in to different Kinetic models, the statistical parameters like intercept (a), slope (b) &
regression coefficient (r) were calculated. Polynomial equations were developed for t10%, t50%, t75%, t90%. Validity of
developed polynomial equations were verified by designing 2 check point formulations(C1, C2). According to
SUPAC guidelines the formulation (F5) containing combination of 5% Carboplol974P and 5% Xanthan gum, is the
most similar formulation (f2=85.04 & No significant difference, t= 0.20046) to marketed product (Retrovir). The
selected formulation (F5) follows Higuchi’s kinetics, the mechanism of drug release was found to be Case-II
transport or typical Zero order release (Non-Fickian, n= 0.915).
Advance Techniques of Bilayer tablet: A Reviewpharmaindexing
This document discusses bilayer tablets, which provide controlled release of two drugs or different release profiles of a single drug. It describes several techniques for developing bilayer tablets, including OROS push-pull technology, L-OROS technology, ENSO TROL technology, and DUROS technology. It also discusses Elan Drug Technologies' DUREDAS bilayer tablet technology, which can provide immediate or sustained release from two layers in a single dosage form for tailored drug release. Bilayer tablets offer advantages like separating incompatible drugs, modifying drug release surfaces, and administering fixed-dose drug combinations.
ABSTRACT
Objective: The main objective of present investigation is to formulate the controlled release tablet of Lamivudine using 3² factorial design. Lamivudine, a basic molecule and antiretroviral drug belongs to BCS Class III, having low permeability and high solubility. Methods: The controlled release tablets of lamivudine were prepared employing different concentrations of Carboplol974P and Xanthan gum in different combinations as a rate retarding agent by Direct Compression technique using 32 factorial design. The quantity/ concentration of rate retarders, Carboplol974P and Xanthan gum required to achieve the desired drug release was selected as independent variables, X1 and X2 respectively whereas, time required for 10% of drug dissolution t10%, t50%, t75%,t90% were selected as dependent variables. Results: Totally nine formulations were designed and are evaluated for hardness, friability, thickness, % drug content, in-vitro drug release. From the results it was concluded that all the formulation were found to be with in the pharmacopoeial limits and the in-vitro dissolution profiles of all formulations were fitted in to different Kinetic models, the statistical parameters like intercept (a), slope (b) & regression coefficient (r) were calculated. Polynomial equations were developed for t10%, t50%, t75%,t90%. Conclusions: According to SUPAC guidelines the formulation (F5) containing combination of 10% Carboplol974P and 10% Xanthan gum, is the most similar formulation (similarity factor f2=85.04 & No significant difference, t= 0.20046) to Innovator product (Lamivir). The selected formulation (F5) follows Higuchi’s kinetics, and the mechanism of drug release was found to be Case-II transport or typical Zero order release (Non-Fickian, n= 0.915).
Objective: The purpose of present research work is to develop the sustained release formulation for Telmisartan using 32 factorial design. Telmisartan an Antihypertensive agent, nonpeptide angiotensin-II receptor (type AT1) antagonist and BCS class-II agent. Methods: Sustained Release tablet formulations of Telmisartan were prepared using different quantities of HPMCK100M and Xanthan Gum in combinations by direct compression technique. The concentration of Polymers, HPMCK100M and Xanthan gum required to achieve the drug release was selected as independent variables, X1 and X2 respectively whereas, time required for 10% of drug release (t10%), 50% (t50%), 75% (t75%) and 90% (t90%) were selected as dependent variables. Nine formulations were prepared and are evaluated for various pharmacopoeial tests. Results: The results reveals that all formulations were found to be with in the pharmacopoeial limits and In vitro drug release profiles of all formulations were fitted in to various Kinetic models. The statistical parameters like intercept, slope & correlation coefficient were calculated. Polynomial equations were developed for dependent variables. Validity of developed polynomial equations were checked by designing 2 check point formulations (C1, C2). Conclusion: According to SUPAC guidelines formulation (F5) containing combination of 15% HPMCK100M and 15% Xanthan gum, is the most identical formulation (similarity factor f2= 90.863, dissimilarity factor f1= 1.665 & No significant difference, t= 0.03379) to marketed product (TELVAS). Best Formulation F5 follows First order, Higuchi’s kinetics, and the mechanism of drug release was found to be Non-Fickian Diffusion Anomalous Transport. (n= 0.828).
Formulation, Development and Evaluation of Uncoated Bi-layer Tablet of Anti-H...Mohanish Shah
This document presents work on developing a bilayer tablet containing metoprolol succinate and hydrochlorothiazide for the treatment of hypertension. The bilayer tablet uses Dual Release Drug Absorption System (DUREDAS) technology to provide sustained release of metoprolol from one layer and immediate release of hydrochlorothiazide from the other layer. Preliminary studies were conducted to select polymers for the sustained release layer and superdisintegrants for the immediate release layer. Calibration curves were developed for both drugs alone and in combination. Materials and equipment used in the experimental work are listed.
Fundamental concept of modified drug releaseAbhinayJha3
Different Terminologies used in a modified release
1. Sustained release
2. Delayed release
3. Prolonged release
4. Extended-release
5. Controlled release
6. Site-specific targeting and receptor targeting
SELECTION OF DRUG CANDIDATE FOR ORAL SUSTAINED RELEASE SYSTEMS, BIOPHARMACEUTICAL CLASSIFICATION SYSTEM.
Cuento metafórico de Isabelle Carrier, que a través de palabras e ilustraciones simples, habla de la superación de un niño con dificultades para sobrellevar el día a día.
El documento resume las posiciones del PP y PSOE sobre posibles sanciones a sus militantes implicados en el caso de las tarjetas opacas de Caja Madrid, incluyendo la posible expulsión de Rodrigo Rato del PP. El PP ha abierto expedientes a todos los afiliados implicados y no descarta expulsar a Rato. El PSOE anuncia una decisión "inminente y contundente" sobre sus militantes. Ambos partidos sienten la indignación pública y prometen ir hasta las últimas consecuencias.
This certificate of completion was presented to Vitaly Glotov on October 30, 2015 for a course in facilitation tools and techniques. The certificate recognizes Vitaly Glotov's completion of training in facilitation skills.
El documento describe las redes sociales más populares actualmente, incluyendo Facebook, Google+, YouTube, Twitter, Instagram, Tumblr y Badoo. Explica que Facebook sigue siendo la red social más exitosa y popular para conectar personas, mientras que Google+ y YouTube son populares para compartir contenido. Twitter es importante para comunicación en tiempo real y noticias actualizadas, e Instagram y Tumblr son populares para compartir fotos y publicaciones cortas. Finalmente, Badoo se enfoca en encontrar amigos o parejas.
- The document presents the results of the second round of the 2015 Argentine general election for President and Vice President. It shows the vote counts for each candidate's formula in each province and in elections abroad.
- The winner was Mauricio Macri's formula with Cambiemos, which received 12,997,937 votes (51.34%) compared to 12,317,330 votes (48.66%) for Daniel Scioli's formula with Frente para la Victoria.
- A total of 25,952,906 votes were counted across the country and abroad, with 330,988 considered null votes.
Aim of the study: The objective of present study is to report a rare Case of contact dermatitis that was seen in 30 years old female from Narasaraopet of Guntur district, South India. Place of study: This case was studied in the outpatient department of Dermatology, Guntur City Hospital, Guntur. Period of Study: This case was studied and investigated in detail in the month of May 2014 in the above hospital. Case Report: A young female aged 30years came with past history of Hyperthyroidism for the past 11months and Obese. She needed support to have food. On examination she had Hoarse throat, Body pains Irregular periods .along with this on application of Raw Garlic for pimples turned into Contact Dermatitis. This study was compared and well correlated with available literature. Conclusion: Since this is a rare case of Garlic Induced Hypersensitivity reaction made us interesting to study.
Los eventos masivos a menudo requieren vigilancia privada para mantener el orden y la seguridad de los asistentes, ya que el gobierno no siempre puede proporcionar esta cobertura. La seguridad privada ayuda a controlar posibles caos, brindando a los asistentes una sensación de seguridad y bienestar para que puedan disfrutar del evento de manera tranquila y responsable.
The document discusses the formulation and evaluation of an artemether sustained release floating bilayer tablet. It aims to develop a floating drug delivery system for artemether to increase its gastric residence time and provide sustained release to ensure optimal drug levels in the blood and minimize side effects. The document provides background on floating drug delivery systems and reviews previous literature on developing such systems for other drugs. It then gives information on the drug artemether and outlines the objectives and methodology that will be used in the study.
