The document discusses the formulation and evaluation of solid dispersions of the drug carvedilol to improve its solubility and dissolution rate. Carvedilol was selected as it has low aqueous solubility and bioavailability. Solid dispersions were prepared using different carriers like poloxamer 407, mannitol, and PEG 4000 via solvent evaporation method. The dispersions were evaluated for dissolution rate and the best formulation was selected based on the evaluation studies. Stability studies were also proposed to be conducted on the best formulation.
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
DEVELOPMENT & EVALUATION OF MUCOADHESIVE MICROSPHERES OF PIOGLITAZONE MALEATERam C Dhakar
This document summarizes the development and evaluation of mucoadhesive microspheres for the controlled release of pioglitazone maleate. Mucoadhesive microspheres were prepared using sodium carboxymethyl cellulose (SCMC), carbopol 934P (CP), and sodium alginate (SA) as polymers via an emulsification solvent evaporation method. The microspheres were evaluated for particle size, drug entrapment efficiency, mucoadhesion, and in vitro drug release. Microspheres containing SCMC showed the smoothest surface, highest mucoadhesion and drug release over 10 hours. Overall, the study developed pioglitazone-loaded microspheres for controlled
Formulation and evaluation of mucoadhesive tablets of carvedilol using natura...Nausheen Fatima
Present work describes formulation and evaluation mucoadhesive tablets of Carvedilol using natural binders such as Chitosan and Guar Gum to reduce the first pass metabolism and frequency of administration.
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
This document describes the development and evaluation of bilayer tablets containing capecitabine and ondansetron. The bilayer tablet uses Dual Release Drug Absorption System (DUREDAS) technology, providing sustained release of capecitabine in one layer and immediate release of ondansetron in another layer. Various excipients were evaluated to optimize the drug release profiles from each layer. Pre-formulation studies and tablet evaluations were conducted to develop a cost-effective bilayer tablet formulation for once-daily treatment of nausea and vomiting.
Formulation and evaluation of Muco adhesive Buccal Tablets of Ramprildoddaapurupa
The buccal mucosa lines the inner cheek and Buccal formulations are placed in the mouth between upper gingiva(gums) and cheek to treat local and systemic conditions.
Drugs which undergoes Extensive first pass metabolism and drug degradation in acidic media, GI tract can be administered through buccal route.
The oral cavity has been used as a site for local and systemic drug delivery.
Formulation and evalution of sustained release matrix tabletsSanthosh Kumar
This document summarizes the formulation and evaluation of sustained release matrix tablets containing gliclazide. The objectives were to develop a once-daily tablet to reduce side effects and fluctuations in drug levels compared to immediate release tablets. Various polymers like HPMC K4M, HPMC K100LV, poloxamer 188, and PVP K30 were used to formulate sustained release matrix tablets by wet granulation. The tablets were evaluated for weight variation, hardness, friability, drug content and in vitro drug release over 20 hours. The optimized formulation showed comparable drug release to the innovator's product over the tested time period.
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
DEVELOPMENT & EVALUATION OF MUCOADHESIVE MICROSPHERES OF PIOGLITAZONE MALEATERam C Dhakar
This document summarizes the development and evaluation of mucoadhesive microspheres for the controlled release of pioglitazone maleate. Mucoadhesive microspheres were prepared using sodium carboxymethyl cellulose (SCMC), carbopol 934P (CP), and sodium alginate (SA) as polymers via an emulsification solvent evaporation method. The microspheres were evaluated for particle size, drug entrapment efficiency, mucoadhesion, and in vitro drug release. Microspheres containing SCMC showed the smoothest surface, highest mucoadhesion and drug release over 10 hours. Overall, the study developed pioglitazone-loaded microspheres for controlled
Formulation and evaluation of mucoadhesive tablets of carvedilol using natura...Nausheen Fatima
Present work describes formulation and evaluation mucoadhesive tablets of Carvedilol using natural binders such as Chitosan and Guar Gum to reduce the first pass metabolism and frequency of administration.
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
This document describes the development and evaluation of bilayer tablets containing capecitabine and ondansetron. The bilayer tablet uses Dual Release Drug Absorption System (DUREDAS) technology, providing sustained release of capecitabine in one layer and immediate release of ondansetron in another layer. Various excipients were evaluated to optimize the drug release profiles from each layer. Pre-formulation studies and tablet evaluations were conducted to develop a cost-effective bilayer tablet formulation for once-daily treatment of nausea and vomiting.
Formulation and evaluation of Muco adhesive Buccal Tablets of Ramprildoddaapurupa
The buccal mucosa lines the inner cheek and Buccal formulations are placed in the mouth between upper gingiva(gums) and cheek to treat local and systemic conditions.
Drugs which undergoes Extensive first pass metabolism and drug degradation in acidic media, GI tract can be administered through buccal route.
The oral cavity has been used as a site for local and systemic drug delivery.
Formulation and evalution of sustained release matrix tabletsSanthosh Kumar
This document summarizes the formulation and evaluation of sustained release matrix tablets containing gliclazide. The objectives were to develop a once-daily tablet to reduce side effects and fluctuations in drug levels compared to immediate release tablets. Various polymers like HPMC K4M, HPMC K100LV, poloxamer 188, and PVP K30 were used to formulate sustained release matrix tablets by wet granulation. The tablets were evaluated for weight variation, hardness, friability, drug content and in vitro drug release over 20 hours. The optimized formulation showed comparable drug release to the innovator's product over the tested time period.
This document provides an overview of enteric coating polymers that are used to protect acid-labile drugs and ensure optimal drug absorption. It discusses various categories of enteric coating polymers including polymethacrylates (Eudragit), cellulose esters, and polyvinyl derivatives. Key points include: Eudragit polymers are commonly used methacrylic acid copolymers that are insoluble in gastric fluid but dissolve in the intestine. Cellulose esters like cellulose acetate phthalate are also widely employed. These polymers form films that protect the drug core from gastric conditions and dissolve above pH 6, allowing drug release in the intestines. The solubility and properties of different enteric coating polymers allow controlling
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 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.
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
Formulation development and invitro evaluation of lamotrigine fast dissolving...SriramNagarajan19
The present study was to formulate and evaluate oral fast dissolving Oral tablet containing Lamotrigine. Present study reveals that all the nine formulated tablet showed satisfactory tablet parameters. It can be concluded that, Oral fast dissolving tablet -containing Lamotrigine can be prepared by direct compression method. 10% CCS (FV) tablet exhibited required disintegration time and dissolution time. The drug release was about 98.7 % in 15min. The accelerated stability studies of the optimized F5 formulation indicates that the formulated oral fast dissolving tablet were unaffected after 3 months storage under accelerated conditions as there were no signs of visually distinguishable changes in appearance, disintegration time and cumulative percentage of drug release. From the present investigation it can be concluded that oral fast dissolving tablet formulation can be a potential novel drug dosage form for pediatric, geriatric and also for general population.
Formulation and Evaluation of Enteric Coated Tablet of Rabeprazole Sodium.Ravindra Lohar
This document presents a dissertation thesis submitted for the degree of Master of Pharmacy in Pharmaceutics. The thesis investigates the formulation and evaluation of enteric coated tablets of Rabeprazole sodium, an anti-ulcer drug. Various studies were conducted including identification of the drug, evaluation of powder blends, drug-excipient compatibility, preparation of core tablets using different disintegrants, and coating of the tablets with an enteric polymer. The formulated tablets were then evaluated for parameters like hardness, thickness, friability, drug content, and disintegration time in acid and buffer media. The results of these evaluations are presented and discussed in the document.
