This document describes the development and in vitro evaluation of sustained release tablets of telmisartan hydrochloride. Various polymers including Eudragit RL 100, guar gum, and ethyl cellulose were used to formulate the sustained release matrix tablets. Tablets were prepared by direct compression and evaluated for physicochemical properties and in vitro drug release over 12 hours. The optimized formulation (F6) containing Eudragit RL 100 showed desired drug release of 96.10% over 12 hours and followed zero-order release kinetics. The document aims to develop a sustained release formulation of telmisartan that can maintain therapeutic drug levels for over 12 hours with once-daily dosing.
Solubility enhancement technique of BCS Class II drug by Solvent EvaporatiomKaustav Dey
I am very happy to share with you my B.Pharm Final semester Presentation. The topic of the presentation was “SOLUBILITY ENHANCEMENT TECHNIQUE OF BCS CLASS II DRUG BY SOLVENT EVAPORATION TECHNIQUE – FORMULATION & EVALUATION" which i have done under the esteemed guidance of Dr. Goutam Kumar Jena. It was a great experience to deliver this topic infront of the expert jury. I would also like thank all my teammates especially Agniv Masanta for his efforts. I hope everyone of you will like presentation and the research and efforts behind it.Thank you for giving your precious time. #research #science #thankyou #experience #share
Solubility enhancement technique of BCS Class II drug by Solvent EvaporatiomKaustav Dey
I am very happy to share with you my B.Pharm Final semester Presentation. The topic of the presentation was “SOLUBILITY ENHANCEMENT TECHNIQUE OF BCS CLASS II DRUG BY SOLVENT EVAPORATION TECHNIQUE – FORMULATION & EVALUATION" which i have done under the esteemed guidance of Dr. Goutam Kumar Jena. It was a great experience to deliver this topic infront of the expert jury. I would also like thank all my teammates especially Agniv Masanta for his efforts. I hope everyone of you will like presentation and the research and efforts behind it.Thank you for giving your precious time. #research #science #thankyou #experience #share
Factors affecting sustained release drug delivery system.Kavya S
contented and precise , Drug delivery system , sustained release preparation.factors like absorption, distribution ,metabolism , therapeutic window , absorption window.
Introduction to Concepts of Similarity and Difference factors,
Importance of dissolution profile comparison,
Objective of dissolution profile comparison,
Method to compare dissolution profile , f1 & f2 Comparison
Presented By
N. Poojitha
Department of Pharmaceutics
Phytosomes are one of the novel drug delivery system containing hydrophilic bioactive phyto-constituents of herbs surrounded and bounded by phospolipids.
Thin film drug delivery (Oral dissolve film )Chouthri D
to know about oral dissolving films, ,thin film dds ,oral dissolve films ,oral dispersal film ,api ,advantage for oral thin film ,ingredient using in thin film ,colouring agent used in thin film ,semisolid casting method ,thin film manufacturing mathods ,solvent casting method ,hot melt extrusion ,roiling method ,plasticizer ,water soluble polymers ,comparing between odt and odf ,solid dispersion extrusion ,application of oral dissolving film ,composition of fds,surfactant,saliva stimulating agent,flavouring agent,thi film manufacturing video
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.
Factors affecting sustained release drug delivery system.Kavya S
contented and precise , Drug delivery system , sustained release preparation.factors like absorption, distribution ,metabolism , therapeutic window , absorption window.
Introduction to Concepts of Similarity and Difference factors,
Importance of dissolution profile comparison,
Objective of dissolution profile comparison,
Method to compare dissolution profile , f1 & f2 Comparison
Presented By
N. Poojitha
Department of Pharmaceutics
Phytosomes are one of the novel drug delivery system containing hydrophilic bioactive phyto-constituents of herbs surrounded and bounded by phospolipids.
Thin film drug delivery (Oral dissolve film )Chouthri D
to know about oral dissolving films, ,thin film dds ,oral dissolve films ,oral dispersal film ,api ,advantage for oral thin film ,ingredient using in thin film ,colouring agent used in thin film ,semisolid casting method ,thin film manufacturing mathods ,solvent casting method ,hot melt extrusion ,roiling method ,plasticizer ,water soluble polymers ,comparing between odt and odf ,solid dispersion extrusion ,application of oral dissolving film ,composition of fds,surfactant,saliva stimulating agent,flavouring agent,thi film manufacturing video
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.
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.
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).
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).
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).
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.
Similar to Development and in vitro evaluation of sustained release formulation of telmisartan hydrochloride (20)
Stability indicating method and validation for the simultaneous estimation of...SriramNagarajan18
Stability indicating method and validation for the simultaneous estimation of metformin and empagliflozin by using RP-HPLC in a bulk and pharmaceutical dosage forms
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Flu Vaccine Alert in Bangalore Karnatakaaddon Scans
As flu season approaches, health officials in Bangalore, Karnataka, are urging residents to get their flu vaccinations. The seasonal flu, while common, can lead to severe health complications, particularly for vulnerable populations such as young children, the elderly, and those with underlying health conditions.