The main aim of present research study is to formulate the floating tablets of Labetalol HCl using 32 factorial design. Labetalol HCl, non selective α, -β- adreno receptor antagonist, Indicated for treatment of Hypertension/moderate Heart Failure. The Floating tablets of Labetalol HCl were prepared employing different concentrations of HPMCK4M and sodium bicarbonate in different combinations by Direct Compression technique. The concentration of HPMCK4M and sodium bicarbonate required to achieve desired drug release was selected as independent variables, X1 and X2 respectively whereas, time required for 10% of drug dissolution (t10%), 50% (t50%), 75% (t75%) and 90% (t90%) were selected as dependent variables. 9 formulations were designed and are evaluated for hardness, friability, thickness, % drug content, Floating Lag time, In-vitro drug release. From the Results concluded that all the formulation were found to be within the Pharmacopoeial limits and the In-vitro dissolution profiles of all formulations were fitted in to different Kinetic models, the statistical parameters like intercept, slope & regression coefficient were calculated. Polynomial equations were developed for t10%, t50%, t75%, t90%. Validity of developed polynomial equations were verified by designing 2 check point formulations. According to SUPAC guidelines the formulation (F8) containing combination of 20% HPMCK4M and 3.75% sodium bicarbonate, is the most identical formulation which meets the objective of work. The selected formulation (F8) follows Higuchi’s kinetics, and the mechanism of drug release was found to be NonFickian Diffusion (n= 1.033, Super Case-II transport).
Design of gastroretentive bilayer floating films of propranolol hydrochloride...Namdeo Shinde
This document summarizes a research study on the design of bilayer floating films for delivery of propranolol hydrochloride and rosuvastatin calcium. The study aimed to develop a single dosage form to provide therapeutic effects for hypertension and hyperlipidemia simultaneously. Various polymers and plasticizers were evaluated for their effects on film properties and drug release. Bilayer films were prepared using solvent casting method, with an immediate release layer of rosuvastatin and a sustained release layer of propranolol. The films were characterized for drug content, floating behavior, drug release and stability studies. The bilayer floating film system showed potential for gastroretention and controlled delivery of both drugs for cardiovascular diseases.
Formulation and Evaluation of Floating Tablet of Metoprolol Succinateijtsrd
The aim of the present work is Formulation and Evaluation of Floating Tablet of Metoprolol Succinate. Metoprolol Succinate is a BCS class I drug used in the treatment of Angina pectoric, Heart attack, Hypertension and has short half life 3 7hours. In the present study it was planned to prepare sustained release floating tablets of Metoprolol succinate by using HPMC E5 and Gum Karaya excipients. The procured sample of drug was authenticated by pre formulation study like melting point, IR spectra, UV analysis were done. Results of pre formulation studies show that Metoprolol Succinate was pure and complies with standard. Prior to compression, the powder blend were evaluated for angle of repose, bulk density, tapped density, compressibility index, Hausners ratio. Results of pre formulation studies show that Metoprolol Succinate was pure and complies with standard. Formulations were evaluated for various evaluation parameters like hardness, thickness, weight variation, friability, drug content, floating lag time, floating time, swelling index and in vitro drug release. From the results of evaluation parameters it was observed that formulation F6 shows best results for floating lag time 4min floating time up to 12 hours and consistent drug release 96.15 as compared to other formulations. So formulation F6 was finalized as a optimized formulation for further study. On the basic of above finding it was concluded that sustained release floating drug delivery system was successfully achieved. Neeta. V. Jadhav | Prof. Mr. Prashant Khade | Dr. Ashok Bhosale "Formulation and Evaluation of Floating Tablet of Metoprolol Succinate" Published in International Journal of Trend in Scientific Research and Development (ijtsrd), ISSN: 2456-6470, Volume-6 | Issue-5 , August 2022, URL: https://www.ijtsrd.com/papers/ijtsrd50409.pdf Paper URL: https://www.ijtsrd.com/pharmacy/pharmaceutics/50409/formulation-and-evaluation-of-floating-tablet-of-metoprolol-succinate/neeta-v-jadhav
In recent years many advancement has been made in research and development of Oral Drug Delivery System. Concept of Novel Drug Delivery System arose to overcome the certain aspect related to physicochemical properties of drug molecule and the related formulations.
Purpose of this review is to compile the recent literature with special focus on Gastro Retentive Drug Delivery Systems to give an update
on pharmaceutical approaches used in enhancing the Gastric Residence Time (GRT). Various approaches are currently used including Gastro Retentive Floating Drug Delivery Systems(GRFDDS),swelling and expanding system, polymeric bioadhesive systems, modifiedshape
systems, high density system and other delayed gastric emptying devices. These systems are very helpful to different problem solve during the formulation of different dosage form. The present work also focuses on the polymers used in floating drug delivery systems
mostly from natural origin. Floating drug delivery systems are less dense than gastric fluids; hence remain buoyant in the upper GIT for a
prolonged period, releasing the drug at the desired/ predeterminedrate. This review article focuses on the recent technological development in floating drug delivery systems with special emphasis on the principal mechanism of floatation and advantages of achieving gastric
retention, brief collection on various polymers employed for floating drug delivery systems etc. In addition this review also summarizes the In –Vitro and In -Vivo studies to evaluate their performance and also their future potential.
Formulation and Evaluation of Gastroretentive Drug Delivery System of Repagli...BRNSSPublicationHubI
This document discusses the formulation and evaluation of a gastroretentive drug delivery system for repaglinide. It begins with an introduction that outlines the advantages of novel drug delivery systems and gastroretentive formulations. It then provides details on the materials and methods used, including the preformulation, formulation, characterization, and evaluation of floating microspheres loaded with repaglinide. The goals of the research were to develop a gastroretentive delivery system for repaglinide to achieve prolonged gastric retention and controlled drug release in the stomach.
MICROBALLOONS: A NOVEL APPROACH IN GASTRO-RETENTION FLOATING DRUG DELIVERY SY...Snehal Patel
ABSTRACT
Oral controlled release dosage forms face several physiological restriction like inability to retain
and position the controlled drug delivery system within the targeted region of the gastrointestinal
tract (GIT) due to fluctuation in gastric emptying. This results in non uniform absorption
pattern, inadequate medication release and shorter residence time of the dosage form in the
stomach. As the fallout of this episode there is inadequate absorption of the drug having
absorption window predominantly, in the upper area of GIT. These contemplations have
provoked to the development of oral controlled release dosage forms with gastroretentive
properties. Microballoons (Hollow microspheres) hold certification as one of the potential
approaches for gastric retention. Microballoons are spherical empty particles without core and
can remain in the gastric region for delayed periods. They significantly increase the gastric
residence time of medication, thereby enhance bioavailability, improves patient compliance by
reducing dosing frequency, lessen the medication waste, enhance retention of medication which
solubilize only in stomach, enhance solubility for medications that are less soluble at a higher pH
environment. The present review preparation methods, characterization, advantages,
disadvantages, mechanism of drug release from microballoons, applications and list of the drugs
formulated as microballoons are discussed.
KEYWORDS: Microballoons, Gastro-retention, Floating drug delivery system (FDDS).
Background: The main objective of present research work is to formulate the Carbamazepine Fast Dissoving tablets. Carbamazepine, an
antiepileptic, belongs to BCS Class-II and used to control some types of seizures in the treatment of epilepsy and Neuropathic Pain by
blocking use-dependent sodium channels. Methods: The Fast Dissoving tablets of Carbamazepine were prepared employing different
concentrations of Crospovidone and Croscarmellose sodium in different combinations as a Sperdisintegrants by Direct Compression technique
using 32
factorial design. The concentration of Crospovidone and Croscarmellose sodium was selected as independent variables, X1
and X2 respectively whereas, wetting time, Disintegration time, t
50% ,t90%were selected as dependent variables. Results and Discussion:
Totally nine formulations were designed and are evaluated for hardness, friability, thickness, Assay, Wetting time, Disintegration time, Invitro
drug release. From the Results concluded that all the formulation were found to be with in the Pharmacopoeial limits and the In-vitro
dissolution profiles of all formulations were fitted in to different Kinetic models, the statistical parameters like intercept (a), slope (b) &
regression coefficient (r) were calculated. Polynomial equations were developed for Wetting time, Disintegration time, t50%, t90%. Validity of
developed polynomial equations were verified by designing 2 check point formulations (C1
, C2
). According to SUPAC guidelines the
formulation (F5
) containing combination of 9.375% Crospovidone and 9.375% Croscarmellose, is the most similar formulation (similarity factor
f
2
=82.675, dissimilarity factor f1
= 2.049 & No significant difference, t= 0.041) to marketed product (TEGRETOL-100). Conclusion: The
selected formulation (F5
) follows First order, Higuchi’s kinetics, mechanism of drug release was found to be Non-Fickian Diffusion (n= 0.665).
KEYWORDS: Carbamazepine, 3
2Factorial Design, Crospovidone , croscarmellose Sodium, Wetting Time, Disintegration Time.
