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.
liquisolid technology is a topic related to pharmaceutics presented by konatham teja kumar reddy from chilkur balaji college of pharmcy ,hyderabad,telangana
Preparation and Characterization of Cyclodextrin Inclusion Complexes for Impr...Jing Zang
Nimesulide (4'-nitro-2'-phenoxy methane sulfonanilide) is a selective cyclooxygenase-2 inhibitor and one of the potent non steroidal anti-inflammatory drugs (NSAIDs). It is practically insoluble in water and hence has a low bioavailability. To improve solubility and dissolution of nimesulide, its β-cyclodextrin complex were prepared.
Nimesulide was complexed with β-cyclodextrin in 1:1, 1:2 and 1:3 molar ratios using solvent evaporation method with the addition of freeze drying. The prepared inclusion complexes were evaluated for solubility, scanning electron microscopy (SEM), differential scanning calorimetry (DSC), X ray powder diffraction (XRPD) and in vitro dissolution study. All the complexes showed about up to 12 fold increase in solubility. The complex prepared in 1:3 ratios showed the greatest improvement in solubility (from 9.67 to 108.60 μg/ml). In SEM, the complexes showed irregular disc shaped non-porous surface. XRPD data indicated that maximum amorphization was induced in the complex prepared with 1:2 ratio. The DSC data confirmed the formation of inclusion complex. The dissolution of the drug in the complexes was also found to be improved. Complex prepared by solvent evaporation method in 1:2 molar ratio showed a marked improvement in dissolution profile (complete release in just 30 minutes) than that of pure drug which showed just 60.02 % drug release at the end of 3 hour. It was concluded that the β-cyclodextrin complex made in 1:2 molar ratio showed good solubility and the dissolution profile as compared to the complex made in 1:1 and 1:3 molar ratio. It was concluded that the complex prepared by solvent evaporation method with 1:2 molar ratio showed the best performance with respect to great improvement in solubility, the best amorphization and the best in vitro dissolution profile as compared to other complexes.
The term solid dispersion refers to a group of solid products consisting of a hydrophilic matrix and a hydrophobic drug frequently prepared by fusion solvent method. The matrix can be amorphous or crystalline in nature .
liquisolid technology is a topic related to pharmaceutics presented by konatham teja kumar reddy from chilkur balaji college of pharmcy ,hyderabad,telangana
Preparation and Characterization of Cyclodextrin Inclusion Complexes for Impr...Jing Zang
Nimesulide (4'-nitro-2'-phenoxy methane sulfonanilide) is a selective cyclooxygenase-2 inhibitor and one of the potent non steroidal anti-inflammatory drugs (NSAIDs). It is practically insoluble in water and hence has a low bioavailability. To improve solubility and dissolution of nimesulide, its β-cyclodextrin complex were prepared.
Nimesulide was complexed with β-cyclodextrin in 1:1, 1:2 and 1:3 molar ratios using solvent evaporation method with the addition of freeze drying. The prepared inclusion complexes were evaluated for solubility, scanning electron microscopy (SEM), differential scanning calorimetry (DSC), X ray powder diffraction (XRPD) and in vitro dissolution study. All the complexes showed about up to 12 fold increase in solubility. The complex prepared in 1:3 ratios showed the greatest improvement in solubility (from 9.67 to 108.60 μg/ml). In SEM, the complexes showed irregular disc shaped non-porous surface. XRPD data indicated that maximum amorphization was induced in the complex prepared with 1:2 ratio. The DSC data confirmed the formation of inclusion complex. The dissolution of the drug in the complexes was also found to be improved. Complex prepared by solvent evaporation method in 1:2 molar ratio showed a marked improvement in dissolution profile (complete release in just 30 minutes) than that of pure drug which showed just 60.02 % drug release at the end of 3 hour. It was concluded that the β-cyclodextrin complex made in 1:2 molar ratio showed good solubility and the dissolution profile as compared to the complex made in 1:1 and 1:3 molar ratio. It was concluded that the complex prepared by solvent evaporation method with 1:2 molar ratio showed the best performance with respect to great improvement in solubility, the best amorphization and the best in vitro dissolution profile as compared to other complexes.