Dr. Vidisha Kumari, a leading epidemiologist in Bangalore, emphasizes the importance of getting vaccinated. "The flu vaccine is our best defense against the influenza virus. It not only protects individuals but also helps prevent the spread of the virus in our communities," he says.
This year, the flu season is expected to coincide with a potential increase in other respiratory illnesses. The Karnataka Health Department has launched an awareness campaign highlighting the significance of flu vaccinations. They have set up multiple vaccination centers across Bangalore, making it convenient for residents to receive their shots.
To encourage widespread vaccination, the government is also collaborating with local schools, workplaces, and community centers to facilitate vaccination drives. Special attention is being given to ensuring that the vaccine is accessible to all, including marginalized communities who may have limited access to healthcare.
Residents are reminded that the flu vaccine is safe and effective. Common side effects are mild and may include soreness at the injection site, mild fever, or muscle aches. These side effects are generally short-lived and far less severe than the flu itself.
Healthcare providers are also stressing the importance of continuing COVID-19 precautions. Wearing masks, practicing good hand hygiene, and maintaining social distancing are still crucial, especially in crowded places.
Protect yourself and your loved ones by getting vaccinated. Together, we can help keep Bangalore healthy and safe this flu season. For more information on vaccination centers and schedules, residents can visit the Karnataka Health Department’s official website or follow their social media pages.
Stay informed, stay safe, and get your flu shot today!
TEST BANK for Operations Management, 14th Edition by William J. Stevenson, Ve...kevinkariuki227
TEST BANK for Operations Management, 14th Edition by William J. Stevenson, Verified Chapters 1 - 19, Complete Newest Version.pdf
TEST BANK for Operations Management, 14th Edition by William J. Stevenson, Verified Chapters 1 - 19, Complete Newest Version.pdf
Ethanol (CH3CH2OH), or beverage alcohol, is a two-carbon alcohol
that is rapidly distributed in the body and brain. Ethanol alters many
neurochemical systems and has rewarding and addictive properties. It
is the oldest recreational drug and likely contributes to more morbidity,
mortality, and public health costs than all illicit drugs combined. The
5th edition of the Diagnostic and Statistical Manual of Mental Disorders
(DSM-5) integrates alcohol abuse and alcohol dependence into a single
disorder called alcohol use disorder (AUD), with mild, moderate,
and severe subclassifications (American Psychiatric Association, 2013).
In the DSM-5, all types of substance abuse and dependence have been
combined into a single substance use disorder (SUD) on a continuum
from mild to severe. A diagnosis of AUD requires that at least two of
the 11 DSM-5 behaviors be present within a 12-month period (mild
AUD: 2–3 criteria; moderate AUD: 4–5 criteria; severe AUD: 6–11 criteria).
The four main behavioral effects of AUD are impaired control over
drinking, negative social consequences, risky use, and altered physiological
effects (tolerance, withdrawal). This chapter presents an overview
of the prevalence and harmful consequences of AUD in the U.S.,
the systemic nature of the disease, neurocircuitry and stages of AUD,
comorbidities, fetal alcohol spectrum disorders, genetic risk factors, and
pharmacotherapies for AUD.
Ozempic: Preoperative Management of Patients on GLP-1 Receptor Agonists Saeid Safari
Preoperative Management of Patients on GLP-1 Receptor Agonists like Ozempic and Semiglutide
ASA GUIDELINE
NYSORA Guideline
2 Case Reports of Gastric Ultrasound
ARTIFICIAL INTELLIGENCE IN HEALTHCARE.pdfAnujkumaranit
Artificial intelligence (AI) refers to the simulation of human intelligence processes by machines, especially computer systems. It encompasses tasks such as learning, reasoning, problem-solving, perception, and language understanding. AI technologies are revolutionizing various fields, from healthcare to finance, by enabling machines to perform tasks that typically require human intelligence.