The main objective of the present research work is to formulate the Clopidogrel Fast Dissolving tablets. Clopidogrel, an antiplatelet drug, belongs to BCS Class-II and used to control Heart attack, Hypertension by inhibiting Platelet activation and aggregation .The Fast Dissolving tablets of Clopidogrel were prepared employing different concentrations of Crospovidone and Croscarmellose sodium in different combinations as a Superdisintegrant by Direct Compression technique using 32 factorial design. The concentration of Crospovidone and Croscarmellose sodium was selected as independent variables, X1 and X2 respectively whereas, wetting time, Disintegration time, t50%, t90% were selected as dependent variables. Totally nine formulations were designed and evaluated for hardness, friability, thickness, Assay, Wetting time, Disintegration time, and in-vitro drug release. From the Results it was concluded that all the formulation were found to be with in the Pharmacopoeial limits and the in-vitro dissolution profiles of all formulations were fitted into different Kinetic models, the statistical parameters like intercept (a), slope (b) and regression coefficient (r) were calculated. Polynomial equations were developed for Wetting time, Disintegration time, t50%, t90%. Validity of developed polynomial equations was verified by designing 2 check point formulations (C1, C2). According to SUPAC guidelines, the formulation (F5) containing combination of 15% Crospovidone and 15% Croscarmellose, is the most similar formulation (similarity factor f2=91.3936, dissimilarity factor f1= 1.203& No significant difference, t= -0.00062) to marketed product (PLAVIX-75). The selected formulation (F1) follows First order, Higuchi’s kinetics, mechanism of drug release found to be Fickian Diffusion (n= 0.226).
The document describes a study that formulated and evaluated polymeric nanoparticles containing the antiviral drug acyclovir for prolonged retention in the stomach. Nanoparticles were prepared using different hydrophilic polymers including bovine serum albumin, chitosan, and gelatin. The nanoparticles were characterized for properties such as particle size, zeta potential, drug loading efficiency, and drug release. Nanoparticles prepared with chitosan in a 1:1 ratio with acyclovir showed a particle size of 312.04 nm, zeta potential of 33.2 mV, drug loading efficiency of 17.54%, and entrapment efficiency of 73.4%, indicating they may be suitable for gastric retention delivery of acyclovir.
This document provides an overview of floating drug delivery systems (FDDS). FDDS are low-density drug delivery systems that remain buoyant in the stomach without affecting gastric emptying rate, resulting in increased gastric retention time and better control of drug concentrations. FDDS are useful for drugs that need to be absorbed in the stomach or have a narrow absorption window in the upper gastrointestinal tract. The document discusses the advantages and disadvantages of FDDS, examples of commercially available FDDS formulations, and different types of FDDS including effervescent systems that use gas-generating agents and non-effervescent systems. It concludes that FDDS can enhance bioavailability for certain drugs but may not be suitable for all drugs depending on factors like
The document provides an overview of oral controlled release drug delivery systems. It discusses the anatomy and physiology related to oral drug administration. Some key advantages of controlled release oral dosage forms are enhanced bioavailability, reduced dosing frequency, and more consistent drug levels in the body. The document also covers various mechanisms for controlled release, including osmotic pumps, floating systems, and coating technologies. It provides examples of commercially available controlled release drugs and classifications of these systems.
The document describes the formulation and evaluation of oral thin films containing the drug pitavastatin. Various oral thin film formulations were prepared using solvent casting method with polymers like povidone and HPMC K4M. The solubility of pitavastatin was studied in different buffers and 0.1N HCl showed highest solubility. Compatibility studies using FTIR showed no interactions between drug and excipients. The formulated films were evaluated for weight uniformity, thickness, folding endurance, drug content uniformity and in vitro drug release. The stable formulation F8 released 99% of drug within 5 minutes and was selected for further stability studies. The results suggested formulation F8 was stable for 3 months. Bioavailability studies are needed before commercialization
This document provides an overview of floating drug delivery systems (FDDS). FDDS are low-density drug delivery systems that remain buoyant in the stomach without affecting gastric emptying rate, resulting in increased gastric retention time and better control of drug concentrations. There are two main types of FDDS - effervescent systems that use gas-generating agents to reduce density, and non-effervescent systems that rely on gel-forming or swellable polymers. FDDS can improve drug absorption for drugs that need to be absorbed in the stomach or have a narrow absorption window in the small intestine. Several commercially available FDDS products and patents are described. Factors like dosage form size and shape, gender, posture, and age
Floating drug delivery approach uses low-density systems that have sufficient buoyancy to flow over the
gastric contents and remains buoyant in the stomach without affecting the stomachic emptying rate for a
chronic period of time. This result is increased gastric retention time and better control of the fluctuations
in plasma drug concentration with a low risk of toxicity. Drugs, which are locally active in the stomach,
drugs having narrow absorption window and unstable in the intestine, and colonic environment, are the
potential drug candidates. The approach not only improves drug absorption but also minimizes the mucosal
irritation of drugs. As the approach requires a high fluid level in the stomach to float and work efficiently,
it makes the approach limited up to some extent. Many buoyant systems have been developed based on
granules, powders, capsules, tablets, laminated films, and hollow microspheres and few formulations have
been commercialized in the market at the present time. This review gives an overview of the approach of
floating drug delivery at present with sequential demystification thus enabling a greater understanding of
their role in medicine and drug delivery
This document provides an overview of floating drug delivery systems (FDDS). FDDS are low-density drug delivery systems that remain buoyant in the stomach without affecting gastric emptying rate, resulting in increased gastric retention time and better control of drug concentrations. There are two main types of FDDS - effervescent systems that use gas-generating agents to reduce density, and non-effervescent systems that rely on gel-forming or swellable polymers. FDDS can improve drug absorption for drugs that need to be absorbed in the stomach or have a narrow absorption window in the small intestine. Several commercially available FDDS products and patents are described. Factors like dosage form size and shape, gender, posture, and age
ABSTRACT The purpose of this study was to prepare and evaluate immediate release itraconazole pellets and comprehensive studies of the same. The itraconazole pellets is prepared using fluid bed processer with different concentration of HPMC (Hydroxy Propyl Methyl Cellulose). The physicochemical compatibility of the drug and the excipient studied by differential scanning calorimetry. The prepared pellets were physically evaluated with size, shape, bulk density, tapped density, compressibility index, hausners ratio, angle of repose, sieve analysis, surface roughness, density, moisture content, assay and drug release etc. The in vitro drug release profile from pellets shows that all the formulation release more than 75% drug within 90min. Optimized formulations were found to have HPMC concentration 2-5% of total weight of pellets to maximize high-quality surface, desired release, and size distribution within the range. These results indicate that pellets containing 10 % HPMC of total weight of pellets give better quality of itraconazole pellets for immediate release. Key Words: Itraconazole, Hydroxyl propyl methyl cellulose and Immediate release.
This document describes the formulation and evaluation of oral thin films containing the drug pitavastatin. Various oral thin film formulations were prepared using solvent casting method with polymers like PVP, HPMC and gelatin. The solubility studies showed pitavastatin has highest solubility in 0.1N HCl. Compatibility studies using FTIR showed no interactions between drug and excipients. The formulated films were evaluated for weight uniformity, thickness, folding endurance, drug content uniformity and in vitro drug release. The stable F8 formulation from 3 months stability studies will be subjected to bioavailability studies and commercialized if requirements are met.
Objective: The purpose of the current research work was to study effect of formulation variables in a statistical way for the SR formulations of Valsartan sodium. Methods: Valsartan sodium is an antihypertensive agent angiotensin‒II receptor blocker belongs to BCS class‒III agent. SR tablet formulations of Valsartan sodium were formulated using variable quantities of HPMCK100M and Xanthan Gum by direct compression method. quantities of polymers was chosen as independent variables, X1 and X2 respectively whereas, time required for dissolution 10%(t10%), 50%(t50%), 75%(t75%) and 90%(t90%) of drug from formulation were chosen as dependent variables. 9 formulations were prepared and evaluated for various pharmacopoeial tests. Results: The results reveals that all formulations were found to be with in the acceptable limits and release rate profiles of all formulations were fitted to kinetic models. The statistical parameters were determined. Polynomial equations were developed for dependent variables. Validity of them was checked by countercheck formulations (C1 ,C2 ). According to SUPAC guidelines, formulation (F4) containing mixture of 12% HPMCK100M and 16% Xanthan gum, was found to be identical formulation (dissimilarity factor f1 =1.763, similarity factor f2 =86.747 & No significant difference, t=0.0478) to marketed product (VALZAAR). Conclusion: Formulation F4 follows First order kinetics, Non‒Fickian Diffusion Anomalous Transport. (n=0.826).
Objective: The purpose of present research work is to develop the sustained release
formulation for Olmesartan medoxomil using 32
factorial design. Olmesartan an
Antihypertensive agent, angiotensin‒II receptor (type AT1) blocker and BCS class‒II
agent.
Methods: Sustained Release tablets of Olmesartan medoxomil were prepared using
different quantities of HPMCK4M and Xanthan Gum in combinations by direct
compression technique. The concentration of Polymers, HPMCK4M and Xanthan gum
required to achieve the drug release was selected as independent variables, X1 and X2
respectively whereas, time required for 10% of drug release (t10%), 50% (t50%), 75%
(t75%) and 90% (t90%) were selected as dependent variables.