The term solid dispersion refers to a group of solid products consisting of a hydrophilic matrix and a hydrophobic drug frequently prepared by fusion solvent method. The matrix can be amorphous or crystalline in nature .
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
Formulation and Evaluation of Solid dispersion for Dissolution Enhancement of...Jing Zang
Nifedipine, a calcium channel blocker antihypertensive drug, is a poorly water soluble drug and belongs to BCS class II. The objective of the research work was to formulate and optimize solid dispersions (SDs) of a poorly water soluble drug, nifedipine, with sodium starch glycollate, croscarmellose sodium, eudragit E-100. Solid dispersions were prepared by solvent evaporation techniques in different weight ratios of polymers. The results indicated that homogeneous or heterogeneous conditions during the preparation methods employed governed the internal structures of the polymer matrices while retaining the drug in an amorphous form. The physical mixtures and solid dispersions were subjected to drug content and dissolution test. The best formulation, nifedipine with croscarmellose sodium in 1:7 ratio, among all was further adsorbed on neusilin US2 to form ternary mixture. The increased dissolution was achieved by more than 70percent and 30percent comparatively to the nifedipine API and marketed product respectively. The tablet dosage form prepared from ternary mixture was stable at stressed conditions 40±2°C and 75±5% RH. The release kinetics of drug from formulation and marketed product follows peppas model. The similar factor f2 was within limit for the product at stressed conditions with the product at room temperature at the same time.
Formulation and Evaluation of Liquisolid Compact of Etoricoxib for Solubility...ijpsmjournal
Liquisolid compact technique is a novel concept for delivery of drug through oral route. This
approach of delivering drug is mostly suitable for lipophilic drug and poorly or water insoluble drugs. The
main objective of present study was to increase the solubility of water in soluble BSc class II drug etoricoxib.
Etoricoxib is alipophilic drug that is practically insoluble in water and exhibit an excessively slow dissolution
rate in class II compound in biopharmaceutics classification system. The liquid solid compacts were prepared
using PEG 400 as non volatile solvent, microcrystalline cellulose as carrier, aerosil 200 as coating material
and Sodium starch glycolate was used as super disintegrating agent. Several formulations of liquid solid
compacts having different drug concentration in PEG 400 (non volatile solvent) with varying ratio of career
to coating material were prepared. The liquid solid compacts were evaluated for Bulk characterization, Flow
properties, solubility studies, drug content, FTIR studies, DSC studies and in vitro drug release studies. The
saturated solubility studies and in vitro drug release studies shows that the increase in solubility of drug and
enhanced drug release rate in liquisolid compacts compared to pure drug. The Formulation F5 andF4 is
considered as best formulation as it has shown highest drug release in short time (1 hr). Our studies showed
that the solubility of the drug can be significantly enhanced with increase in the carrier content there is
increase in the solubility resulting and enhanced drug release rate.
Solid dispersion is an effective way of improving the dissolution rate of poorly water soluble drugs and hence its bioavailability. The water soluble carriers used in preparation of solid dispersion enhance the dissolution rate of the poorly water soluble drug. This work reflects the improvement of Dissolution Characteristics as well as Bioavailability of poorly aqueous soluble drug Hydrochlorothiazide. It belongs to BCS class 2 i.e. it has poor water solubility but good permeability.
SEEDS- SELF EMULSIFYING DRUG DELIVERY SYSTEMSSiva Prasad U
A self-microemulsifying drug delivery system is a drug delivery system that uses a microemulsion achieved by chemical rather than mechanical means. That is, by an intrinsic property of the drug formulation, rather than by special mixing and handling.
** Disclaimer: All photos, logos, etc. used in this presentation are the property of their respective copyright owners and are used here for educational purposes only.
Cubosomal nanoparticles as an ocular delivery system of fluconazoleSidharth Mehta
The optimized cubosomal dispersion exhibited spherical nanosized particles and reasonable EE% along with higher
FCZ corneal permeation (twofold) as compared to that of FCZ solution.