Formulation and Evaluation of Liquisolid Compacts of CarvedilolIOSR Journals
The purpose of this study is to develop a novel liquisolid technique to enhance the dissolution rate of
poorly water soluble drug Carvedilol, a BCS class II drug, which is a β-blocker, by using different excipients.
The main components of a liquisolid system are a non volatile solvent, carrier and coating materials and a
disintegrant. Liquisolid system refers to the formulations that are formed by conversion of liquid drugs, drug
suspensions or drug solution in non-volatile solvents into dry, non adherent, free flowing and compressible
powder mixture by blending with suitable carrier and coating materials. Hence the dissolution step, a prerequisite
for drug absorption, is by passed and better bioavailability of poorly soluble drug is achieved.
Liquisolid tablets of carvedilol are prepared by using PEG, PG, glycerine as non volatile liquid vehicles and
Avicel PH 101 and 102, Aerosil as carrier and coating materials respectively. Optimized formulation containing
20% drug in PEG 400, with Avicel 101 as carrier and Aerosil as coating material has shown 98.4% drug
release within 20 min which is better than marketed product (CARCA 12.5mg, Intas). The DSC and X-RD
studies are performed to investigate the physicochemical properties of formulation and drug excipient
interactions. The results are found to be satisfactory
liquisolid technology is a topic related to pharmaceutics presented by konatham teja kumar reddy from chilkur balaji college of pharmcy ,hyderabad,telangana
Formulation and evaluation ofmetformin HCl micro beads by ionotropic gelation...Sagar Savale
The Metformin HCL Micro Beads is formulated by the Ionotropic Gelation Method. The CMC is a Swellable
polymer is responsible for the Sustained release action or activity. A combination of CMC (Carboxy Methyl
Cellulose) and Sodium Alginate shows better sustained release activity. The PreparedSustained released Micro
Beadsis Evaluated In terms of bulk density, tapped density, angle of repose, Carr’s Index, Swelling Index, Drug
Content, % Encapsulation Efficiency and vitro study. The result associated in Optimized batch is good to
Satisfactory and having a good free flowing property. The Drug Content and % Encapsulation Efficiency values are
within the pharmacopeia limit. The in vitro Dissolution studies shows Maximum percentage of release of drug
(71.15) with in end of 4 Hours.
This document discusses the formulation and evaluation of bilayer tablets containing domperidone maleate. Bilayer tablets provide dual drug release and separation of incompatible substances. Domperidone is an antiemetic and used to treat nausea. Various pre-compression studies were conducted on formulations to optimize flow and compressibility. Tablets were developed using wet granulation and contained different polymers for immediate and sustained release layers. Post-compression testing included weight variation, hardness, friability, disintegration and dissolution studies. The project timeline included formulation, evaluation, stability studies and report preparation over 4 months.
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
Abstract:
The purpose of present research work was to
optimize the formulation of fast dissolving tablet
of carbamazepine. Carbamazepine is one the most
prescribed antiepileptic drug. Fast dissolving
tablets of carbamazepine were prepared by using
different types of superdisintegrants like
croscarmellose sodium and sodium starch
glycolate. Fast dissolving tablet is prepared by
direct compression method. The formulations
were evaluated for wetting time, hardness,
friability, content uniformity, invitro
disintegration time, release profile. The result
revealed that the formulation F5 which containing
the 5% croscarmellose sodium as a
superdisintegrant have good dissolution profile
with shortest Disintegration time. It can be
concluded that the tablet of carbamazepine with
better pharmaceutical properties than conventional
tablets could be obtained using formulation F5.
Effect of novel carrier on liquisolid compact of carbamazepineVishal Mohite
This document provides an introduction and objectives for a study on the effect of novel carriers on the properties of liquisolid compacts of carbamazepine. The study aims to formulate liquisolid compacts using carbamazepine as a model drug and evaluate the dissolution and drug release properties. Various experimental works are outlined, including preformulation studies of the drug and excipients, determination of solubility in non-volatile solvents, measurement of flowable liquid retention potential of carriers, and development and evaluation of liquisolid tablets. The overall goal is to investigate the use of novel porous carriers to enhance solubility and dissolution rate for drugs with high therapeutic doses.
Formulation and evaluation of effervescent tablets.pptxParimal Hadge
This document discusses the formulation and evaluation of effervescent tablets. It begins by defining effervescent tablets as tablets intended to be dissolved or dispersed in water before administration. They generally contain acid substances that react with carbonates or bicarbonates to release carbon dioxide when exposed to water. The document then outlines the advantages of effervescent tablets such as fast onset of action and improved palatability. It provides details on common active ingredients, preparation methods, ingredients used, manufacturing techniques, and evaluation parameters for effervescent tablets including disintegration time, dissolution testing, and content uniformity.
Formulation and Evaluation of Risperidone Fast Dissolving TabletsSunil Vadithya
The document discusses the formulation and evaluation of risperidone fast dissolving tablets. Four formulations of risperidone FDTs were developed using different concentrations and combinations of crospovidone and croscarmellose sodium as superdisintegrants. The tablets were prepared by direct compression method and evaluated for characteristics like hardness, friability, thickness, drug content, wetting time, disintegration time and in-vitro drug release. Formulation F2 showed the most promising results with no drug-excipient interactions. Stability studies on F2 for one month also showed acceptable results, making it the optimized risperidone FDT formulation.
This document discusses approaches for injectable controlled release formulations. It begins by defining controlled release as the delivery of a drug at a predetermined rate to maintain optimal levels over a prolonged duration. It then discusses various approaches including dissolution controlled, adsorption type depots, encapsulation systems, and esterification type depots. Specific examples are provided for each approach. The document also discusses formulations like microparticles, nanoparticles, and liposomes that can provide controlled release when administered via injection.
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.
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.
The document describes the preparation and evaluation of controlled release matrix tablets of metformin hydrochloride. Ten formulations of matrix tablets were prepared using different amounts of polymers HPMC K100 and Carbapol 934 by direct compression method. The tablets were evaluated for pre-compression and post-compression parameters. In vitro drug release studies showed sustained release of the drug from the matrix tablets over an extended period of time based on the type and concentration of polymer used. The kinetic analysis of drug release indicated that the release followed non-fickian or anomalous transport mechanism.
This document provides a synopsis for a Master's thesis project titled "Formulation and Evaluation of Fast Dissolving Films of Lisinopril". The project aims to develop fast dissolving films of the hypertension drug Lisinopril to improve patient compliance. Literature on fast dissolving drug delivery systems and films has been reviewed. The planned work involves preparing Lisinopril films using natural and synthetic polymers through various techniques and evaluating the films for properties like drug content, dissolution, and pharmacodynamics. If successful, the fast dissolving Lisinopril films could provide quick action and ease of administration benefits for hypertension patients.