Results: Nine formulations were prepared and are evaluated for various
pharmacopoeial tests. The results reveals that all formulations were found to be with
in the pharmacopoeial limits and In vitro drug release profiles of all formulations were
fitted in to various Kinetic models. The statistical parameters like intercept, slope
& correlation coefficient were calculated. Polynomial equations were developed for
dependent variables. Validity of developed polynomial equations were checked by
designing 2 check point formulations (C1
, C2
).
Conclusion: According to SUPAC guidelines formulation (F5
) containing combination
of 15% HPMCK4M and 15% Xanthan gum, is the most identical formulation (similarity
factor f2
= 91.979, dissimilarity factor f1
= 1.546 & No significant difference, t=0.0338)
to marketed product (BENICAR). Best Formulation F5 follows First order, Higuchi’s
kinetics, and the mechanism of drug release was found to be Non‒Fickian Diffusion
Anomalous Transport. (n=0.828).
The main objective was to formulate fast dissolving tablets of Amisulpride using a 32 full factorial design to study the effects of different concentrations of crospovidone and croscarmellose sodium on tablet properties. Nine formulations were prepared using combinations of 9%, 7%, or 5% crospovidone and 9%, 7%, or 5% croscarmellose sodium. Tablet properties like disintegration time, wetting time, and drug release at 50% and 90% were evaluated. Formulation F1 containing 9% of each superdisintegrant showed the fastest disintegration and drug release, most similar to the marketed product. Polynomial equations were derived relating the superdisintegrant concentrations to the response variables.
ABSTRACT
Objective: Stroke is one of the leading causes of death and disabilities worldwide. Cost-effectiveness analysis helps identify neglected opportunities
by highlighting interventions that are relatively inexpensive, yet have the potential to reduce the disease burden substantially. In India, there are
wide social and economic disparities. Socioeconomic environment influences occupation, lifestyle, and nutrition of social classes which in turn would
influence the prevalence and profile of stroke. By reduction of delays in access to hospital and improving provision of affordable treatments can
reduce morbidity and mortality in patients with stroke in India. This study is designed to measure and compare the costs (resources consumed) and
consequences (clinical, economic, and humanistic) of pharmaceutical products and services and their impact on individuals, healthcare systems and
society.
Methods: The purpose of this study is to analyze and conduct a cost-effectiveness analysis for the treatment of stroke in Guntur City Hospitals.
The patients were treated either with aspirin or clopidogrel. The health outcomes were measured using Modified Rankin Scale, A prominent risk
assessment scale for stroke. The pharmacoeconomic data were computed from the patient data collection forms.
Result: The incremental cost-effectiveness ratio of aspirin and clopidogrel were calculated to be Rs. 8046.2/year.
Conclusion: The study concludes that aspirin has the increased socioeconomic impact when compared to Clopidogrel and we can see that the earlier
therapy has supported discharge, home-based rehabilitation along with reduced hospital stay and hence preferable.
Keywords: Stroke, Pharmacoeconomics, Cost-effectiveness analysis, Aspirin, Clopidogrel, Incremental cost-effectiveness ratio.
This document discusses the rational use of drugs and the issues with irrational drug use. It begins by discussing how antibiotics were initially hailed as miracle drugs that saved many lives, but bacteria eventually evolved resistance. It then defines rational drug use as prescribing the correct drug, dose, and duration based on a patient's needs. Some reasons for irrational drug use include a lack of information, training, diagnostic facilities, and effective regulation. The hazards of irrational drug use include ineffective treatment, prolonged illness, increased costs, and harm to patients. It emphasizes only using antibiotics with proper dosing and duration, avoiding self-medication, and educating others. In conclusion, it states that medicines must be used properly to be effective and avoid harm.
The document discusses antidepressants in chronic pain relief. It provides background on chronic pain and classifies pain based on pathophysiology, duration, etiology, and anatomy. It then discusses the pathophysiology of nociceptive and neuropathic pain in detail. The document reviews various types of antidepressants and their mechanisms of action. It summarizes evidence from multiple studies that tricyclic antidepressants and selective serotonin reuptake inhibitors can effectively treat chronic pain conditions like diabetic neuropathy and post-herpetic neuralgia at doses lower than those used for depression. The antidepressants may relieve pain through mechanisms other than their antidepressant effects.
Background: The main aim of present research investigation is to formulate the Risperidone Fast Dissolving tablets. Risperidone, an atypical antipsychotic, belongs to BCS Class-II and used for treating schizophrenia, bipolar mania and autism by blocking D2 and 5-HT2A receptors. Methods: The Fast Dissolving tablets of Risperidone were prepared employing different concentrations of Crospovidone and Croscarmellose sodium in different combinations as a Superdisintegrants by Direct Compression technique using 32 factorial design. The concentration of Crospovidone and Croscarmellose sodium was selected as independent variables, X1 and X2 respectively whereas, wetting time, Disintegration time, t50% ,t90%were selected as dependent variables. Results and Discussion:
Totally nine formulations were designed, preapred and are evaluated for hardness, friability, thickness, Assay, Wetting time, Disintegration time, In-vitro drug release. From the Results concluded that all the formulation were found to be with in the Pharmacopoeial limits and the In-vitro dissolution profiles of all formulations were fitted in to different Kinetic models, the statistical parameters like intercept (a), slope (b) & regression coefficient (r) were calculated. Polynomial equations were developed for Wetting time, Disintegration time, t50%, t90%. Validity of developed polynomial equations were verified by designing 2 check point formulations (C1, C2). According to SUPAC guidelines the formulation (F5) containing combination of 10% Crospovidone and 10% Croscarmellose, is the most similar formulation (similarity factor f2= 93.556, dissimilarity factor f1= 0.976& No significant difference, t= 0.022) to marketed product (RISPERDAL-4). Conclusion: The selected formulation (F5) follows First order, Higuchi’s kinetics, mechanism of drug release was found to be Fickian Diffusion (n= 0.383).
ABSTRACT
Background:The main objective of the study is to determine the anti-arthritic effect of whole plant ethanolic extract of Polygonum glabrum
belonging to the family Polygonaceae in Female wistar rats using the Freund’s Complete Adjuvant (FCA) model . Methods:The plants areal
parts were collected near Tirupathi hills, Chittoor district of Andhra Pradesh in India. The Phytoconstituents were identified through the
chemical tests. Ethanol (95%) was used to obtain the whole plant extraction through Soxhlet extractor. Female SD rats were used for antiarthritic
screening. Arthritis was induced using FCA, and the anti-arthritic effect of the ethanolic extract of P.glabrum was studied at doses
of 250 and500 mg/kg. The effects were compared with those of indomethacin (10 mg/kg). At the end of the study, theliver enzyme levels were
determined and a radiological examination was carried out. Results and Discussion:The preliminary phytochemical analysis of the ethanolic
extract of Polygonum glabrum showed the presence of alkaloids, tannins, flavonoids and saponins. P. glabrum at 250 and 500 mg/kg
significantly inhibited the FCA-induced arthritis in the rats. This was manifested by as a decrease in the paw volume. The arthritic control
animals exhibited a significant decrease in body weight compared with control animals without arthritis. P. glabrum treated animals showed
dose dependent reduction in decrease in body weight and arthritis.At the same time, P.glabrum significantly altered the biochemical and
haematological changes induced by FCA (P < 0.05). The anti-arthritic effect of P.glabrum was comparable with that of Indomethacin.
Conclusion:The whole plant extract of P.glabrum showed significant anti-arthritic activity against FCA-induced arthritis in female Wistar
rats.
ABSTRACT
Over the last decade, diabetes mellitus has emerged as an important clinical and public health
problem throughout the world. The aim of the study is perceive the Potentiality of a newer oral
Antihyperglycemic combination therapy over conventional therapy in type 2 diabetes. The
prospective study was conducted over a period of six months in the department of Medicine,
Guntur City Hospital. The prevalence of type2 diabetes was high in male 65.79 % than female
34.21%. Majority of the patients (23.68 %) belonged to age group of 51–55 years. Majority of
patients (55.26%) having a family history of Diabetes. Majority of patients receiving Combination
of Glibenclamide + Metformin (60.53%), evaluated for effect on FPG for both combinations. The
mean changes in FPG were noted. In the same way effect on HbA1c also noted. Mean changes in
for every month HbA1c will be noted. Our study reveals that Combination therapy with Metformin
plus Glimepiride is more effective than Glibenclamide plus Metformin; in improving glycemic
control in type 2 diabetes, while also allowing a reduction of the dosage of each drug.
This study evaluated the anti-inflammatory properties of the aqueous extract of Solena amplexicaulis leaves in rats. Rats were injected with egg white to induce paw edema and treated with the extract, diclofenac sodium (standard drug), or saline (control). Paw volume was measured over 60 minutes. The extract significantly reduced paw edema compared to control, demonstrating anti-inflammatory effects comparable to diclofenac sodium. The extract likely inhibits the release of inflammatory mediators like histamine and prostaglandins. Therefore, the aqueous extract of S. amplexicaulis leaves has potent anti-inflammatory activity.