Moreover, the in vivo study proved the efficacy and safety FCZ-loaded
cubosomal dispersion in treatment of induced keratomycosis
in rats compared to aqueous FCZ solution after topical ocular
application.
Based on the previous results, the use of
cubosomal dispersion as an ocular drug delivery system is
expected to improve antifungal activity of FCZ in treatment
of fungal keratitis.
Dissolution enhancement of glimepiride by solid dispersion technique.Santosh Adhikari
Dissolution Enhancement of Glimepiride by Solid Dispersion Technique.
Priyanka Shrestha1*, Shiva Kumar Bhandari1, SM Ashraful Islam1, and Santosh Adhikari2.
1Department of Pharmacy, University of Asia Pacific, Dhanmondi, Dhaka-1209, Bangladesh.
2Department of Pharmacy, Rajiv Gandhi University of Health Science, Banglore-560 041.
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.
Improved and Novel Excipients – Need, sources of new excipients-co-processing and particle engineering, benefits of co-processed excipients, characterization, examples, regulatory aspects
A project paper submitted to the Department of Pharmacy, University of Asia Pacific in partial fulfilment of the requirements for the degree of Master of Science in Pharmaceutical Technology.
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
Formulation and Evaluation of Solid dispersion for Dissolution Enhancement of...Jing Zang
Nifedipine, a calcium channel blocker antihypertensive drug, is a poorly water soluble drug and belongs to BCS class II. The objective of the research work was to formulate and optimize solid dispersions (SDs) of a poorly water soluble drug, nifedipine, with sodium starch glycollate, croscarmellose sodium, eudragit E-100. Solid dispersions were prepared by solvent evaporation techniques in different weight ratios of polymers. The results indicated that homogeneous or heterogeneous conditions during the preparation methods employed governed the internal structures of the polymer matrices while retaining the drug in an amorphous form. The physical mixtures and solid dispersions were subjected to drug content and dissolution test. The best formulation, nifedipine with croscarmellose sodium in 1:7 ratio, among all was further adsorbed on neusilin US2 to form ternary mixture. The increased dissolution was achieved by more than 70percent and 30percent comparatively to the nifedipine API and marketed product respectively. The tablet dosage form prepared from ternary mixture was stable at stressed conditions 40±2°C and 75±5% RH. The release kinetics of drug from formulation and marketed product follows peppas model. The similar factor f2 was within limit for the product at stressed conditions with the product at room temperature at the same time.
Formulation and Evaluation of Liquisolid Compact of Etoricoxib for Solubility...ijpsmjournal
Liquisolid compact technique is a novel concept for delivery of drug through oral route. This
approach of delivering drug is mostly suitable for lipophilic drug and poorly or water insoluble drugs. The
main objective of present study was to increase the solubility of water in soluble BSc class II drug etoricoxib.
Etoricoxib is alipophilic drug that is practically insoluble in water and exhibit an excessively slow dissolution
rate in class II compound in biopharmaceutics classification system. The liquid solid compacts were prepared
using PEG 400 as non volatile solvent, microcrystalline cellulose as carrier, aerosil 200 as coating material
and Sodium starch glycolate was used as super disintegrating agent. Several formulations of liquid solid
compacts having different drug concentration in PEG 400 (non volatile solvent) with varying ratio of career
to coating material were prepared. The liquid solid compacts were evaluated for Bulk characterization, Flow
properties, solubility studies, drug content, FTIR studies, DSC studies and in vitro drug release studies. The
saturated solubility studies and in vitro drug release studies shows that the increase in solubility of drug and
enhanced drug release rate in liquisolid compacts compared to pure drug. The Formulation F5 andF4 is
considered as best formulation as it has shown highest drug release in short time (1 hr). Our studies showed
that the solubility of the drug can be significantly enhanced with increase in the carrier content there is
increase in the solubility resulting and enhanced drug release rate.
Solid dispersion is an effective way of improving the dissolution rate of poorly water soluble drugs and hence its bioavailability. The water soluble carriers used in preparation of solid dispersion enhance the dissolution rate of the poorly water soluble drug. This work reflects the improvement of Dissolution Characteristics as well as Bioavailability of poorly aqueous soluble drug Hydrochlorothiazide. It belongs to BCS class 2 i.e. it has poor water solubility but good permeability.