Lung Cancer: Artificial Intelligence, Synergetics, Complex System Analysis, S...Oleg Kshivets
RESULTS: Overall life span (LS) was 2252.1±1742.5 days and cumulative 5-year survival (5YS) reached 73.2%, 10 years – 64.8%, 20 years – 42.5%. 513 LCP lived more than 5 years (LS=3124.6±1525.6 days), 148 LCP – more than 10 years (LS=5054.4±1504.1 days).199 LCP died because of LC (LS=562.7±374.5 days). 5YS of LCP after bi/lobectomies was significantly superior in comparison with LCP after pneumonectomies (78.1% vs.63.7%, P=0.00001 by log-rank test). AT significantly improved 5YS (66.3% vs. 34.8%) (P=0.00000 by log-rank test) only for LCP with N1-2. Cox modeling displayed that 5YS of LCP significantly depended on: phase transition (PT) early-invasive LC in terms of synergetics, PT N0—N12, cell ratio factors (ratio between cancer cells- CC and blood cells subpopulations), G1-3, histology, glucose, AT, blood cell circuit, prothrombin index, heparin tolerance, recalcification time (P=0.000-0.038). Neural networks, genetic algorithm selection and bootstrap simulation revealed relationships between 5YS and PT early-invasive LC (rank=1), PT N0—N12 (rank=2), thrombocytes/CC (3), erythrocytes/CC (4), eosinophils/CC (5), healthy cells/CC (6), lymphocytes/CC (7), segmented neutrophils/CC (8), stick neutrophils/CC (9), monocytes/CC (10); leucocytes/CC (11). Correct prediction of 5YS was 100% by neural networks computing (area under ROC curve=1.0; error=0.0).
CONCLUSIONS: 5YS of LCP after radical procedures significantly depended on: 1) PT early-invasive cancer; 2) PT N0--N12; 3) cell ratio factors; 4) blood cell circuit; 5) biochemical factors; 6) hemostasis system; 7) AT; 8) LC characteristics; 9) LC cell dynamics; 10) surgery type: lobectomy/pneumonectomy; 11) anthropometric data. Optimal diagnosis and treatment strategies for LC are: 1) screening and early detection of LC; 2) availability of experienced thoracic surgeons because of complexity of radical procedures; 3) aggressive en block surgery and adequate lymph node dissection for completeness; 4) precise prediction; 5) adjuvant chemoimmunoradiotherapy for LCP with unfavorable prognosis.
Couples presenting to the infertility clinic- Do they really have infertility...Sujoy Dasgupta
Dr Sujoy Dasgupta presented the study on "Couples presenting to the infertility clinic- Do they really have infertility? – The unexplored stories of non-consummation" in the 13th Congress of the Asia Pacific Initiative on Reproduction (ASPIRE 2024) at Manila on 24 May, 2024.
MANAGEMENT OF ATRIOVENTRICULAR CONDUCTION BLOCK.pdfJim Jacob Roy
Cardiac conduction defects can occur due to various causes.
Atrioventricular conduction blocks ( AV blocks ) are classified into 3 types.
This document describes the acute management of AV block.
New Directions in Targeted Therapeutic Approaches for Older Adults With Mantl...i3 Health
i3 Health is pleased to make the speaker slides from this activity available for use as a non-accredited self-study or teaching resource.
This slide deck presented by Dr. Kami Maddocks, Professor-Clinical in the Division of Hematology and
Associate Division Director for Ambulatory Operations
The Ohio State University Comprehensive Cancer Center, will provide insight into new directions in targeted therapeutic approaches for older adults with mantle cell lymphoma.
STATEMENT OF NEED
Mantle cell lymphoma (MCL) is a rare, aggressive B-cell non-Hodgkin lymphoma (NHL) accounting for 5% to 7% of all lymphomas. Its prognosis ranges from indolent disease that does not require treatment for years to very aggressive disease, which is associated with poor survival (Silkenstedt et al, 2021). Typically, MCL is diagnosed at advanced stage and in older patients who cannot tolerate intensive therapy (NCCN, 2022). Although recent advances have slightly increased remission rates, recurrence and relapse remain very common, leading to a median overall survival between 3 and 6 years (LLS, 2021). Though there are several effective options, progress is still needed towards establishing an accepted frontline approach for MCL (Castellino et al, 2022). Treatment selection and management of MCL are complicated by the heterogeneity of prognosis, advanced age and comorbidities of patients, and lack of an established standard approach for treatment, making it vital that clinicians be familiar with the latest research and advances in this area. In this activity chaired by Michael Wang, MD, Professor in the Department of Lymphoma & Myeloma at MD Anderson Cancer Center, expert faculty will discuss prognostic factors informing treatment, the promising results of recent trials in new therapeutic approaches, and the implications of treatment resistance in therapeutic selection for MCL.
Target Audience
Hematology/oncology fellows, attending faculty, and other health care professionals involved in the treatment of patients with mantle cell lymphoma (MCL).
Learning Objectives
1.) Identify clinical and biological prognostic factors that can guide treatment decision making for older adults with MCL
2.) Evaluate emerging data on targeted therapeutic approaches for treatment-naive and relapsed/refractory MCL and their applicability to older adults
3.) Assess mechanisms of resistance to targeted therapies for MCL and their implications for treatment selection
The prostate is an exocrine gland of the male mammalian reproductive system
It is a walnut-sized gland that forms part of the male reproductive system and is located in front of the rectum and just below the urinary bladder
Function is to store and secrete a clear, slightly alkaline fluid that constitutes 10-30% of the volume of the seminal fluid that along with the spermatozoa, constitutes semen
A healthy human prostate measures (4cm-vertical, by 3cm-horizontal, 2cm ant-post ).