The document discusses rectal drug delivery systems. It provides a brief history of rectal medications dating back to ancient civilizations. It describes the anatomy and physiology of the human rectum, noting its length, pH, blood supply, and limited surface area available for drug absorption. Several advantages and disadvantages of the rectal route are outlined. Factors affecting drug absorption from the rectum include physiological factors of the drug and rectum as well as physicochemical properties of the drug. Common rectal dosage forms include creams, ointments, suppositories, solutions, and suspensions. The document discusses these forms in detail and provides examples of commercial rectal products.
The document discusses osmotic drug delivery systems, which use osmotic pressure to control drug release. It describes the principles of osmosis, advantages and disadvantages of osmotic systems, components of osmotic pumps like semipermeable membranes and osmogens, and various types of osmotic pumps. The document provides details on the design and working of osmotic pumps for controlled drug delivery.
This document discusses ocular drug delivery systems. It begins by noting the importance of the eye and challenges in delivering drugs to it. Topical eye drops and ointments are commonly used but much of the drug is quickly drained away. Novel delivery systems aim to increase drug absorption and targeting to the front and back segments of the eye. These include microemulsions, nanosuspensions, nanoparticles, and liposomes, which can help prolong drug residence time and enhance permeability. The document also reviews challenges in ocular delivery and strategies to improve bioavailability such as viscosity enhancers, gels, prodrugs, and bioadhesive polymers.
This document discusses nasal drug delivery systems. It covers advantages like avoidance of first-pass metabolism and rapid drug absorption. Disadvantages include potential nasal irritation and smaller absorption surface area compared to the GI tract. Factors influencing nasal absorption are drug properties, pH, and permeability enhancers. Common formulations use drugs, viscosity agents, solubilizers, and preservatives. Nasal delivery can be used for non-peptide drugs, peptides, and diagnostics by exploiting the nasal mucosa for absorption.
The document discusses buccal drug delivery using the buccal mucosa. It notes that the buccal mucosa lines the inner cheek and can be used to treat both local and systemic conditions. It then discusses the advantages of buccal delivery in avoiding first-pass metabolism and providing a less hostile environment than the GI tract. Various buccal dosage forms are described including tablets, patches, films and gels. Key factors influencing drug delivery via this route like drug properties and type of dosage form are also summarized.
This document discusses bioadhesive drug delivery systems. It begins by defining bioadhesion as the interfacial molecular forces that allow polymers to adhere to biological surfaces for extended periods of time. It then discusses various bioadhesive polymers, both natural and synthetic, that are commonly used in drug delivery formulations. These include polymers like acacia gum, alginic acid, carbomers, and hyaluronic acid. The document also outlines the three main mechanisms by which bioadhesion occurs: wetting and swelling of polymers, interpenetration of polymer chains with mucosal membranes, and formation of chemical bonds between entangled chains. Finally, it provides examples of different types of bioadhesive drug delivery formulations that can
The document discusses various topics related to tablet compression including compression, consolidation, compaction, energy involved, tablet strength parameters like crushing strength and friability, and issues like lamination. It provides details on the energy expended during different stages of compression and how lubricants can reduce this. Tablet strength is found to increase with compression force and binder concentration but decrease with porosity. Tests for evaluating tablet properties like hardness, friability and lamination tendency are also summarized.
This document appears to be a student presentation on controlled release drug delivery systems. It includes definitions of key terms like drug, dosage form, controlled release, sustained release and conventional release. It then discusses challenges with conventional release and benefits of controlled release like improved patient compliance and maintenance of therapeutic drug levels. The rest of the document provides details on various controlled release mechanisms, technologies, products, equations and challenges.
1. Asian Journal of Pharmaceutics • Oct-Dec 2015 (Suppl) • 9 (4) | S34
Design, Formulation and Evaluation of
Atenolol Gastro Retentive Floating Tablets
Raghavendra Kumar Gunda1
, J. N. Suresh Kumar1
, Chandan Kumar Brahma1
,
V. Satyanarayana2
, K. Naga Prashant3
1
Department of Pharmaceutics, Narasaraopeta Institute of Pharmaceutical Sciences, Narasaraopet, Guntur,
Andhra Pradesh, India, 2
Department of Pharmacy Practice, Narasaraopeta Institute of Pharmaceutical
Sciences, Narasaraopet, Guntur, Andhra Pradesh, India, 3
Department of Pharmaceutical Chemistry,
Narasaraopeta Institute of Pharmaceutical Sciences, Narasaraopet, Guntur, Andhra Pradesh, India
Abstract
The main objective of present research work is to formulate the floating tablets of atenolol using 32
factorial
design. Atenolol, β-blocker belongs to Biopharmaceutical Classification System Class-III. The floating tablets
of atenolol were prepared employing different concentrations of hydroxypropyl methylcellulose (HPMC) K15M
and sodium bicarbonate in different combinations by direct compression technique using 32
factorial design. The
concentration of HPMC K15M and sodium bicarbonate required to achieve desired drug release was selected as
independent variables, X1
and X2
, respectively, whereas time required for 10% of drug dissolution (t10%
), 50%
(t50%
), 75% (t75%
), and 90% (t90%
) were selected as dependent variables. Totally, nine formulations were designed
and are evaluated for hardness, friability, thickness, % drug content, floating lag time, in vitro drug release. From
the results, concluded that all the formulation were found to be within the pharmacopoeial limits and the in vitro
dissolution profiles of all formulations were fitted into different Kinetic models, the statistical parameters like
intercept (a), slope (b) and regression coefficient (r) were calculated. Polynomial equations were developed for
t10%
, t50%
, t75%
, t90%
.Validity of developed polynomial equations was verifiedby designing 2 checkpoint formulations
(C1
, C2
). According to SUPAC guidelines the formulation (F8
) containing combination of 25% HPMC K15M and
3.75% sodium bicarbonate, is the most similar formulation (similarity factor f2
= 87.797, dissimilarity factor
f1
= 2.248 and no significant difference, t = 0.098) to marketed product (BETACARD). The selected formulation
(F8
) follows Higuchi’s kinetics, and the mechanism of drug release was found to be non-Fickian diffusion
(n = 1.029, Super Case-II transport).
Key words: 32
factorial design, atenolol, floating lag time, gastro retentive floating tablet, hydroxypropyl methyl
cellulose K15M, non-Fickian diffusion mechanism, sodium bicarbonate, SUPAC
Address for correspondence:
Raghavendra Kumar Gunda, Department of
Pharmaceutics, Narasaraopeta Institute of Pharmaceutical
Sciences, Narasaraopet, Guntur - 522 601,
Andhra Pradesh, India. E-mail: raghav.gunda@gmail.com
Received: 21-10-2015
Revised: 27-11-2015
Accepted: 07-12-2015
INTRODUCTION
O
raladministrationisthemostconvenient,
widely used route for both conventional
and novel drug delivery systems, and
preferred route of drug delivery for systemic
action. Tablets are the most popular oral solid
formulations available in the market and are
preferred by patients and physicians alike. There
are many reasons for this, not the least of which
would include acceptance by the patient and
ease of administration, patient compliance and
flexibility in formulation, etc. From immediate
release to site-specific delivery, oral dosage
forms have really progressed.
In long-term therapy for the treatment of chronic
disease conditions, conventional formulations
are required to be administered in multiple doses and,
therefore, have several disadvantages.[1]
However, when
administered orally, many therapeutic agents are subjected
to extensive pre-systemic elimination by gastrointestinal
degradation and/or first-pass hepatic metabolism as a result
of which low systemic bioavailability and shorter duration
of therapeutic activity and formation of inactive or toxic
metabolites.[2]
ORIGINALARTICLE
2. Gunda, et al.: Formulation development and evaluation of Atenolol Gastro Retentive Floating Tablets
Asian Journal of Pharmaceutics • Oct-Dec 2015 (Suppl) • 9 (4) | S35
Rapid gastrointestinal transit can result in incomplete drug
release from a device above the absorption zone, leading to
the diminished efficacy of the administered dose. Therefore,
different approaches have been proposed to retain the dosage
form in the stomach. These include bio adhesive systems,
swelling and expanding systems and floating systems.
Large single-unit dosage forms undergo significant swelling
after oral administration, and the swollen matrix inhibits
gastric emptying even when the pyloric sphincter is in an
uncontracted state.[3]
Gastric floating drug delivery system
(GFDDS) can overcome at least some of these problems and
is particularly useful for drugs that are primarily absorbed
in the duodenum and upper jejunum segments. The GFDDS
is able to prolong the retention time of a dosage form in the
stomach, thereby improving the oral bioavailability of the
drug.
Gastroretentive dosage forms significantly extend the period
of time, over which drug may be released and thus prolong
dosing intervals and increase patient compliance.[4,5]
Such
retention systems are important for those drug that are
degraded in the intestine like antacids or certain antibiotics,
enzymes that act locally in the stomach. These systems can
be retained in the stomach and assist in improving the oral
sustained delivery of drugs that have an absorption window in
a particular region of the gastrointestinal tract, thus ensuring
optimal bioavailability.