SEEDS- SELF EMULSIFYING DRUG DELIVERY SYSTEMSSiva Prasad U
A self-microemulsifying drug delivery system is a drug delivery system that uses a microemulsion achieved by chemical rather than mechanical means. That is, by an intrinsic property of the drug formulation, rather than by special mixing and handling.
** Disclaimer: All photos, logos, etc. used in this presentation are the property of their respective copyright owners and are used here for educational purposes only.
Cubosomal nanoparticles as an ocular delivery system of fluconazoleSidharth Mehta
The optimized cubosomal dispersion exhibited spherical nanosized particles and reasonable EE% along with higher
FCZ corneal permeation (twofold) as compared to that of FCZ solution.
Moreover, the in vivo study proved the efficacy and safety FCZ-loaded
cubosomal dispersion in treatment of induced keratomycosis
in rats compared to aqueous FCZ solution after topical ocular
application.
Based on the previous results, the use of
cubosomal dispersion as an ocular drug delivery system is
expected to improve antifungal activity of FCZ in treatment
of fungal keratitis.
Dissolution enhancement of glimepiride by solid dispersion technique.Santosh Adhikari
Dissolution Enhancement of Glimepiride by Solid Dispersion Technique.
Priyanka Shrestha1*, Shiva Kumar Bhandari1, SM Ashraful Islam1, and Santosh Adhikari2.
1Department of Pharmacy, University of Asia Pacific, Dhanmondi, Dhaka-1209, Bangladesh.
2Department of Pharmacy, Rajiv Gandhi University of Health Science, Banglore-560 041.
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.
Improved and Novel Excipients – Need, sources of new excipients-co-processing and particle engineering, benefits of co-processed excipients, characterization, examples, regulatory aspects
A project paper submitted to the Department of Pharmacy, University of Asia Pacific in partial fulfilment of the requirements for the degree of Master of Science in Pharmaceutical Technology.
Basic intro to WordPress themes presented at WordCamp Minneapolis 2016 Foundation Friday. Overview of what themes are, what a theme does, where to find themes, how to evaluate themes, searching for themes, installing themes, activating themes, and using the customizer.
Content marketing is awesome. It’s even more awesome (and effective!) when your business has a solid plan in place to guide your content creation efforts.
Thoughtful content strategy helps you understand why content marketing is important to your business, how content creation & promotion can help you meet your goals, and how to measure your results to see what’s working well and what still needs to be fine-tuned. This session will take you step-by-step through the process of creating a basic content strategy plan for your WordPress website.
Presented at WordCamp Minneapolis 2016.
Keyword Mapping: Developing a Content Strategy That Supports SEOJen Jamar
Does your content strategy support ranking well for keywords that drive traffic to your site? The function of a search engine is to deliver relevant results to their users (your potential readers & customers). Each time a user searches on Google, they have the potential to click through to hundreds of thousands of answers to their query. That’s a lot of competition.
Keyword mapping helps define which search queries your site answers best. We’ll begin with an overview of the keyword mapping process, then discuss how apply a keyword map in WordPress to create a framework for your content strategy.
Presented at: WordCamp Minneapolis April 2015
Beginner training on WordPress media and images presented at WordCamp Minneapolis 2016 Foundation Friday. Slides include an introduction to media and images, embeds and uploads, finding images, Creative Commons & Flickr, and managing media on your WordPress site.
Reputation Monitoring & Protection: DATA EVERYWHEREJen Jamar
Presentation by Jen Jamar & Michelle Stinson Ross at Zenith Digital Marketing Conference 2016 #Zenith2016
Session description:
There is a nearly zen relationship between a person or company’s actual BEHAVIOR in the world and the ensuing “reputation” which must be monitored, managed, triaged, contained, grown and/or amplified to advantage.
In other words, even if your company is being trolled by idiots and lauded by loyalists, there’s a more DIRECT relationship between how your company IS in the world and what the Internet SAYS IT IS.