It surrounds the urethra just below the urinary bladder. It has anterior, median, posterior and two lateral lobes
It’s work is regulated by androgens which are responsible for male sex characteristics
Generalised disease of the prostate due to hormonal derangement which leads to non malignant enlargement of the gland (increase in the number of epithelial cells and stromal tissue)to cause compression of the urethra leading to symptoms (LUTS
Tom Selleck Health: A Comprehensive Look at the Iconic Actor’s Wellness Journeygreendigital
Tom Selleck, an enduring figure in Hollywood. has captivated audiences for decades with his rugged charm, iconic moustache. and memorable roles in television and film. From his breakout role as Thomas Magnum in Magnum P.I. to his current portrayal of Frank Reagan in Blue Bloods. Selleck's career has spanned over 50 years. But beyond his professional achievements. fans have often been curious about Tom Selleck Health. especially as he has aged in the public eye.
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Introduction
Many have been interested in Tom Selleck health. not only because of his enduring presence on screen but also because of the challenges. and lifestyle choices he has faced and made over the years. This article delves into the various aspects of Tom Selleck health. exploring his fitness regimen, diet, mental health. and the challenges he has encountered as he ages. We'll look at how he maintains his well-being. the health issues he has faced, and his approach to ageing .
Early Life and Career
Childhood and Athletic Beginnings
Tom Selleck was born on January 29, 1945, in Detroit, Michigan, and grew up in Sherman Oaks, California. From an early age, he was involved in sports, particularly basketball. which played a significant role in his physical development. His athletic pursuits continued into college. where he attended the University of Southern California (USC) on a basketball scholarship. This early involvement in sports laid a strong foundation for his physical health and disciplined lifestyle.
Transition to Acting
Selleck's transition from an athlete to an actor came with its physical demands. His first significant role in "Magnum P.I." required him to perform various stunts and maintain a fit appearance. This role, which he played from 1980 to 1988. necessitated a rigorous fitness routine to meet the show's demands. setting the stage for his long-term commitment to health and wellness.
Fitness Regimen
Workout Routine
Tom Selleck health and fitness regimen has evolved. adapting to his changing roles and age. During his "Magnum, P.I." days. Selleck's workouts were intense and focused on building and maintaining muscle mass. His routine included weightlifting, cardiovascular exercises. and specific training for the stunts he performed on the show.
Selleck adjusted his fitness routine as he aged to suit his body's needs. Today, his workouts focus on maintaining flexibility, strength, and cardiovascular health. He incorporates low-impact exercises such as swimming, walking, and light weightlifting. This balanced approach helps him stay fit without putting undue strain on his joints and muscles.
Importance of Flexibility and Mobility
In recent years, Selleck has emphasized the importance of flexibility and mobility in his fitness regimen. Understanding the natural decline in muscle mass and joint flexibility with age. he includes stretching and yoga in his routine. These practices help prevent injuries, improve posture, and maintain mobilit
Tom Selleck Health: A Comprehensive Look at the Iconic Actor’s Wellness Journey
Development and in vitro evaluation of sustained release formulation of telmisartan hydrochloride
1. Pamu. S et al / Int. J. of Farmacia, Vol-1, Issue 1, (July. – Sep. 2015), Pg. 20 -29
20
International Journal of Farmacia
Journal Home page: www.ijfjournal.com
Development and in vitro evaluation of sustained release formulation of
telmisartan hydrochloride
Pamu. Sandhya *1
, K S K. Rao Patnaik 1
, C V.S. Subrahmanyam 2
1*
Department of Pharmacy, University College of Technology, Osmania University, Telangana
State, Hyderabad
2
Gokaraju Rangaraju College of Pharmacy, Bachupally, Hyderabad, India
*Email: sandhyapasikanti@gmail.com
Abstract
The aim of the present study was to develop sustained release formulation of Telmisartan HCl to maintain constant
therapeutic levels of the drug for over 12 hrs. Eudragit RL 100, Guar gum and ethyl cellulose were employed as
polymers. Telmisartan HCl dose was fixed as 20 mg. Total weight of the tablet was considered as 300 mg. Polymers
were used in the concentration of 30, 60 and 90 mg concentration. All the formulations were passed various
physicochemical evaluation parameters and they were found to be within limits. Whereas from the dissolution
studies it was evident that the formulation (F6) showed better and desired drug release pattern i.e., 96.10 % in 12
hours. Optimized formulation drug release was fitted into different drug release kinetics, it followed zero order
release kinetics mechanism.
Keywords: Telmisartan HCL, Eudragit RL 100, Guar gum, Ethyl cellulose, Sustained release tablets.