Over the past 30 years, as the expense and complications
involved in marketing new drug entities have increased,
with concomitant recognition of the therapeutic advantages
of controlled drug delivery, the goal in the designing
sustained/controlled drug delivery system is to reduce the
dosing frequency or to increase effectiveness of the drug by
localization at the site of action, reducing the dose required,
or providing uniform drug delivery.[3]
Since the early 1950s, the application of polymeric materials
for medical purposes is growing very fast. Polymers have
been used in the medical field for a large extent.[4]
Natural
polymers remain attractive primarily because they are
inexpensive, readily available, be capable of chemical
modifications, non-carcinogenicity, mucoadhesivity,
biodegradable, biocompatible, high drug holding capacity,
and high thermal stability and easy of compression.[5]
This
led to its application as excipient in hydrophilic drug delivery
system. The various natural gums and mucilages have been
examined as polymers for sustained drug release in the last
few decades for example; sodium bicarbonate, tragacanth
gum, xanthan gum, pectin, alginates, etc. In the development
of a gastro-retentive floating tablet dosage form. Availability
of wide variety of polymer and frequent dosing interval
helps the scientist to develop sustained release product.
cellulose derivatives such as carboxymethylcellulose (CMC),
sodium CMC, hydroxyproyl cellulose, and hydroxypropyl
methylcellulose (HPMC) have been extensively studied as
the polymer in the Floating tablet formulations along with gas
generating agent like NaHCO3
.[6]
These polymers are most
preferred because of its cost effectiveness, broad regulatory
acceptance, non-toxic and easy of compression. These dosage
forms are available in the extended release, targeted release,
delayed release, prolonged action dosage form. Some factors
like molecular size, diffusivity, pKa-ionization constant,
release rate, dose, and stability, duration of action, absorption
window, therapeutic index, protein binding, and metabolism
affect the design of sustained release formulation. The future
of sustained-release products is promising in some area
like chronopharmacokinetic system, targeted drug delivery
system, mucoadhesive system, particulate system that
provide high promise and acceptability.
Developing floating formulations Biopharmaceutical
Classification System Class-III drugs has become a
challenge to the pharmaceutical technologists. Fast
release drug generally causes toxicity if not formulated as
extended release dosage form. Among various formulation
approaches, in controlling the release of water-soluble drugs,
the development of sustained release coated granules has a
unique advantage of lessening the chance of dose dumping
which is a major problem when the highly water-soluble drug
is formulated as matrix tablets.
Oral sustained release dosage form by direct compression
technique is a simple approach of drug delivery systems that
proved to be rational in the pharmaceutical arena for its ease,
compliance, faster production, avoid hydrolytic, or oxidative
reactions occurred during processing of dosage forms.[7]
The selection of the drug candidates for floating drug delivery
system needs consideration of several biopharmaceutical,
pharmacokinetic and pharmacodynamic properties of the
drug molecule.[8]
In the present study, a gastro-retentive floating dosage form
of atenolol has been developed that makes less frequent
administering of the drug also to improve bioavailability.
Atenolol is a cardioselective β-blocker, selective β1
adrenergic antagonist it is widely used in the treatment of
hypertension and angina pectoris. The chemical name of
atenolol is 4-[2-hydroxy-3-[(1-methyl ethyl)amino]propoxy]
benzene acetamide. Undergoes little or no hepatic first pass
metabolism and its elimination half-life is 6-7 h. The present
modes of administration of atenolol are oral and parenteral.
It is incompletely absorbed from the gastrointestinal tract
and has an oral bioavailability of only 50% while the
remaining is excreted unchanged in feces. The human jejunal
permeability and extent of absorption are low. Thus, it seems
that an in gastric residence time may increase the extent of
absorption and bioavailability of the drug. The recommended
adult oral dosage of atenolol is 50 mg twice daily for the
effective treatment of hypertension. However, fluctuations
of drug concentration in plasma may occur, resulting in
side effects or a reduction in drug concentration at receptor
3. Gunda, et al.: Formulation development and evaluation of Atenolol Gastro Retentive Floating Tablets
Asian Journal of Pharmaceutics • Oct-Dec 2015 (Suppl) • 9 (4) | S36
side. As the drug is effective when the plasma fluctuations
are minimized, therefore sustained release dosage form of
atenolol is desirable.[9]
The short biological half-life of drug
(6-8 h) also favors the development of sustained release
formulations.
The gastro-retentive drug delivery systems can be retained
in the stomach and assist in improving the oral sustained
delivery of drugs that have an absorption window in a
particular region of the gastrointestinal tract. These systems
help in continuously releasing the drug before it reaches the
absorption window, thus ensuring optimal bioavailability.
Thus, there is a need to maintain atenolol at its steady state
plasma concentration. Hence, the study was carried out to
formulate and evaluate floating dosage form of atenolol
as a model drug and had aim that final batch formulation
parameters should show prolong drug release.
Development of dosage form depends on chemical nature
of the drug/polymers, matrix structure, swelling, diffusion,
erosion, release mechanism, and the in vivo environment.
It is an important issue is to design an optimized formulation
with an appropriate dissolution rate in a short time period and
minimum trials. Many statistical experimental designs have
been recognized as useful techniques to optimize the process
variables. For this purpose, response surface methodology
(RSM) utilizing a polynomial equation has been widely
used. Different types of RSM designs include 3-level
factorial design, central composite design, Box-Behnken
design, and D-optimal design. RSM is used when only a few
significant factors are involved in experimental optimization.
The technique requires less experimentation and time, thus
proving to be far more effective and cost-effective than
the conventional methods of formulating sustained release
dosage forms.[10-13]
Hence, an attempt is made in this research work to formulate
floating tablets of atenolol using HPMC K15M and sodium
bicarbonate. Instead of the normal and trial method, a
standard statistical tool design of experiments is employed
to study the effect of formulation variables on the release
properties.
Large scale production needs more simplicity in the
formulation with economic and cheapest dosage form. The
floating tablets formulation by direct compression method is
most acceptable in large scale production.
A 32
full factorial design was employed to systematically
study the drug release profile. A 32
full factorial design
was employed to investigate the effect of two independent
variables (factors), i.e., the amounts of HPMC K15M and
sodium bicarbonate on the dependent variables, i.e., t10%
,
t50%
, t75%
, t90%
(Time taken to release 10%, 50% 75%, 90%,
respectively).
MATERIALS AND METHODS
Materials used in this study were obtained from the different
sources. Atenolol was a gift sample from Aurobindo Pharma
Ltd, Hyderabad, India. HPMC K15M from colorcon, sodium
bicarbonate, Di-Calcium Phosphate were procured from
Loba Chemie Pvt. Ltd, Mumbai. Other excipients such as
stearic acid, citric acid, aerosil, and talc were procured from
S.D. Fine Chem. Ltd., Mumbai, Maharashtra, India.
Formulation development of atenolol sustained-
release tablets
The factorial design is a technique that allows identification
of factors involved in a process and assesses their relative
importance. In addition, any interaction between factors
chosen can be identified. Construction of a factorial design
involves the selection of parameters and the choice of
responses.[14]
A selected three level, two-factor experimental design
(32
factorial design) describe the proportion in which the
independent variables HPMC K15M and sodium bicarbonate
were used in the formulation of atenolol floating tablets. The
time required for 10% (t10%
), 50% (t50%
), 75% (t75%
), and 90%
(t90%
) drug dissolution were selected as dependent variables.
Significance terms were chosen at 95% confidence interval
(P < 0.05) for Final Equations. Polynomial equations were
developed for t10%
, t50%
, t75%
, t90%
, (step-wise backward Linear
Regression Analysis).
The three levels of factor X1
(HPMC K15M) at a concentration
of 25%, 31.25%, 37.25%. three levels of factor X2
(sodium
bicarbonate) at a concentration of 3.75%, 7.5%, 11.25%
(% with respect to total tablet weight) was taken as the rationale
for the design of the Atenolol floating tablet formulation.
Totally,nineAtenololfloatingtabletformulationswereprepared
employing selected combinations of the two factors, i.e., X1
, X2
as per 32
Factorial and evaluated to find out the significance of
combined effects of X1
, X2
to select the best combination and the
concentration required to achieve the desired prolonged release
of drug (by providing gastro retentivity) from the dosage form.
Preparation of atenolol floating tablets
All the ingredients were accurately weighed and passed
through mesh # 60. To mix the ingredients thoroughly drug
and polymer were blended geometrically in a mortar and
pestle for 15 min then sodium bicarbonate, talc and aerosil
were mixed one by one. After thoroughly mixing these
ingredients, the powder blend was passed through # 44 mesh.
Powder blend was compressed by using rotary tablet
punching machine (RIMEK), Ahmedabad). Compressed
tablets were examined as per official standards and unofficial
tests. Tablets were packaged in well closed light resistance
and moisture proof containers.