This session will support attendees to:
-Self audit by listening to brand, competitor and category keywords on the right spectrum of channels
-Take a closer look inward to parse what the Internet SAYS you are vs. who you really are. B.S.U.R.S.I.M.I.M (Be as you are, as I am I am)
-Appreciate opportunities by way of examples where other companies and individuals benefitted from positive chatter and look for opportunities yourself
-Experience reputation nightmares through the eyes of many failed companies and learn to not repeat their follies
-Handle trolls who don’t care how good your company is and simply want to say bad things about you (and the wisdom to know the difference)
-Discern if a channel-chatter-challenge is above the listener’s pay grade and when to involve stakeholders and legal
-Get A guided tour of our panelists’ favorite listening tools
-BONUS! Repurpose reputation data for psychographic targeting
Join our panel of hardened Internet war heroes and hold onto your lovin’ hats. When this session is over, you may have a new take on reputation and how your company behaves.
Formulation and Evaluation of W/O/W Multiple Emulsions with Diclofenac SodiumSagar Savale
Multiple emulsion is novel approach of drug delivery system
for enhancement of bioavailability and pharmacological
activity. It is important to prevent the problem of oral drug
delivery system and they are stabilized by using of combination
of hydrophilic and lipophilic surfactant. The specific ratio of
surfactant concentration is responsible for maintaining the
stability of multiple emulsions, the importance of this study was
to prepare multiple emulsion of Diclofenac sodium by using
two step emulsification process, by using the non-ionic
surfactant units. In multiple emulsion, the stability of multiple
emulsion was evaluated, percent entrapment efficiency as well
as in vitro studies are conducted. The process of primary and
secondary emulsification was optimized to get the stable
multiple emulsion with the high entrapment efficiency. Multiple
emulsion to improve bioavailability with the hypothesis that
improvement of drug release profile will reflect the
enhancement of bioavailability of the drug.
Formulation and Evaluation of Fast Disintegrating Tablet of Solid Dispersion ...ijtsrd
The aim of the present work is Formulation and Evaluation of Fast Disintegrating Tablet of Solid Dispersion of Carvedilol. The solid dispersions of Carvedilol were prepared with PEG6000 and PVP K30 in 1 1, 1 2, 1 3 by using Kneading method. The prepared solid dispersions were analyzed for FTIR. Solid dispersions showed a better dissolution compared to the pure drugs and among all the other formulations. The F3 formulation shows high percentage drug release i.e. 96.61 in 40 min and selected as an optimized formulation for the preparation of fast disintegrating tablets of Carvedilol. Crosscarmellose sodium and Crospovidone used in the preparation of fast disintegrating tablets prepared by direct compression method. The post compression parameters of all the prepared tablets were within the limits. FD6 was selected as optimized formulation based on its highest disintegration time 48 sec and drug release 94.87 in 40 min. Hence it concluded that solid dispersions incorporated fast disintegrating tablets is very useful approach for fast disintegration of Carvedilol to treat high blood pressure. Akshada Gavhane | Prof. Mr. Prashant Khade | Dr. Ashok Bhosale "Formulation and Evaluation of Fast Disintegrating Tablet of Solid Dispersion of Carvedilol - A Research" Published in International Journal of Trend in Scientific Research and Development (ijtsrd), ISSN: 2456-6470, Volume-6 | Issue-5 , August 2022, URL: https://www.ijtsrd.com/papers/ijtsrd50379.pdf Paper URL: https://www.ijtsrd.com/pharmacy/pharmaceutics/50379/formulation-and-evaluation-of-fast-disintegrating-tablet-of-solid-dispersion-of-carvedilol--a-research/akshada-gavhane
These lecture slides, by Dr Sidra Arshad, offer a quick overview of physiological basis of a normal electrocardiogram.