This document provides an overview of enteric coating polymers that are used to protect acid-labile drugs and ensure optimal drug absorption. It discusses various categories of enteric coating polymers including polymethacrylates (Eudragit), cellulose esters, and polyvinyl derivatives. Key points include: Eudragit polymers are commonly used methacrylic acid copolymers that are insoluble in gastric fluid but dissolve in the intestine. Cellulose esters like cellulose acetate phthalate are also widely employed. These polymers form films that protect the drug core from gastric conditions and dissolve above pH 6, allowing drug release in the intestines. The solubility and properties of different enteric coating polymers allow controlling
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 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.
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
Formulation development and invitro evaluation of lamotrigine fast dissolving...SriramNagarajan19
The present study was to formulate and evaluate oral fast dissolving Oral tablet containing Lamotrigine. Present study reveals that all the nine formulated tablet showed satisfactory tablet parameters. It can be concluded that, Oral fast dissolving tablet -containing Lamotrigine can be prepared by direct compression method. 10% CCS (FV) tablet exhibited required disintegration time and dissolution time. The drug release was about 98.7 % in 15min. The accelerated stability studies of the optimized F5 formulation indicates that the formulated oral fast dissolving tablet were unaffected after 3 months storage under accelerated conditions as there were no signs of visually distinguishable changes in appearance, disintegration time and cumulative percentage of drug release. From the present investigation it can be concluded that oral fast dissolving tablet formulation can be a potential novel drug dosage form for pediatric, geriatric and also for general population.
Formulation and Evaluation of Enteric Coated Tablet of Rabeprazole Sodium.Ravindra Lohar
This document presents a dissertation thesis submitted for the degree of Master of Pharmacy in Pharmaceutics. The thesis investigates the formulation and evaluation of enteric coated tablets of Rabeprazole sodium, an anti-ulcer drug. Various studies were conducted including identification of the drug, evaluation of powder blends, drug-excipient compatibility, preparation of core tablets using different disintegrants, and coating of the tablets with an enteric polymer. The formulated tablets were then evaluated for parameters like hardness, thickness, friability, drug content, and disintegration time in acid and buffer media. The results of these evaluations are presented and discussed in the document.
Formulation and Evaluation of Liquisolid Compacts of CarvedilolIOSR Journals
The purpose of this study is to develop a novel liquisolid technique to enhance the dissolution rate of
poorly water soluble drug Carvedilol, a BCS class II drug, which is a β-blocker, by using different excipients.
The main components of a liquisolid system are a non volatile solvent, carrier and coating materials and a
disintegrant. Liquisolid system refers to the formulations that are formed by conversion of liquid drugs, drug
suspensions or drug solution in non-volatile solvents into dry, non adherent, free flowing and compressible
powder mixture by blending with suitable carrier and coating materials. Hence the dissolution step, a prerequisite
for drug absorption, is by passed and better bioavailability of poorly soluble drug is achieved.
Liquisolid tablets of carvedilol are prepared by using PEG, PG, glycerine as non volatile liquid vehicles and
Avicel PH 101 and 102, Aerosil as carrier and coating materials respectively. Optimized formulation containing
20% drug in PEG 400, with Avicel 101 as carrier and Aerosil as coating material has shown 98.4% drug
release within 20 min which is better than marketed product (CARCA 12.5mg, Intas). The DSC and X-RD
studies are performed to investigate the physicochemical properties of formulation and drug excipient
interactions. The results are found to be satisfactory
liquisolid technology is a topic related to pharmaceutics presented by konatham teja kumar reddy from chilkur balaji college of pharmcy ,hyderabad,telangana
Formulation and evaluation ofmetformin HCl micro beads by ionotropic gelation...Sagar Savale
The Metformin HCL Micro Beads is formulated by the Ionotropic Gelation Method. The CMC is a Swellable
polymer is responsible for the Sustained release action or activity. A combination of CMC (Carboxy Methyl
Cellulose) and Sodium Alginate shows better sustained release activity. The PreparedSustained released Micro
Beadsis Evaluated In terms of bulk density, tapped density, angle of repose, Carr’s Index, Swelling Index, Drug
Content, % Encapsulation Efficiency and vitro study. The result associated in Optimized batch is good to
Satisfactory and having a good free flowing property. The Drug Content and % Encapsulation Efficiency values are
within the pharmacopeia limit. The in vitro Dissolution studies shows Maximum percentage of release of drug
(71.15) with in end of 4 Hours.
This document discusses the formulation and evaluation of bilayer tablets containing domperidone maleate. Bilayer tablets provide dual drug release and separation of incompatible substances. Domperidone is an antiemetic and used to treat nausea. Various pre-compression studies were conducted on formulations to optimize flow and compressibility. Tablets were developed using wet granulation and contained different polymers for immediate and sustained release layers. Post-compression testing included weight variation, hardness, friability, disintegration and dissolution studies. The project timeline included formulation, evaluation, stability studies and report preparation over 4 months.
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
Abstract:
The purpose of present research work was to
optimize the formulation of fast dissolving tablet
of carbamazepine. Carbamazepine is one the most
prescribed antiepileptic drug. Fast dissolving
tablets of carbamazepine were prepared by using
different types of superdisintegrants like
croscarmellose sodium and sodium starch
glycolate. Fast dissolving tablet is prepared by
direct compression method. The formulations
were evaluated for wetting time, hardness,
friability, content uniformity, invitro
disintegration time, release profile. The result
revealed that the formulation F5 which containing
the 5% croscarmellose sodium as a
superdisintegrant have good dissolution profile
with shortest Disintegration time. It can be
concluded that the tablet of carbamazepine with
better pharmaceutical properties than conventional
tablets could be obtained using formulation F5.
Effect of novel carrier on liquisolid compact of carbamazepineVishal Mohite
This document provides an introduction and objectives for a study on the effect of novel carriers on the properties of liquisolid compacts of carbamazepine. The study aims to formulate liquisolid compacts using carbamazepine as a model drug and evaluate the dissolution and drug release properties. Various experimental works are outlined, including preformulation studies of the drug and excipients, determination of solubility in non-volatile solvents, measurement of flowable liquid retention potential of carriers, and development and evaluation of liquisolid tablets. The overall goal is to investigate the use of novel porous carriers to enhance solubility and dissolution rate for drugs with high therapeutic doses.
Formulation and evaluation of effervescent tablets.pptxParimal Hadge
This document discusses the formulation and evaluation of effervescent tablets. It begins by defining effervescent tablets as tablets intended to be dissolved or dispersed in water before administration. They generally contain acid substances that react with carbonates or bicarbonates to release carbon dioxide when exposed to water. The document then outlines the advantages of effervescent tablets such as fast onset of action and improved palatability. It provides details on common active ingredients, preparation methods, ingredients used, manufacturing techniques, and evaluation parameters for effervescent tablets including disintegration time, dissolution testing, and content uniformity.
Formulation and Evaluation of Risperidone Fast Dissolving TabletsSunil Vadithya
The document discusses the formulation and evaluation of risperidone fast dissolving tablets. Four formulations of risperidone FDTs were developed using different concentrations and combinations of crospovidone and croscarmellose sodium as superdisintegrants. The tablets were prepared by direct compression method and evaluated for characteristics like hardness, friability, thickness, drug content, wetting time, disintegration time and in-vitro drug release. Formulation F2 showed the most promising results with no drug-excipient interactions. Stability studies on F2 for one month also showed acceptable results, making it the optimized risperidone FDT formulation.