4. Gunda, et al.: Formulation development and evaluation of Atenolol Gastro Retentive Floating Tablets
Asian Journal of Pharmaceutics • Oct-Dec 2015 (Suppl) • 9 (4) | S37
Experimental design
Experimental design utilized in present investigation
for the optimization of excipients concentration such
as concentration of HPMC K15M was taken as X1
and
concentration of sodium bicarbonate was taken as X2
.
Experimental design was given in Table 1. Three levels for
the concentration of HPMC K15M were selected and coded
as −1 = 25%, 0 = 31.25%, +1 = 37.5%. Three levels for the
concentration of sodium bicarbonate were selected and coded
as −1 = 3.75%, 0 = 7.5%, +1 = 11.25%. Formulae for all the
experimental batches were given in Table 2.[15]
Evaluation of atenololsustained release tablets
Hardness[16]
Thehardnessofthetabletswastestedbydiametriccompression
using a monsanto hardness tester. A tablet hardness of about
2-4 kg/cm2
is considered adequate for mechanical stability.
Friability16
ThefriabilityofthetabletswasmeasuredinaRochefriabilator
(Camp-Bell Electronics, Mumbai, Maharashtra, India).
Tablets of a known weight (W0
) or a sample of 20 tablets are
dedusted in a drum for a fixed time (100 revolutions) and
weighed (W) again. Percentage friability was calculated from
the loss in weight as given in equation as below. The weight
loss should not be more than 1%.
Friability (%) = [(Initial weight−Final weight)/(Initial
weight)] × 100
Content uniformity[16]
In this test, 20 tablets were randomly selected, and the percent
drug content was determined, the tablets contained not less
than 85% or more than 115% of the labeled drug content can
be considered as the test was passed.
Assay[17]
The drug content in each formulation was determined by
triturating 20 tablets, and powder equivalent to average weight
was added in 100 ml of 0.1 N hydrochloric acid, followed by
stirring. The solution was filtered through a 0.45 μ membrane
filter, diluted suitably, and the absorbance of the resultant
solution was measured spectrophotometrically at 224 nm
using 0.1 N hydrochloric acid as blank.
Thickness
Thickness of the all tablet formulations was measured using
vernier calipers by placing tablet between two arms of the
vernier calipers.[16]
In vitro buoyancy studies
The tablets were placed in a 100 mL beaker containing 0.1 N
HCl. The time required for the tablet to rise to the surface and
float was determined as floating lag time.[18,19]
In vitro dissolution study[20]
The In vitro dissolution study for the atenolol floating tablets
were carried out in USPXXIII type-II dissolution test apparatus
(Paddle type) using 900 ml of 0.1 N HCl as dissolution medium
Table 1: Experimental design layout
Formulation code X1
X2
F1
1 1
F2
1 0
F3
1 −1
F4
0 1
F5
0 0
F6
0 −1
F7
−1 1
F8
−1 0
F9
−1 −1
F1
‑F9
: Factorial formulations
Table 2: Formulae for the preparation of atenolol floating tablets as per experimental design
Name of
ingredients
Quantity of ingredients per each tablet (mg)
F1
F2
F3
F4
F5
F6
F7
F8
F9
Atenolol 50 50 50 50 50 50 50 50 50
HPMC K15M 150 150 150 125 125 125 100 100 100
Sodium bicarbonate 45 30 15 45 30 15 45 30 15
Di calcium phosphate 97 112 127 112 137 152 147 162 177
Stearic acid 40 40 40 40 40 40 40 40 40
Citric acid 10 10 10 10 10 10 10 10 10
Aerosil 4 4 4 4 4 4 4 4 4
Talc 4 4 4 4 4 4 4 4 4
Total weight 400 400 400 400 400 400 400 400 400
HPMC: Hydroxypropyl methylcellulose
5. Gunda, et al.: Formulation development and evaluation of Atenolol Gastro Retentive Floating Tablets
Asian Journal of Pharmaceutics • Oct-Dec 2015 (Suppl) • 9 (4) | S38
at 50 rpm and temperature 37 ± 0.5°C. At predetermined time
intervals, 5 ml of the samples were withdrawn by means of a
syringe fitted with a pre-filter, the volume withdrawn at each
interval was replaced with the same quantity of fresh dissolution
medium. The resultant samples were analyzed for the presence
of the drug release by measuring the absorbance at 224 nm
using UV-Visible spectrophotometer after suitable dilutions.
The determinations were performed in triplicate (n = 3).
Kinetic modeling of drug release[21-24]
The dissolution profile of all the formulations was fitted
into zero-order, first-order, Higuchi, and Korsmeyer–Peppas
models to ascertain the kinetic modeling of drug release.
RESULTS AND DISCUSSION
Gastro retentive floating tablets of atenolol were prepared and
optimized by 32
factorial design to select the best combination
of different release rate modifiers, HPMC K15M, sodium
bicarbonate and also to achieve the desired prolonged
release of drug from the dosage form (by retaining drug at
gastric environment). The two-factorial parameters involved
in the development of formulations are quantity of HPMC
K15M and sodium bicarbonate polymers as independent
variables (X1
, X2
), and In vitro dissolution parameters such
as t10%
, t50%,
t75%
, and t90%
as dependent variables.
Totally, nine
formulations were prepared using 3 levels of 2 factors and all
the formulations containing 50 mg of Atenolol were prepared
as a floating tablet dosage form by direct compression
technique as per the formulae given in Table 2.
All the prepared tablets were evaluated for different post-
compression parameters, drug content, mean hardness,
friability, mean thickness, mean diameter, floating lag time
as per official methods, and results are given in Table 3. The
hardness of tablets was in the range of 4.49-4.69 Kg/cm2
.
Weight loss in the friability test was less than 0.68%. Drug
content of prepared tablets was within acceptance range only.
Results for all Post-compression parameters were tabulated or
shown in Table 3. In vitro dissolution studies were performed
for prepared tablets using 0.1 N HCl as a dissolution media at
50 rpm and temperature 37 ± 0.5°C. The in vitro dissolution
profiles of tablets are shown in Figure 1 and the dissolution
parameters are given in Table 4. Cumulative % drug release of
factorial design formulations F1
-F9
at 10 Hr were found to be
in the range of 72.91-100.80 %. From the results, it reveals that
as the amount of polymer in the tablet formulation increases,
the drug release rate decreases and as the concentration of
gas generating agent (NaHCO3
) increases the drug release
increases and at the same time floating lags time decreases.
Therefore, required release of drug can be obtained by
manipulating the composition of HPMC K15M and sodium
bicarbonate.
Many variations were observed in the t10%
, t50%,
t75%,
and t90%
due
to formulation variables. Formulation F8
containing 100 mg of
HPMCK15M,30 mgofsodiumbicarbonateshowedpromising
dissolution parameter (t10%=
0.418 h, t50% =
2.747 h, t75% =
5.494 h,
t90% =
9.128 h) which meets the objective of work by providing
more gastric retentivity and maximum drug release. The
difference in burst effect of the initial time is a result of the
difference in the viscosity of the polymeric mixtures. Dortunc
and Gunal have reported that increased viscosity resulted in a
Figure 1: Comparative zero order plots for F1
-F9
Table 3: Post‑compression parameters for the formulations
Formulation
code
Hardness
(kg/cm2
)
Floating lag
time (min)
Diameter
(mm)
Thickness
(mm)
Friability
(%)
Weight
variation
Drug
content (%)
F1
4.66 1.1 9.94 4.66 0.64 400.07 95.55
F2
4.67 3.5 9.96 4.67 0.62 400.32 95.77
F3
4.69 4.3 9.97 4.68 0.57 400.05 95.72
F4
4.51 0.9 9.95 4.51 0.69 400.60 93.49
F5
4.59 3.2 9.98 4.59 0.65 400.45 95.70
F6
4.62 4.1 10.05 4.62 0.53 400.90 97.15
F7
4.42 0.3 10.00 4.42 0.68 400.23 94.57
F8
4.49 2.9 10.02 4.49 0.61 400.66 97.09
F9
4.54 3.8 10.01 4.54 0.55 400.03 96.83
F1
‑F9
: Factorial formulations
6. Gunda, et al.: Formulation development and evaluation of Atenolol Gastro Retentive Floating Tablets
Asian Journal of Pharmaceutics • Oct-Dec 2015 (Suppl) • 9 (4) | S39
corresponding decrease in the drug release, which might be
due to the result of thicker gel layer formulation.[25]
The in vitro dissolution data of atenolol floating formulations
was subjected to the goodness of fit test by linear regression
analysis according to zero order and first order kinetic
equations, Higuchi’s and Korsmeyer–Peppas models to assess
the mechanism of drug release. The results of linear regression
analysis including regression coefficients are summarized in
Table 4 and plots shown in Figures 1-4. It was observed from
the above that dissolution of all the tablets followed first order
kinetics with co-efficient of determination (R2
) values in the
range of 0.872-0.998. The values of r of factorial formulations
for Higuchi’s equation was found to be in the range of 0.931-
0.997, which shows that the dissolution data/drug release fitted
well to Higuchi’s square root of time equation confirming the
release followed diffusion mechanism. Kinetic data also treated
for Peppas equation, the slope (n) values ranges from 0.809
to 1.056 that shows non-Fickian diffusion mechanism (Super
Case-II Transport). Polynomial equations were derived for t10%,
t50%,
t75%
,and t90%
values by backward stepwise linear regression
analysis using PCP Disso software and Contour plots,
Response surface plots were constructed using SIGMAPLOT
V13 software. The Response surface plots and Contour plots
AQ3
were shown in Figures 5-12 for t10% to t90% using X1 and X2
on both the axes. The dissolution data (Kinetic parameters) of
factorial formulations F1
to F9
are shown in Table 5.