Learning objectives:
1. Define an electrocardiogram (ECG) and electrocardiography
2. Describe how dipoles generated by the heart produce the waveforms of the ECG
3. Describe the components of a normal electrocardiogram of a typical bipolar leads (limb II)
4. Differentiate between intervals and segments
5. Enlist some common indications for obtaining an ECG
Study Resources:
1. Chapter 11, Guyton and Hall Textbook of Medical Physiology, 14th edition
2. Chapter 9, Human Physiology - From Cells to Systems, Lauralee Sherwood, 9th edition
3. Chapter 29, Ganong’s Review of Medical Physiology, 26th edition
4. Electrocardiogram, StatPearls - https://www.ncbi.nlm.nih.gov/books/NBK549803/
5. ECG in Medical Practice by ABM Abdullah, 4th edition
6. ECG Basics, http://www.nataliescasebook.com/tag/e-c-g-basics
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
These simplified slides by Dr. Sidra Arshad present an overview of the non-respiratory functions of the respiratory tract.
Learning objectives:
1. Enlist the non-respiratory functions of the respiratory tract
2. Briefly explain how these functions are carried out
3. Discuss the significance of dead space
4. Differentiate between minute ventilation and alveolar ventilation
5. Describe the cough and sneeze reflexes
Study Resources:
1. Chapter 39, Guyton and Hall Textbook of Medical Physiology, 14th edition
2. Chapter 34, Ganong’s Review of Medical Physiology, 26th edition
3. Chapter 17, Human Physiology by Lauralee Sherwood, 9th edition
4. Non-respiratory functions of the lungs https://academic.oup.com/bjaed/article/13/3/98/278874
Prix Galien International 2024 Forum ProgramLevi Shapiro
June 20, 2024, Prix Galien International and Jerusalem Ethics Forum in ROME. Detailed agenda including panels:
- ADVANCES IN CARDIOLOGY: A NEW PARADIGM IS COMING
- WOMEN’S HEALTH: FERTILITY PRESERVATION
- WHAT’S NEW IN THE TREATMENT OF INFECTIOUS,
ONCOLOGICAL AND INFLAMMATORY SKIN DISEASES?
- ARTIFICIAL INTELLIGENCE AND ETHICS
- GENE THERAPY
- BEYOND BORDERS: GLOBAL INITIATIVES FOR DEMOCRATIZING LIFE SCIENCE TECHNOLOGIES AND PROMOTING ACCESS TO HEALTHCARE
- ETHICAL CHALLENGES IN LIFE SCIENCES
- Prix Galien International Awards Ceremony
Recomendações da OMS sobre cuidados maternos e neonatais para uma experiência pós-natal positiva.
Em consonância com os ODS – Objetivos do Desenvolvimento Sustentável e a Estratégia Global para a Saúde das Mulheres, Crianças e Adolescentes, e aplicando uma abordagem baseada nos direitos humanos, os esforços de cuidados pós-natais devem expandir-se para além da cobertura e da simples sobrevivência, de modo a incluir cuidados de qualidade.
Estas diretrizes visam melhorar a qualidade dos cuidados pós-natais essenciais e de rotina prestados às mulheres e aos recém-nascidos, com o objetivo final de melhorar a saúde e o bem-estar materno e neonatal.
Uma “experiência pós-natal positiva” é um resultado importante para todas as mulheres que dão à luz e para os seus recém-nascidos, estabelecendo as bases para a melhoria da saúde e do bem-estar a curto e longo prazo. Uma experiência pós-natal positiva é definida como aquela em que as mulheres, pessoas que gestam, os recém-nascidos, os casais, os pais, os cuidadores e as famílias recebem informação consistente, garantia e apoio de profissionais de saúde motivados; e onde um sistema de saúde flexível e com recursos reconheça as necessidades das mulheres e dos bebês e respeite o seu contexto cultural.
Estas diretrizes consolidadas apresentam algumas recomendações novas e já bem fundamentadas sobre cuidados pós-natais de rotina para mulheres e neonatos que recebem cuidados no pós-parto em unidades de saúde ou na comunidade, independentemente dos recursos disponíveis.