This document discusses approaches for injectable controlled release formulations. It begins by defining controlled release as the delivery of a drug at a predetermined rate to maintain optimal levels over a prolonged duration. It then discusses various approaches including dissolution controlled, adsorption type depots, encapsulation systems, and esterification type depots. Specific examples are provided for each approach. The document also discusses formulations like microparticles, nanoparticles, and liposomes that can provide controlled release when administered via injection.
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.
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.
The document describes the preparation and evaluation of controlled release matrix tablets of metformin hydrochloride. Ten formulations of matrix tablets were prepared using different amounts of polymers HPMC K100 and Carbapol 934 by direct compression method. The tablets were evaluated for pre-compression and post-compression parameters. In vitro drug release studies showed sustained release of the drug from the matrix tablets over an extended period of time based on the type and concentration of polymer used. The kinetic analysis of drug release indicated that the release followed non-fickian or anomalous transport mechanism.
This document provides a synopsis for a Master's thesis project titled "Formulation and Evaluation of Fast Dissolving Films of Lisinopril". The project aims to develop fast dissolving films of the hypertension drug Lisinopril to improve patient compliance. Literature on fast dissolving drug delivery systems and films has been reviewed. The planned work involves preparing Lisinopril films using natural and synthetic polymers through various techniques and evaluating the films for properties like drug content, dissolution, and pharmacodynamics. If successful, the fast dissolving Lisinopril films could provide quick action and ease of administration benefits for hypertension patients.
Formulation and Evaluation of Solid dispersion for Dissolution Enhancement of...Jing Zang
The document summarizes research on developing solid dispersions of the poorly water soluble drug nifedipine to enhance its dissolution rate. Solid dispersions of nifedipine were prepared using different polymers (sodium starch glycollate, croscarmellose sodium, eudragit E-100) at various weight ratios using solvent evaporation. The best formulation with croscarmellose sodium at a 1:7 ratio showed over 70% increased dissolution compared to nifedipine API. This formulation was further adsorbed onto neusilin US2 to form a ternary mixture, which showed over 30% higher dissolution than the marketed product. Tablets prepared from the ternary mixture were stable
Formulation and evaluation of Tretinoin emulgel – an advanced approach for enhanced topical drug delivery
This document discusses the formulation and evaluation of an emulgel containing the drug Tretinoin for topical delivery. Tretinoin emulgel was developed to improve the topical delivery and skin permeation of Tretinoin compared to conventional formulations. Various emulgel formulations with different concentrations of ingredients were prepared and evaluated based on parameters like physical appearance, pH, viscosity, drug content and diffusion studies. The results showed that formulations with optimal concentrations of surfactants and permeation enhancers demonstrated better properties for topical delivery of Tretinoin.
Formulation and Evaluation of Fast Disintegrating Tablet of Solid Dispersion ...ijtsrd
This document describes the formulation and evaluation of fast-disintegrating tablets containing a solid dispersion of the poorly water-soluble drug carvedilol. Solid dispersions of carvedilol with PEG6000 and PVP K30 in various ratios were prepared using the kneading method and evaluated for solubility, drug content, and in vitro drug release. The F3 formulation with PEG6000 in a 1:3 ratio showed the highest drug release of 96.61% within 40 minutes. This optimized solid dispersion was then used to prepare fast-disintegrating tablets by direct compression. The tablets were evaluated for disintegration time, drug release, and other parameters. Tablet FD6 was selected as the optimized formulation as it
Investigating the Effect of Molecular Weight of Polyvinylpyrrolidone and Hydr...Smruti Chaudhari, Ph.D.
This document summarizes a study investigating the effect of molecular weight of polyvinylpyrrolidone (PVP) and hydroxypropyl methyl cellulose (HPMC) polymers on maintaining supersaturation of the weakly acidic drug indomethacin. Non-formulated methods like solvent shift and solvent casting were used to screen the ability of different PVP and HPMC grades to generate and maintain indomethacin supersaturation. Solid dispersions of indomethacin with PVP and HPMC were also prepared using spray drying. Results showed that higher molecular weight PVP generated greater supersaturation while higher molecular weight HPMC generated lower supersaturation. Solid dispersions with high molecular weight P
The document discusses a study on enhancing the solubility of loratadine, a class II drug with low solubility and high permeability, through solid dispersion techniques. Loratadine's solubility decreases with increasing pH. The study prepares solid dispersions of loratadine with β-cyclodextrin, HPC, and PEG-6000 and finds their solubility is greatly improved, especially at higher pH levels. Solubility is tested in buffers from pH 1.2 to 7.4. The co-precipitation method provides better solubility results than physical mixing for the dispersions tested.
The document discusses self-emulsifying drug delivery systems (SEDDS), which are isotropic mixtures of oils, surfactants, and co-solvents that can improve the oral bioavailability of lipophilic drugs. SEDDS form fine oil-in-water emulsions when exposed to aqueous fluids in the gastrointestinal tract. The document defines SEDDS and outlines their advantages, components, mechanisms of self-emulsification, evaluation methods, and formulations like capsules. SEDDS are a promising approach for improving absorption of BCS Class II and IV drugs with poor solubility.
International Journal of Drug Research and Technology covers: Medicinal Chemistry, Computational Chemistry and Molecular Drug Design, Drug Synthesis, Pharmaceutical Chemistry, Pharmacology and Toxicology, Pharmaceutical Technology, Pharmacognosy and Phytochemistry, Pharmaceutics, Pharmacy Practice, Biopharmaceutics, Pharmacokinetics and Drug Metabolism, Pharmaceutical Analysis and Quality Assurance, Clinical and Hospital Pharmacy, Pharmaceutical Biotechnology, Cell Biology, Genomics and Proteomics, Pharmacogenomics, Bioinformatics, Clinical Research, Pharmaceutical Management & Regulatory Affairs and Nanotechnology related to Drug Discovery and all the branches of Medical Science or related disciplines.
International Journal of Drug Research and Technology covers: Medicinal Chemistry, Computational Chemistry and Molecular Drug Design, Drug Synthesis, Pharmaceutical Chemistry, Pharmacology and Toxicology, Pharmaceutical Technology, Pharmacognosy and Phytochemistry, Pharmaceutics, Pharmacy Practice, Biopharmaceutics, Pharmacokinetics and Drug Metabolism, Pharmaceutical Analysis and Quality Assurance, Clinical and Hospital Pharmacy, Pharmaceutical Biotechnology, Cell Biology, Genomics and Proteomics, Pharmacogenomics, Bioinformatics, Clinical Research, Pharmaceutical Management & Regulatory Affairs and Nanotechnology related to Drug Discovery and all the branches of Medical Science or related disciplines.
International Journal of Drug Research and Technology IJDRT.COM, Research Article, Review Article,innovative papers, literature reviews, mini-reviews, current topics health journal, journal online, free journal, pharmaceutical journal, scientific journal,web journal.
The document summarizes the formulation and evaluation of diclofenac sodium and thiocolchicoside as a topical gel. It describes preparing 6 formulations of gel using different polymers and permeation enhancers. The formulations were characterized for physical properties, pH, drug content, viscosity, spreadability, extrudability and stability. In vitro drug permeation and skin irritation studies were also performed to select the best formulation. Preformulation studies including solubility, melting point, UV, FTIR and DSC were done on the drugs and excipients to ensure compatibility. The results of various evaluation tests are presented and the best gel formulation is selected based on desired properties.