Polynomial equation for 3² full factorial designs is given in
Equation:
Table 4: Regression analysis data of 32
factorial design formulations of atenolol
Formulation
code
Kinetic parameters
Zero order First order Higuchi Korsmeyer–Peppas
a b r a b r a b r a b r
F1
12.134 7.713 0.969 1.992 0.071 0.996 5.284 27.408 0.991 0.959 1.056 0.938
F2
10.577 7.330 0.975 1.991 0.063 0.998 5.716 25.920 0.992 0.934 1.050 0.941
F3
9.402 7.168 0.978 1.991 0.058 0.998 6.300 25.234 0.991 0.909 1.059 0.949
F4
14.530 8.269 0.961 2.004 0.090 0.994 4.639 29.625 0.991 0.998 1.062 0.919
F5
12.924 7.403 0.959 1.978 0.066 0.994 4.295 26.553 0.990 0.965 1.043 0.914
F6
10.516 7.484 0.965 1.989 0.064 0.994 6.388 26.596 0.986 0.901 1.104 0.924
F7
42.206 6.711 0.808 1.926 0.159 0.872 20.915 26.853 0.931 1.300 0.809 0.822
F8
18.631 8.402 0.952 2.018 0.110 0.984 1.682 30.512 0.995 1.056 1.029 0.890
F9
16.334 8.466 0.964 2.026 0.105 0.986 3.459 30.413 0.997 1.031 1.044 0.910
MP 19.614 8.484 0.951 2.028 0.118 0.982 1.058 30.889 0.996 1.070 1.023 0.888
F1
‑F9
: Factorial formulations, r: Correlation coefficient, a: Intercept, b: Slope, MP: Marketed product
Figure 2: Comparative first order plots for F1
-F9
Figure 3: Comparative Higuchi plots for F1
-F9
Figure 4: Comparative Korsmeyer–Peppas plots for F1
-F9
7. Gunda, et al.: Formulation development and evaluation of Atenolol Gastro Retentive Floating Tablets
Asian Journal of Pharmaceutics • Oct-Dec 2015 (Suppl) • 9 (4) | S40
Y=b0
+b1
X1
+b2
X2
+b12
X1
X2
+b11
X1
2
+b22
X2
2
Where, Y is dependent variable, b0
arithmetic mean response
of nine batches, and b1
estimated co-efficient for factor X1
.
The main effects (X1
and X2
) represent the average result
of changing one factor at a time from its low to high value.
The interaction term (X1
X2
) shows how the response changes
when two factors are simultaneously changed. The polynomial
terms (X1
2
and X2
2
) are included to investigate non-linearity.
Validity of derived equations was verified by preparing two
checkpoint formulations of Intermediate concentration (C1
,C2
)
C1
is X1
=-0.5 X2
=-0.5 and C2
is X1
=0.5, X2
=0.5.
The equations for t10%
, t50%
t75%
,and t90%
developed as follows:
Y 58 169X 83X 2X X 9 7 X
52X (fo
1 2 1 2
2
2
1 = + - + -
-
0 0 0 0 0 0 00 0 0 0
0 0
1
2
. . . . .
. rr t )10%
Y 3 815 1112X 546X 12X X 597 X
341X (for
1 2 1 2
2
2
2 = + - + -
-
. . . . .
.
0 0 0 0
0
1
2
t )50%
Y 7 628 2 224X 1 93X 23X X 1193 X
681X (for t
1 2 1 23 = + - + -
-
. . . . .0 0 0 1
2
2
2
775% )
Figure 5: Response surface plot for t10%
Figure 6: Contour plot for t10%
Figure 7: Response surface plot for t50%
Figure 8: Contour plot for t50%
Table 5: Dissolution parameters of atenolol floating
tablets 3² full factorial design batches
Formulation
code
Kinetic parameters
t10%
(h) t50%
(h) t75%
(h) t90%
(h)
F1
0.641 4.215 8.429 14.005
F2
0.731 4.811 9.621 15.985
F3
0.784 5.157 10.314 17.137
F4
0.511 3.361 6.721 11.167
F5
0.694 4.567 9.133 15.175
F6
0.716 4.709 9.418 15.649
F7
0.287 1.888 3.775 6.273
F8
0.418 2.747 5.494 9.128
F9
0.437 2.876 5.751 9.555
MP 0.387 2.546 5.093 8.462
F1
‑F9
: Factorial formulations, MP: Marketed product
8. Gunda, et al.: Formulation development and evaluation of Atenolol Gastro Retentive Floating Tablets
Asian Journal of Pharmaceutics • Oct-Dec 2015 (Suppl) • 9 (4) | S41
Y 12 675 3 695X 1816X 375X X 1983 X
1132X (f
1 2 1 24 = + - + -
-
. . . . .
.
0 0 1
2
2
2
oor t )90%
The positive sign for co-efficient of X1
in Y1,
Y2,
Y3
, and Y4
equations indicates that, as the concentration of HPMC
K15M increases, t10%,
t50%,
t75%
and t90%
value increases. In other
words, the data demonstrate that both X1
(amount of HPMC
K15M) and X2
(amount of sodium bicarbonate) affect the
time required for drug release (t10%,
t50%,
t75%
and t90%
). From the
results, it can be concluded that, as the amount of polymer in
the tablet formulation increases, the drug release rate decreases
and as the concentration of gas generating agent (NaHCO3
)
increases the drug release increases, drug release pattern may
be changed by appropriate selection of the X1
and X2
levels.
The dissolution parameters for predicted from the polynomial
equations derived and those actual observed from experimental
results are summarized in Table 6. The closeness of predicted
and observed values for t10%,
t50%,
t75%
and t90%
indicates the
validity of derived equations for dependent variables. The
contour plots were presented to show the effects of X1
and X2
on t10%,
t50%,
t75%
,and t90%.
The final best (optimized) formulation
(F8
) is compared with marketed product (BETACARD) shows
similarity factor (f2
) 87.797, difference factor (f1
) 2.225 (There
is no significant difference in drug release because tcal
is <0.05).
CONCLUSION
The present research work envisages the applicability of rate
retarding agent and Gas generating agent such as HPMC
Figure 10: Contour plot for t75%
Figure 11: Response surface plot for t90%
Figure 12: Contour plot for t90%
Figure 9: Response surface plot for t75%
Table 6: Dissolution parameters for predicted and observed values for check point formulations
Formulation
code
Predicted value Actual observed value
t10%
(h) t50%
(h) t75%
(h) t90%
(h) t10%
(h) t50%
(h) t75%
(h) t90%
(h)
C1 0.502 3.300 6.600 10.966 0.505 3.303 6.602 10.970
C2 0.588 3.867 7.731 12.845 0.588 3.870 7.735 12.848
9. Gunda, et al.: Formulation development and evaluation of Atenolol Gastro Retentive Floating Tablets
Asian Journal of Pharmaceutics • Oct-Dec 2015 (Suppl) • 9 (4) | S42
K15M and sodium bicarbonate respectively in the design and
developmentofGastroRetentiveFloatingtabletformulationsof
Atenolol utilizing the 32
factorial design. From the results, it was
clearly understand that As the amount of polymer in the tablet
formulation increases, the drug release rate decreases and as the
concentration of gas generating agent (NaHCO3
) increases the
drug release increases and both of these polymers can be used
in combination since do not interact with the drug which may
be more helpful in achieving the desired floating delivery of the
drug for longer periods. The optimized formulation followed
Higuchi’s kinetics while the drug release mechanism was found
to be non-Fickian diffusion (Super Case-II Transport), first
order release type, controlled by diffusion through the swollen
matrix. On the basis of evaluation parameters, the optimized
formulation F8
may be used once a day administration in the
management of hypertension and angina pectoris.
ACKNOWLEDGMENTS
The author would like to thank Management, Principal,
Teaching, Non-teaching Staff of Narasaraopeta Institute of
Pharmaceutical Sciences, Narasaraopet, Guntur, Andhra
Pradesh,Indiaforprovidingsupportforsuccessfulcompletion
of research work.
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Source of Support: Nil. Conflict of Interest: None declared.