INTRODUCTION
Sustained release tablets are commonly taken only
once or twice daily, compared with counterpart
conventional forms that may have to take three or four
times daily to achieve the same therapeutic effect.
Sustained release, prolonged release, modified release,
extended release or depot formulations are terms used
to identify drug delivery systems that are designed to
achieve or extend therapeutic effect by continuously
releasing medication over an extended period of time
after administration of a single dose. The goal in
designing sustained or sustained delivery systems is to
reduce the frequency of the dosing or to increase
effectiveness of the drug by localization at the site of
action, reducing the dose required or providing
uniform drug delivery. So, sustained release dosage
form is a dosage form that release one or more drugs
continuously in predetermined pattern for a fixed
period of time, either systemically or to a specified
target organ. Introduction of matrix tablet as sustained
release (SR) has given a new breakthrough for novel
drug delivery system in the field of Pharmaceutical
technology. It excludes complex production
procedures such as coating and Pelletization during
manufacturing and drug release rate from the dosage
form is controlled mainly by the type and proportion
of polymer used in the preparations. Hydrophilic
polymer matrix is widely used for formulating an SR
dosage form. Because of increased complication and
expense involved in marketing of new drug entities,
has focused greater attention on development of
sustained release or controlled release drug delivery
systems. Matrix systems are widely used for the
purpose of sustained release. It is the release system
which prolongs and controls the release of the drug
that is dissolved or dispersed. Modified release
delivery systems may be divided conveniently in to
four categories.
Delayed release
These systems are those that use repetitive,
intermittent dosing of a drug from one or more
immediate release units incorporated into a single
dosage form. Examples of delayed release systems
include repeat action tablets and capsules and enteric-
2. Pamu. S et al / Int. J. of Farmacia, Vol-1, Issue 1, (July. – Sep. 2015), Pg. 20 -29
21
coated tablets where timed release is achieved by a
barrier coating.
Sustained release
During the last two decades there has been remarkable
increase in interest in sustained release drug delivery
system. This has been due to various factor viz. the
prohibitive cost of developing new drug entities,
expiration of existing international patents, discovery
of new polymeric materials suitable for prolonging the
drug release, and the improvement in therapeutic
efficiency and safety achieved by these delivery
systems. Now-a-days the technology of sustained
release is also being applied to veterinary products.
These systems also provide a slow release of drug over
an extended period of time and also can provide some
control, whether this be of a temporal or spatial nature,
or both, of drug release in the body, or in other words,
the system is successful at maintaining constant drug
levels in the target tissue or cells.
Controlled release
These systems include any drug delivery system that
achieves slow release of drug over an extended period
of time.
Extended release
Pharmaceutical dosage forms that release the drug
slower than normal manner at predetermined rate &
necessarily reduce the dosage frequency by two folds
Site specific targeting
These systems refer to targeting of a drug directly to a
certain biological location. In this case the target is
adjacent to or in the diseased organ or tissue.
Receptor targeting
These systems refer to targeting of a drug directly to a
certain biological location. In this case the target is the
particular receptor for a drug within an organ or tissue.
Site specific targeting and receptor targeting systems
satisfy the spatial aspect of drug delivery and are also
considered to be sustained drug delivery systems.
Design and formulation of oral sustained release
drug delivery system
The oral route of administration is the most preferred
route due to flexibility in dosage form, design and
patient compliance. But here one has to take into
consideration, the various pH that the dosage form
would encounter during its transit, the gastrointestinal
motility, the enzyme system and its influence on the
drug and the dosage form. The majority of oral
sustained release systems rely on dissolution, diffusion
or a combination of both mechanisms, to generate
slow release of drug to the gastrointestinal milieu.
Theoretically and desirably a sustained release
delivery device, should release the drug by a zero-
order process which would result in a blood level time
profile similar to that after intravenous constant rate
infusion. Sustained (zero-order) drug release has been
attempted to be achieved with various classes of
sustained drug delivery system
AIM AND OBJECTIVE
Aim of the study is to formulate and evaluate
Telmisartan HCl sustained release tablets using
different polymers such as Guar gum, Ethyl cellulose
and various grades of polymethacrylate polymers.
Microcrystalline cellulose as diluents
METHODOLOGY
Analytical method development
Determination of absorption maxima
100mg of Telmisartan HCl pure drug was dissolved in
100ml of Methanol (stock solution)10ml of above
solution was taken and make up with100ml by using
0.1 N HCl (100μg/ml).From this 10ml was taken and
make up with 100 ml of 0.1 N HCl (10μg/ml) and pH
6.8 Phosphate buffer UV spectrums was taken using
Double beam UV/VIS spectrophotometer. The solution
was scanned in the range of 200 – 400.