SOLID DISPERSION
Definition: The technology is the science of dispersing one or more active ingredients in an inert matrix in the solid stage.
Need of solid dispersion:
Increases Oral bioavailability of a drug
Increased dissolution rate.
Enhanced release of drugs from ointment.
Improved the solubility & stability.
The concept of solid dispersion was originally proposed by Sekiguchi & obi.
Increasing the dissolution, absorption & therapeutic efficacy of drugs in dosage forms.
Increasing solubility in water.
Improving the oral absorption and bioavailability of BCS Class II drugs.
The document discusses the formulation and evaluation of gastro-retentive mucoadhesive microballoons of nizatidine for the management of peptic ulcer. It provides background information on peptic ulcers, drug delivery systems, gastroretentive drug delivery systems, and mechanisms of bioadhesion. The objective is to develop mucoadhesive microballoons of nizatidine to increase its retention time in the stomach and improve the treatment of peptic ulcers.
ABSTRACT
The aim of the present research work was to enhance the solubility of
Carvedilol by solid dispersion method and to formulate a mouth
dissolving tablet. Drugs are more frequently taken by oral
administration. The solubility of Carvedilol enhanced with different
ratios of PVP by the solvent evaporation method .In-vitro release
profile of solid dispersion obtained in SGF without enzymes and Ph
6.8 phosphate buffer indicate that 100% drug release found within 20
min. These solid dispersion were directly compressed into tablets using
Crospovidone, sodium starch glycol ate, croscarmellose sodium and
polyacrylic potassium in different concentrations as a super
disintegrants. The prepared tablets containing the solid dispersion of
Carvedilol having sufficient strength of 2.5-4 kg/cm2. The
disintegrated in the oral cavity with in 21 sec. contain Crospovidone
(5%) as super disintegrant.
KEYWORDS: Carvedilol, PVP, Super Disintegrants, Mouth Dissolving Tablet.
The document describes the formulation and evaluation of Ritonavir floating tablets. It discusses Ritonavir's properties and uses floating drug delivery systems to prolong its release rate in the stomach. Several polymers like HPMC K4M, HPMC K15M, Eudragit RSPO and ethyl cellulose were used to formulate the tablets. The tablets were evaluated for parameters like weight variation, thickness, hardness, drug content and in vitro buoyancy and dissolution studies. The results showed that the floating tablets were able to prolong the release of Ritonavir in the stomach.
The document describes a study that aimed to enhance the solubility and dissolution of the poorly water soluble drug Artesunate by preparing solid dispersions using two polymers, β-cyclodextrin and PEG 6000. Solid dispersions of Artesunate with the polymers were produced using different methods and showed increased solubility and dissolution compared to pure Artesunate. The solid dispersions were characterized using solubility studies, FTIR, XRD, and DSC to analyze drug-carrier interactions. The developed formulations improved Artesunate bioavailability by overcoming limitations of existing sustained release formulations.
Evaluating the Effects of Different Molecular Weights of Polymers in Stabiliz...Smruti Chaudhari, Ph.D.
This document evaluates the effects of different molecular weights of polymers on stabilizing supersaturated drug solutions and formulations using fenofibrate as a model drug. Three grades each of HPMC (E5, E15, E50) and PVP (K12, K29, K90) were studied using two approaches - a non-formulated drug method (solvent shift) and a formulated drug method (solvent casting and spray drying). Miniaturized testing suggested HPMC E5 and PVP K29 best extended and stabilized supersaturated solutions. Spray-dried dispersions showed polymer molecular weight and amount influenced stability, with high molecular weight polymers more stable at high drug loading, though governing dissolution.
Nanosuspensions accelerate drug substance dissolution rates by increasing surface area and reducing particle size. The key to nanosuspension development is the identification of a suitable delivery system, such that nano-technology.
Formulation and development of garcinia indica nano suspension
srikanth final presentation
1. UNDER THE GUIDANCE OF
Smt. BALA Tripura Sundari
Assistant professor
Navuluri Srikanth
170512886003
M.Pharm II yr
Pharmaceutics
FORMULATION AND EVALUATION OF SOLID
DISPERSIONS OF CARVEDILOL
2. Contents
Aim and Objective
Plan of work
literature survey
Experimental Methodology
Results and Discussions
References
Sri Venkateshwara College of Pharmacy, Madhapur 216/12/2014
3. Aim and Objective:
To improve Solubility and dissolution rate of
Carvedilol
To Prepare and Evaluate Solid Dispersions of
Carvedilol.
Fill solid dispersions in Capsules and Optimization
Sri Venkateshwara College of Pharmacy, Madhapur 316/12/2014
4. INTRODUCTION
“ Solid dispersion technology is the science of dispersing
one or more active ingredients in an inert matrix in the
solid stage to achieve an increased dissolution rate or
sustained release of drug, altered solid state properties and
improved stability”.
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5. Types of Solid Dispersions
Simple Eutectic Mixtures
Solid solutions
Glass solutions
Compound or complex formation
Amorphous precipitation
Sri Venkateshwara College of Pharmacy, Madhapur 516/12/2014
6. Methods of preparation of Solid dispersions :
Various methods used for preparation of solid dispersions
are given bellow-
A) Fusion method
B) Solvent Evaporation method
C) Fusion solvent method (melt evaporation)
D) Melt extrusion methods
E) Lyophilization techniques
F) Melt agglomeration Process
G) The use of surfactant
H) Electro spinning
Sri Venkateshwara College of Pharmacy, Madhapur 616/12/2014
7. Applications of solid dispersions
To obtain a homogenous distribution of small amount of drugs
at solid state.
To stabilize unstable drugs.
To dispense liquid or gaseous compounds
To formulate a faster release priming dose in a sustained
release dosage form.
To improve the absorption of drugs by improving solubility of
the drug
The bioavailability of the drug is also increased by using solid
dispersions.
Sri Venkateshwara College of Pharmacy, Madhapur 716/12/2014
8. Materials used as carriers for solid dispersions :
1.Sugars:Dextrose, Sucrose, Galactose, Sorbitol, Maltose, Mannitol.
2 .Acids :Citric acid, Succinic Acid .
3 .Polymeric materials : PVP, PEG
4.Celluloses like HPMC,HEC, HPC, Pectin, Galactomannan, CDs .
5 .Insoluble/ enteric polymers like HPMC, Phthalate, Eudragits .
6 .Surfactants : Polyoxyethylene stearate, Renex, Poloxamers, texafor,
Deoxycholic acid, Tweens, Spans.
Sri Venkateshwara College of Pharmacy, Madhapur 816/12/2014
9. Solid dispersions can be Formulated in-
Spraying on sugar beads using a fluidized bed coating
system.
Direct Capsule filling
Electrostatic Spinning method
Self Emulsifying Drug Delivery Systems (Solid
dispersions).
Sri Venkateshwara College of Pharmacy, Madhapur 916/12/2014
10. Marketed solid dispersions
S.NO Trade Name Drug Company Polymer
1 Afeditab Nifedifine ELAN CORP. PVP
2 Certican Everolimus NOVARTIS HPMC
3 Fenoglide Fenofibrate LIFE CYCLE PEG
4 Intelence Etaverine TIBOTEC HPMC
5 Isoptin SRE-
240
Verapamil SOLIQS Various
6 Kaletra Ritonavir &
Lopinavir
ABOTT PVP
PVA
7 LCP-Tacro Tacrolimus LIFE CYCLE HPMC
8 Sporanox Itraconazole JANSSEN HPMC
Sri Venkateshwara College of Pharmacy, Madhapur 1016/12/2014
12. Plan Of Work
Selection of drug.
Determination of λmax of Carvedilol drug and preparation of
standard graph.
Formulation of Carvedilol Solid dispersions.
Evaluation of Solid dispersions.
In vitro drug release studies.
Selection of the best formulation based on the above studies.
Drug-Interaction studies for best formulation.
Stability studies.
Sri Venkateshwara College of Pharmacy, Madhapur 1216/12/2014
13. Literature survey
Sarita Jangra Bhyan et al (2013), Formulated and evaluated Mouth
dissolving tablets containing Carvedilol solid dispersions by using Polyvinyl
pyrrolidine (PVP k30) as carrier the formulation showed almost 100% drug
release at the end of 15 minutes.
Kadam vaishali et al (2013), formulated and evaluated and evaluated
Carvedilol solid dispersions by using various carriers like poloxamer 188,
Polyvinyl pyrrolidine k90 which showed increased dissolution rates. FTIR
showed no shift of peaks and no interaction between drug and excipients.
Gita Chaurasia et al (2013), formulated and evaluated cyclodextrins based
solid inclusion compounds by using β-cyclodextrins, Hydroxo propyl β
cyclodextrins. The molar ratio containing 1:2 showed to have greater drug
content and aqueous solubility.
Sri Venkateshwara College of Pharmacy, Madhapur 1316/12/2014
14. Amit Taps et al (2012), formulated Carvedilol solid dispersions by
using polymers PVP k30 for improving physico chemical properties
of Carvedilol.
Y. Srinivasa rao et al (2012), formulated and evaluated Carvedilol
solid dispersions by using various polymers such as mannitol,
lactose, urea, PEG 4000 for enhancing dissolution rate. PEG 4000
formulation showed higher dissolution rate.
G.Sowjanya and T.E.G.K Murthy et al (2011), formulated and
evaluated inclusion complexes of Carvedilol by using β-
cyclodextrins by employing kneading method. The inclusion
complex prepared in 1:2 molar ratio showed 100% release in 4
minutes.
Sri Venkateshwara College of Pharmacy, Madhapur 1416/12/2014
15. Gehen balatla et al (2009), formuted and evaluated solid dispersions and
inclusion complexes of Ketocanozole by using pvp k-17 and β-
cyclodextrins respectively and showed improvement in solubility and
dissolution rate of Carvedilol.
Amit.R.Tapas et al (2008), formulated and evaluated carvedilol solid
dispersions which are in the form of spherical crystals by emulsion solvent
diffusion method by using polymers-pluronics F68 and F127 which showed
better dissolution rates there by bioavailability.
S.N.Hiremath et al (2007), formulated and evaluated inclusion complexes
of carvedilol by using β-cyclodextrins. In vitro dissolution rate was found to
increase with this formulation.
Sri Venkateshwara College of Pharmacy, Madhapur 1516/12/2014
16. Hyma ponnaganti et al (2013), formulated and evaluated Nabumetone
solid dispersion by using polymers like PEG 6000, PEG 4000 as carriers by
using solid evaporation method. Different ratios like 1:2,1:4 were prepared
and characterized by FTIR and XRD.
Irin deewan et al (2012), formulated and evaluated solid dispersions of
Carvedilol by using various polymers like PEG 6000, poloxamer 407,
HPMC 6 cps and sodium starch glycolate. Solid dispersions prepared by
poloxamer 407 showed higher dissolution rates.
Annamma devi et al (2012), studied the effect of hydrophilic polymers like
HPMC 6cps,PVA on Carvedilol solid dispersions. The solid dispersions
prepared by HPMC showed maximum dissolution rate.
Sri Venkateshwara College of Pharmacy, Madhapur 1616/12/2014
17. Ramesh Jagadeesan et al (2013), listed few novel approaches in the
preparation of solid dispersions for improving solubility. The drying
methods like hot extrusion method, spray drying, surface solid dispersion
technology, solvent evaporation method, lyophilization, electrostatic
spinning method and supercritical fluid technology.
Kovacic et al (2010), formulated and evaluated solid dispersions of
Carvedilol by using porous silica (sylsia 350) as carrier for improving
dissolution rate and physical stability of carvedilol.
Anu Sharma and C.P Jain et al (2013), prepared and characterized
carvedilol –β-cyclodextrin inclusion systems and showed in vitro evaluation
of this system which improved solubility and dissolution rate of Carvedilol.
Sri Venkateshwara College of Pharmacy, Madhapur 1716/12/2014
18. •The drug (Carvedilol) was selected based on its
category (anti hypertensive) and based on its physical
properties
•Carvedilol has less aqueous solubility so it has poor
bioavailability
•It belongs to class 2 (less solubility and
bioavailability) according to BCS classification
•Various methods are there for improving solubility an
bioavailability of carvedilol
Drug selection
19. Drug profile
1) Name: Carvedilol
2) Molecular weight : 406.50
3) Melting point : 114º C
4) Physico-chemical properties: A white crystalline powder, slightly soluble
in water
Absorption: Carvedilol bioavailability is 25 to 30% due to significant
degree of first-pass metabolism.
Elimination half life of carvedilol ranges from 4-6 hours.
Distribution: Carvedilol is widely distributed. It crosses the blood brain
barrier very efficiently due to high lipid solubility.
Metabolism: Carvedilol is extensively metabolized .
Excretion: The metabolites are excreted from bile to faeces.
Sri Venkateshwara College of Pharmacy, Madhapur 1916/12/2014
20. Materials used
Carvedilol-Drug
Methanol-Solvent
Carriers-Polaxomer 407,B-cyclodextrins,D-mannitol,PEG
4000.
Glassware and Buffers.
Sri Venkateshwara College of Pharmacy, Madhapur 2016/12/2014
21. Method of preparation of Solid dispersions
Sri Venkateshwara College of Pharmacy,
Madhapur 21
Methanol
Solvent evaporation
Drying
Sieving in 60# mesh
Dessication
Filling of powder
In Capsules
Carvedilol Carrier
16/12/2014
22. Formulation of solid dispersions
Sri Venkateshwara College of Pharmacy, Madhapur 22
Here in the preparation of solid dispersions Polaxomer 407 is used as a carrier
S.NO INGREDIE
NTS
SDP 2 SDP 3 SDP 5 SDP 8
1 Carvedilol
(mg)
300 300 300 300
2 Methanol
(ml)
1.5 1.5 1.5 1.5
3 Polaxomer
407 (mg)
600 900 1500 2400
16/12/2014
23. Formulations
S.NO INGREDIE
NTS
SDM 2 SDM 3 SDM 5 SDM 8
1 Carvedilol
(mg)
300 300 300 300
2 Methanol
(ml)
1.5 1.5 1.5 1.5
3 Mannitol
(mg)
600 900 1500 2400
Sri Venkateshwara College of Pharmacy, Madhapur 23
Here in the preparation of solid dispersions Mannitol is used as a carrier
16/12/2014
24. Formulations
S.NO INGREDIE
NTS
SDPE 2 SDPE 3 SDPE 5 SDPE 8
1 Carvedilol
(mg)
300 300 300 300
2 Methanol
(ml)
1.5 1.5 1.5 1.5
3 PEG 4000
(mg)
600 900 1500 2400
Sri Venkateshwara College of Pharmacy, Madhapur 24
Here in the preparation of solid dispersions PEG 4000 is used as a carrier
16/12/2014
25. Formulations
S.NO INGREDIE
NTS
SDB 2 SDB 3 SDB 5 SDB 8
1 Carvedilol
(mg)
300 300 300 300
2 Methanol
(ml)
1.5 1.5 1.5 1.5
3 β-
cyclodextri
n (mg)
600 900 1500 2400
Sri Venkateshwara College of Pharmacy, Madhapur 25
Here in the preparation of solid dispersions β-cyclodextrin is used as a carrier
16/12/2014
26. Formulations
SDM 2, SDM 3, SDM 5, SDM 8 – solid dispersions using
various ratios of Mannitol.