Preparation of calibration curve
100mg of Telmisartan HCl pure drug was dissolved in
100ml of Methanol (stock solution)10ml of above
solution was taken and make up with100ml by using
0.1 N HCl (100μg/ml).From this 10ml was taken and
make up with 100 ml of 0.1 N HCl (10μg/ml). The
above solution was subsequently diluted with 0.1N
HCl to obtain series of dilutions Containing 5,10,15,20
and 25 μg/ml of Telmisartan per ml of solution. The
absorbance of the above dilutions was measured at 232
nm by using UV-Spectrophotometer taking 0.1N HCl
as blank. Then a graph was plotted by taking
Concentration on X-Axis and Absorbance on Y-Axis
which gives a straight line Linearity of standard curve
was assessed from the square of correlation coefficient
(R2
)which determined by least-square linear regression
analysis.
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22
Table 1: Formulation chart Fourier transform infrared (FTIR) spectroscopy
The physical properties of the physical mixture were
compared with those of plain drug. Samples was mixed
thoroughly with 100mg potassium bromide IR powder
and compacted under vacuum at a pressure of about 12
psi for 3 minutes. The resultant disc was mounted in a
suitable holder in Perkin Elmer IR spectrophotometer
and the IR spectrum was recorded from 3500 cm to
500 cm. The resultant spectrum was compared for any
spectrum changes.
Preformulation parameters
The quality of tablet, once formulated by rule, is
generally dictated by the quality of physicochemical
properties of blends. There are many formulations and
process variables involved in mixing and all these can
affect the characteristics of blends produced. The
various characteristics of blends tested as per
Pharmacopoeia.
Formulation development of tablets
All the formulations were prepared by direct
compression. The compositions of different
formulations are given in Table 1.The tablets were
prepared as per the procedure given below and aim i
s to prolong the release of Telmisartan. Total weight of
the tablet was considered as 300mg.
Evaluation of post compression parameters for
prepared tablets
Weight variation test
Thickness
Hardness
Friability
Formulation composition for tablets
Determination of drug content
Tablets were tested for their drug content. Ten tablets
were finely powdered quantities of the powder
equivalent to one tablet weight of drug were accurately
weighed, transferred to a 100 ml volumetric flask
containing 50 ml water and were allowed to stand to
ensure complete solubility of the drug. The mixture
was made up to volume with media. The solution was
suitably diluted and the absorption was determined by
UV –Visible spectrophotometer. The drug
concentration was calculated from the calibration
curve.
In vitro drug release studies
Dissolution parameters
Apparatus -- USP-II,
Paddle type
Dissolution Medium -- 0.1 N HCl pH
1.2, p H 6.8 Phophate buffer
RPM -- 50
Sampling intervals (hrs)
0.5,1,2,3,4,5,6,7,8,10,11,12
Temperature -- 37°c + 0.5°
Procedure
900ml 0f 0.1 HCl was placed in vessel and the USP
apparatus –II (Paddle Method) was assembled. The
medium was allowed to equilibrate to temp of 37°c +
Form
No.
Telmisartan β
cyclodextrin
Eudragit RL
100
Guar
gum
Ethyl
cellulose
Mag.
Stearate
Talc MCC
pH
102
F1 20 15 30 - - 3 3 244
F2 20 15 60 - - 3 3 86
F3 20 15 90 - - 3 3 116
F4 20 15 - 30 - 3 3 56
F5 20 15 - 60 - 3 3 86
F6 20 15 - 90 - 3 3 116
F7 20 15 - - 30 3 3 56
F8 20 15 - - 60 3 3 86
F9 20 15 - - 90 3 3 96
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23
0.5°c. Tablet was placed in the vessel and apparatus
was operated for 2 hours and then the media 0.1 N
HCl was removed and pH 6.8 phosphate buffer was
added process was continued from upto 12 hrs at 50
rpm. At definite time intervals withdrawn 5 ml of
sample, filtered and again 5ml media was replaced.
Suitable dilutions were done with media and analyzed
by spectrophotometrically at 232 and 233nm using
UV-spectrophotometer.
Application of release rate kinetics to dissolution
data
Various models were tested for explaining the kinetics
of drug release. To analyze the mechanism of the drug
release rate kinetics of the dosage form, the obtained
data were fitted into zero-order, first order, Higuchi,
and Korsmeyer-Peppas release model.
Zero order release rate kinetics
To study the zero–order release kinetics the release rate
data ar e fitted to the following equation.
F = Ko t Where, ‘F’ is the drug release at time ‘t’, and
‘Ko’ is the zero order release rate constant. The plot of
% drug release versus time is linear.
First order release rate kinetics
The release rate data are fitted to the following
equation Log (100-F) = kt A plot of log cumulative
percent of drug remaining to be released vs. time is
plotted then it gives first order release.
Higuchi release model
To study the Higuchi release kinetics, the release rate
data were fitted to the following equation.