Similarly, SDP,SDB and SDPE code for solid dispersions
with Polaxomer 407, B-cyclodextrins and PEG 4000 as
carriers respectively.
Sri Venkateshwara College of Pharmacy, Madhapur 2616/12/2014
27. EVALUATION
Powder flow properties
Solubility studies
Drug content
In vitro dissolution
Surface characteristics
Drug interaction studies
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29. Scan spectrum of Carvedilol
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λmax – 240nm
16/12/2014
30. Standard graph of Carvedilol in 0.1N HCl
Concentration Absorbance
0 0
2 0.218
4 0.475
6 0.678
8 0.928
Sri Venkateshwara College of Pharmacy, Madhapur 30
y = 0.1158x - 0.0034
R² = 0.999
-0.2
0
0.2
0.4
0.6
0.8
1
0 2 4 6 8 10
Absorbance
Concentation (mcgml)
16/12/2014
31. Standard graph in pH 6.8 Buffer
Concentratio
n
Absorbance
0 0
2 0.228
4 0.422
6 0.580
8 0.736
10 0.893
Sri Venkateshwara College of Pharmacy, Madhapur 31
y = 0.1756x - 0.1382
R² = 0.9935
0
0.1
0.2
0.3
0.4
0.5
0.6
0.7
0.8
0.9
1
0 1 2 3 4 5 6 7
Absorbance
Concentration (mcg/ml)
Standard graph
16/12/2014
32. FTIR spectrum of Pure Carvedilol
Sri Venkateshwara College of Pharmacy, Madhapur 3216/12/2014
33. Characteristic IR peaks of Carvedilol plain drug
Functional group Observed Frequency
N-H Stretching 3343.34
C-H stretching 2842.60
C=O stretching 1097.31
C-H Stretching 2923.68
Sri Venkateshwara College of Pharmacy, Madhapur 3316/12/2014
34. Drug content studies
Solid dispersions were subjected to Drug content studies
by using solvent (methanol) and are analyzed by using Uv
visible spectrophotometer at 240nm. Drug content is
calculated by using the formula
% Drug content = Mact/Mt x 100
Sri Venkateshwara College of Pharmacy, Madhapur 3416/12/2014
35. Drug content studies
S.NO FORMULATION % DRUG CONTENT
1 SDP 2 84.27
2 SDP 3 87.42
3 SDP 5 95.25
4 SDP 8 85.12
5 SDM 2 86.18
6 SDM 3 88.36
7 SDM 5 91.17
8 SDM 8 87.26
Sri Venkateshwara College of Pharmacy, Madhapur 3516/12/2014
36. Drug Content studies
S.NO FORMULATION % DRUG CONTENT
9 SDB 2 88.22
10 SDB 3 91.20
11 SDB 5 93.45
12 SDB 8 89.32
13 SDPE 2 81.23
14 SDPE 3 83.32
15 SDPE 5 90.21
16 SDPE 8 87.29
Sri Venkateshwara College of Pharmacy, Madhapur 3616/12/2014
37. Solubility Studies
Solid dispersions were tested for their solubility in water
In this method initially solid dispersions were added to
distilled water
Later this solution is filtered and with buffer analyzed for
Carvedilol at 240nm
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39. FTIR Spectrum of Optimized
formulation SDP 5
Sri Venkateshwara College of Pharmacy, Madhapur 3916/12/2014
40. Percentage yield
Percentage yield of the prepared solid dispersion powder
was calculated by using the following formula
% Yield = Actual weight/Theoretical weight x 100
Yield of the solid dispersion powder was found to be more
than 90 %.
Sri Venkateshwara College of Pharmacy, Madhapur 4016/12/2014
41. Powdered drug characteristics
Bulk Density and Taped density
Bulk Density = mass of powder/Bulk volume
Tapped density = mass of powder/Tapped Volume
Sri Venkateshwara College of Pharmacy, Madhapur 4116/12/2014
42. Hausner’s Ratio
Hausner’s Ratio = Tapped density/Bulk density
Compressibility index (CI)
CI = Tapped density—Bulk density
------------------------------------- --- x 100
Tapped Density
Sri Venkateshwara College of Pharmacy, Madhapur 4216/12/2014
43. FLOW PROPERTIES OF POWDER
Code Bulk
density
Tapped0.5
4 density
Carr’s
index
Hausner’s
ratio
Angle of
repose
SDP 2 0.45 0.57 21.05 1.26 30.91
SDP3 0.47 0.54 13.00 1.14 31.23
SDP 5 0.46 0.53 13.70 1.15 29.34
SDP 8 0.46 0.55 16.30 1.19 26.71
SDPE 2 0.50 0.58 13.72 1.16 25.34
SDPE 3 0.43 0.55 21.18 1.27 29.23
SDPE 5 0.49 0.58 15.51 1.18 31.34
SDPE 8 0.41 0.50 18.00 1.21 30.78
Sri Venkateshwara College of Pharmacy, Madhapur 4316/12/2014
44. FLOW PROPERTIES OF POWDER
Code Bulk
Density
Tapped
density
Carr’s
index
Hausner’s
ratio
Angle of
repose
SDB 2 0.46 0.56 17.80 1.21 32.05
SDB 3 046 0.55 16.30 1.19 26.71
SDB 5 0.46 0.53 13.70 1.15 29.34
SDB 8 0.47 0.54 13.00 1.14 31.23
SDM 2 0.41 0.50 18.00 1.21 30.78
SDM 3 0.49 0.58 15.51 1.18 31.34
SDM 5 0.50 0.58 13.72 1.16 25.34
SDM 8 0.46 0.55 16.30 1.19 26.71
Sri Venkateshwara College of Pharmacy, Madhapur 4416/12/2014
45. In Vitro Dissolution Studies
In vitro dissolution studies were performed in USP basket
type I apparatus
Using 0.1 N Hcl as medium
Temperature – 37˚ C
Time intervals -5,10,15,30,45,60 minutes
Finally analysed by UV visible spectrophotometer at 240
nm.