F = k t1/2 Where, ‘k’ is the Higuchi constant. In
higuchi model, a plot of % drug release versus square
root of time is linear.
Korsmeyer and Peppas release model
The mechanism of drug release was evaluated by
plotting the log percentage of drug released versus log
time according to Korsmeyer- Peppas equation. The
exponent ‘n’ indicates the mechanism of drug release
calculated through the slope of the straight Line.
Mt/ M∞ = K tn
Where, Mt/ M∞ is fraction of drug released at time ‘t’, k
represents a constant, and ‘n’ is the diffusional
exponent, which characterizes the type of release
mechanism during the dissolution process. For non-
Fickian release, the value of n falls between 0.5 and
1.0;while in case of Fickian diffusion, n = 0.5; for zero-
order release (case I I transport),n=1; and for super case
II transport, n > 1.In this model, a plot of log (Mt/ M∞)
versus log (time) is linear.
Hixson-crowell release model
(100-Qt)1/3
= 1001/3
– KHC.t Where, k is the Hixson-
Crowell rate constant. Hixson-Crowell model describes
the release of drugs from an insoluble matrix through
mainly erosion. (Where there is a change in surface
area and diameter of particles or tablets).
RESULTS AND DISCUSSION
The present study was aimed to developing Sustained
release tablets of Telmisartan using various polymers.
All the formulations were evaluated for
physicochemical properties and invitro drug release
studies.
Analytical method
Graphs of Telmisartan were taken in Simulated Gastric
fluid (pH 1.2) and in p H 6.8 phosphate buffer at 232
nm and 233 nm respectively.
Table 2: Observations for standard graph of telmisartan in 0.1N Hcl (232nm)
Conc [µg/ml] Absorbance
0 0
5 0.104
10 0.205
15 0.302
20 0.411
25 0.503
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24
Fig 1: Standard graph of Telmisartan in 0.1N HCl
Table 3: Observations for graph of Telmisartan in pH 6.8 phosphate buffer (233nm)
Conc [µg/l] Abs
0 0
5 0.098
10 0.195
15 0.298
20 0.392
25 0.490
Fig 2: Standard graph of Telmisartan pH 6.8 phosphate buffer (233nm
y = 0.0196x + 0.0001
R² = 0.9999
0
0.1
0.2
0.3
0.4
0.5
0.6
0 5 10 15 20 25 30
Absorbance
Conc. µg/ml
Standard graph of telmisartan in 0.1N HCl (232nm)
y = 0.0196x + 0.0001
R² = 0.9999
0
0.1
0.2
0.3
0.4
0.5
0.6
0 5 10 15 20 25 30
Absorbance
Conc. µg/ml
Standard graph of telmisartan in pH 6.8 phosphate buffer
(233nm)
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25
Drug – Excipient compatability studies Fourier transform-infrared spectroscopy
Fig 3: FT-TR Spectrum of Telmisartan pure drug
Fig 4: FT-IR Spectrum of Optimised Formulation
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26
Table 4: Preformulation parameters of powder blend
Formulation
Code
Angle of
Repose
Bulk density
(gm/ml)
Tapped density
(gm/ml)
Carr’s index
(%)
Hausner’s
Ratio
F1 25.11 0.49±0.04 0.54±0.04 16.21±0.06 1.10±0.06
F2 25.67 0.42±0.09 0.52±0.04 16.87±0.05 1.23±0.05
F3 25.54 0.50±0.05 0.58±0.05 17.11±0.01 1.16±0.03
F4 25.43 0.51±0.06 0.59±0.07 17.67±0.08 1.15±0.04
F5 25.34 0.47±0.03 0.57±0.03 16.92±0.04 1.2±0.08
F6 24.22 0.53±0.04 0.56±0.06 17.65±0.09 1.06±0.09
F7 25.18 0.49±0.06 0.59±0.04 16.43±0.05 1.2±0.03
F8 24.22 0.58±0.04 0.67±0.02 17.97±0.02 1.15±0.09
F9 25.05 0.45±0.08 0.52±0.03 17.54±0.09 1.15±0.02
Pre-formulation parameters of core blend
Tablet powder blend was subjected to various pre-
formulation parameters. The angle of repose values
indicates that the powder blend has good flow
properties. The bulk density of all the formulations
was found to be in the range of 0.42±0.07 to
0.58±0.06 (gm/cm3) showing that the powder has
good flow properties. The tapped density of all the
formulations was found to be in the range of
0.52±0.04 to 0.67±0.02 showing the powder has good
flow properties. The compressibility index of all the
formulations was found to be ranging between 16 to
18 which shows that the powder has good flow
properties. All the formulations has shown the hausner
ratio ranging between 0 to 1.2 indicating the powder
has good flow properties.
Quality control tests
Tablet quality control tests such as weight variation,
hardness, and friability, thickness, and drug release
studies in different media were performed on the
compression coated tablet.
Table 5: Quality control tests
Formulation Weight
variation(mg)
Hardness(kg/cm2) Friability
(%loss)
Thickness
(mm)
Drug content
(%)
F1 312.5 4.5 0.50 3.8 99.76
F2 305.4 4.5 0.51 3.9 99.45
F3 308.6 4.4 0.51 3.9 98.34
F4 300.6 4.5 0.55 3.9 98.87
F5 309.4 4.4 0.56 3.7 99.14
F6 310.7 4.5 0.45 3.7 98.56
F7 302.3 4.1 0.51 3.4 98.42
F8 301.2 4.3 0.49 3.7 99.65
F9 298.3 4.5 0.55 3.6 99.12
In-vitro quality control parameters for tablets
All the parameters such as weight variation, friability,
hardness, thickness and drug content were found to be
within limits.
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27
Table 6: In-vitro drug release studies
Time
(hr)
Cumulative percent drug dissolved
F1 F2 F3 F4 F5 F6 F7 F8 F9
0.5 25.5 20.1 16.4 17.25 16.42 14.62 10.4 9.4 8.5
1 46.7 33.4 23.7 38.26 25.73 19.86 16.5 15.6 14.5
2 76.5 45.3 31.6 54.16 36.63 22.35 28.6 21.4 18.4
3 98.4 56.3 40.4 72.01 45.04 31.45 39.5 36.7 23.4
4 77.3 53.4 88.26 58.25 39.80 48.5 42.4 28.2
5 89.4 59.4 97.10 65.33 45.25 59.4 49.6 34.8
6 95.34 65.4 76.41 58.24 69.2 55.3 40.2
7 71.5 84.84 66.73 74.5 60.3 44.8
8 87.3 97.80 71.34 82.3 72.8 50.4
9 97.45 75.52 87.78 83.52 63.34
10 82.17 98.78 88.65 69.27
11 87.10 96.56 74.86
12 96.10 79.97
Fig 5: In-vitro drug release studies
Application of release rate kinetics to dissolution
data
Various models were tested for explaining the kinetics
of drug release. To analyze the mechanism of the drug
release rate kinetics of the dosage form, the obtained
data were fitted into zero-order, first order, Higuchi,
and Korsmeyer-Peppas release model.
Table 7: Release rate kinetics
Cumulativepercentdrugdissolved
Time (hours)
Dissolution profile of Telmisartan formulations F1- F9
F1
F2
F3
F4
F5
F6
F7
F8
F9
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29
Fig 8: Peppas release kinetics graph for F6
Fig 9: First order release kinetics graph for F6
From the above graphs it was evident that the
formulation F6 was followed Zero order release
kinetics.
CONCLUSION
The aim of the present study was to develop sustained
release formulation of Telmisartan HCl. Eudragit RL
100, Guar gum and ethyl cellulose were employed as
polymers. Telmisartan HCl dose was fixed as 20 mg.
Total weight of the tablet was 300 mg. Polymers were
used in the concentration of 10, 20 and 30 %
concentration. All the formulations were passed
various physicochemical evaluation parameters and
they were found to be within limits. Whereas from the
dissolution studies it was evident that the formulation
(F6) showed better and desired drug release pattern
i.e., 96.10 % in 12 hours. The drug release pattern
followed zero order release kinetics mechanism.
REFERENCES
[1]. Altaf AS, Friend DR, MASRx and COSRx. Sustained-Release Technology in Rathbone MJ, Hadgraft J, Robert
MS, Modified Release Drug Delivery Technology, Marcell Dekker Inc., New York, 2003; 1: 102-117.
[2]. Reddy KR., Mutalik S, Reddy S. AAPS Pharm. Sci. Tech.2003; 4: 19. 121-125.
[3]. Mohammed AD et al. Release of propranolol hydrochloride from matrix tablets containing sodium
carboxymethylcellulose and Hydroxypropyl methyl cellulose. Pharm Dev Tech.1999; 4: 313-324.
[4]. Salsa T, Veiga F. Drug Develop. Ind Pharm. 1997; 23: 931.
[5]. Jantzen GM, Robinson JR, Sustained and controlled-release drug delivery systems, inBanker GS, Rhodes CT
(Eds.) Modern Pharmaceutics, 3rd
Ed, Revised andExpanded, Drugs and the Pharmaceutical Sciences., Marcell
Dekker, Inc. NewYork. 1995; 72: 575-609.
[6]. Jantzen GM, Robinson JR. Sustained and Controlled- Release Drug Delivery systems Modern Pharmaceutics,
4th
ed; 2003; 121: 501-502.
y = 60.23x + 15.834
R² = 0.8582
LogCumulative%drug
release
Log Time
Peppas drug release kinetics
y = -0.0912x + 2.084
R² = 0.8755
Log%drugremaining
time
First order drug release kinetics