Sri Venkateshwara College of Pharmacy, Madhapur 4516/12/2014
47. S.NO Time SDB 2 SDB 3 SDB 5 SDB 8 SDM2 SDM
3
SDM
5
SDM
8
1 5 4.93 5.43 11.23 8.48 4.39 5.97 11.37 9.07
2 10 5.55 6.70 24.37 11.5 5.46 7.62 21.21 13.73
3 15 14.88 15.76 41.72 15.64 11.27 11.24 32.18 16.72
4 30 21.58 39.62 61.89 26.05 19.98 25.78 58.27 26.78
5 45 41.59 43.85 79.9 39.97 28.89 39.48 76.89 32.98
6 60 47.42 52.98 96.27 54.26 42.56 49.27 93.18 51.78
Sri Venkateshwara College of Pharmacy, Madhapur 47
Of this formulations the drug release for SDP 5 was found to be
more so, it is considered as optimized formulation
% Drug release of various formulations
16/12/2014
48. Comparison of drug release from various SD
Formulations
Time % DR of
SDP5
%DR of SDB
5
% DR of SDM
5
% DR of SDM
5
0 0 0 0 0
5 10.2 11.23 11.37 10.37
10 25.22 24.37 21.21 23.78
15 42.78 41.72 32.18 33.28
30 65.67 61.89 58.27 59.28
45 82.37 79.9 76.89 75.48
60 98.27 96.27 93.18 90.89
Sri Venkateshwara College of Pharmacy, Madhapur 4816/12/2014
49. Drug release of SDP 5
Time % Drug
release
0
0
5
10.2
10
25.22
15
42.78
30
65.67
45
82.37
60
98.27
Sri Venkateshwara College of Pharmacy, Madhapur 49
0
20
40
60
80
100
120
0 20 40 60 80
cumulative%release
Time (min)
SDP 5
16/12/2014
50. Comparison of Inclusion complex and Pure
drug
Time
(min)
Cumulat
ive %
drug
release
Cumulat
ive %
drug
release
- SDB 5 Pure
drug
0 0 0
5 11.23 6.14
10 24.37 8.92
15 41.72 16.84
30 61.89 28.12
45 79.9 42.45
60 96.27 45.31
Sri Venkateshwara College of Pharmacy, Madhapur 50
0
20
40
60
80
100
120
0 5 10 15 30 45 60
Cumulative%release
Time (min)
SDB 5
Crude drug
16/12/2014
51. Drug release of Pure drug and Optimized
Formulation (SDP 5)
Time
(min)
Cumulat
ive %
drug
release
Cumulat
ive %
drug
release
- Crude
drug
SDP 5
0 0 0
5 6.148 10.2
10 8.92 25.22
15 16.848 42.78
30 28.12 65.67
45 42.45 82.37
60 45.31 98.27
Sri Venkateshwara College of Pharmacy, Madhapur
51
0
20
40
60
80
100
120
0 5 10 15 30 45 60
cumulative%release
Time (min)
SDP 5
Pure Drug
16/12/2014
52. Solid dispersion drug release
0
20
40
60
80
100
120
0 10 20 30 40 50 60 70
Cuulative%reelease
Time (min)
SDP 5
SDB 5
SDM 5
SDPE 5
Sri Venkateshwara College of Pharmacy, Madhapur 5216/12/2014
53. In dissolution studies formulation SDP 5 was found to
have better drug release when compared to other
formulations.
So, it was studied further for FTIR and Surface
Characteristics for optimization.
Sri Venkateshwara College of Pharmacy, Madhapur 5316/12/2014
54. Surface characteristics
Surface characteristics of the powdered solid dispersion
can be studied by using Scanning Electron Microscopy
(SEM).
The optimized solid dispersion (SDP 5) was subjected to
SEM study and powder was found to be Spherical in
shape.
Sri Venkateshwara College of Pharmacy, Madhapur 5416/12/2014
55. SEM of SDP 5
Sri Venkateshwara College of Pharmacy, Madhapur 5516/12/2014
56. STABILTY STUDIES
Solid dispersions are subjected to stability studies for
about 3 months and tested for drug release it gave a very
or little change in drug release so, solid dispersions are
stable at normal and intermediate conditions.
Sri Venkateshwara College of Pharmacy, Madhapur 5616/12/2014
57. Drug release of SDP 5
TIME % DR
of SDP
5
% DR
of SDP
5 (90
days)
5 10.2 9.8
10 25.22 23.52
15 42.78 40.27
30 65.67 63.45
45 82.37 80.21
60 98.27 98.16
Sri Venkateshwara College of Pharmacy, Madhapur 57
0
20
40
60
80
100
120
0 5 10 15 30 45 60
Cum%drugrelease
Time (min)
Stability studies
SDP 5 (1 month)
SDP 5 ( 3 months)
16/12/2014
58. Conclusions
Solid dispersions of carvedilol were successfully prepared
for improving the solubility and dissolution rate of this
poorly water soluble drug and evaluated.
The results were found to be satisfactory that certain
carriers like Polaxomers when used in the preparation of
solid dispersions improved solubility of poorly water
soluble drugs like Carvedilol,Valsartan
Sri Venkateshwara College of Pharmacy, Madhapur 5816/12/2014
59. Conclusions
The stability studies results showed that prepared solid
dispersions drug release and physical appearance.
The method solvent evaporation is very easy and efficient
for the preparation of solid dispersions.
Sri Venkateshwara College of Pharmacy, Madhapur 5916/12/2014
60. References
Irin Dewan et al “Formulation and Evaluation of Solid Dispersions of
Carvedilol, a Poorly Water Soluble Drug by Using Different Polymers”,
IJRPC 2012, 2(3), 585-593.
J. Vijaya Ratna,” Effect of Hydrophilic Polymers on Solid Dispersions of
Carvedilol For Enhancing Its Dissolution Rate” ,Journal of Global Trends in
Pharmaceutical Sciences Vol.3, Issue 2, pp -708-713, April–June 2012.
Y. Srinivasa Rao et al,” Formulation and Evaluation of Carvedilol Solid
Dispersions for Dissolution Rate Enhancement, IJAPBC – Vol. 1(4), Oct-
Dec, 2012 489-494.
T.E.G.K. Murthy, Evaluation of Some Methods For Preparing Carvedilol-
Hydroxy Propyl- Β -Cyclodextrin Inclusion Complexes, Asian Journal of
Biochemical and Pharmaceutical Research Issue 2 (Vol. 1) 2011,676-683.
Sri Venkateshwara College of Pharmacy, Madhapur 6016/12/2014
61. Tapan Kumar Giri , Physicochemical Classification and Formulation
Development Of Solid Dispersion Of Poorly Water Soluble Drugs: An
Updated Review , International Journal of Pharmaceutical & Biological
Archives 2010; 1(4): 309-324 .
Sarita Jangra Bhyan,” Formulation and evaluation of mouth dissolving
tablets containing carvedilol solid dispersion”, Der Pharmacia Lettre, 2013,
5 (6):31-42.
Dipika Mandal et al,” Effect of Carriers on Solid Dispersions of Simvastatin
(Sim): Physico- Chemical Characterizations and Dissolution Studies, Der
Pharmacia Lettre, 2010, 2(4): 47-56
Anshu Sharma and C.P. Jain,” Carvedilol-β-cyclodextrin Systems:
Preparation,Characterization and in vitro Evaluation, J. Pharm. Sci. 12(1):
51-58, 2013 (June)
Sri Venkateshwara College of Pharmacy, Madhapur 6116/12/2014