É fornecido um conjunto abrangente de recomendações para cuidados durante o período puerperal, com ênfase nos cuidados essenciais que todas as mulheres e recém-nascidos devem receber, e com a devida atenção à qualidade dos cuidados; isto é, a entrega e a experiência do cuidado recebido. Estas diretrizes atualizam e ampliam as recomendações da OMS de 2014 sobre cuidados pós-natais da mãe e do recém-nascido e complementam as atuais diretrizes da OMS sobre a gestão de complicações pós-natais.
O estabelecimento da amamentação e o manejo das principais intercorrências é contemplada.
Recomendamos muito.
Vamos discutir essas recomendações no nosso curso de pós-graduação em Aleitamento no Instituto Ciclos.
Esta publicação só está disponível em inglês até o momento.
Prof. Marcus Renato de Carvalho
www.agostodourado.com
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
263778731218 Abortion Clinic /Pills In Harare ,sisternakatoto
263778731218 Abortion Clinic /Pills In Harare ,ABORTION WOMEN’S CLINIC +27730423979 IN women clinic we believe that every woman should be able to make choices in her pregnancy. Our job is to provide compassionate care, safety,affordable and confidential services. That’s why we have won the trust from all generations of women all over the world. we use non surgical method(Abortion pills) to terminate…Dr.LISA +27730423979women Clinic is committed to providing the highest quality of obstetrical and gynecological care to women of all ages. Our dedicated staff aim to treat each patient and her health concerns with compassion and respect.Our dedicated group ABORTION WOMEN’S CLINIC +27730423979 IN women clinic we believe that every woman should be able to make choices in her pregnancy. Our job is to provide compassionate care, safety,affordable and confidential services. That’s why we have won the trust from all generations of women all over the world. we use non surgical method(Abortion pills) to terminate…Dr.LISA +27730423979women Clinic is committed to providing the highest quality of obstetrical and gynecological care to women of all ages. Our dedicated staff aim to treat each patient and her health concerns with compassion and respect.Our dedicated group of receptionists, nurses, and physicians have worked together as a teamof receptionists, nurses, and physicians have worked together as a team wwww.lisywomensclinic.co.za/
Pulmonary Thromboembolism - etilogy, types, medical- Surgical and nursing man...VarunMahajani
Disruption of blood supply to lung alveoli due to blockage of one or more pulmonary blood vessels is called as Pulmonary thromboembolism. In this presentation we will discuss its causes, types and its management in depth.
Couples presenting to the infertility clinic- Do they really have infertility...Sujoy Dasgupta
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Ijdrt issue march-april-2015_article1
1. http://www.ijdrt.com 81
Int. J. Drug Res. Tech. 2015, Vol. 5 (2), 81-102 ISSN 2277 - 1506
International Journal of Drug Research and Technology
Available online at http://www.ijdrt.com
Original Research Paper
ENHANCEMENT OF SOLUBILITY AND DISSOLUTION OF CARVEDILOL BY
SOLID DISPERSION TECHNIQUE USING ROTA-EVAPORATION AND
LYOPHILIZATION METHODS
Shivangi Madhok* and Akankasha Madhok
Department of Pharmaceutics, ASBASJSM College of Pharmacy, Bela-140 111, Ropar, India
ABSTRACT
Despite significant advancements in the science of drug delivery, solubilization of poorly aqueous soluble
drugs still remains a challenging task for formulation. The purpose of the study was to improve the
physicochemical properties of poorly aqueous soluble drug carvedilol (CAR) like solubility, dissolution
properties and stability of poorly soluble drug by forming dispersion with skimmed milk powder as carrier.
CAR was formulated by solid dispersions using rota-evaporation method and lyophilization method in
different ratios 1:1, 1:3, 1:5, and 1:7 of drug and carrier (skimmed milk powder). The formulations were
evaluated for various in vitro parameters (Drug content, Drug release, phase solubility studies, dissolution
efficiency, DSC, SEM, XRD) as well as changes in the physical state during storage under different
humidity conditions. Good uniformity of drug content was observed with all formulations and lies between
96.29 % to 99.13 %. All the solid dispersions showed dissolution improvement compare to pure drug. The
solubility was also increased from 23.28 μg/ml in case of carvedilol pure drug to 224.68 μg/ml and 205.31
μg/ml in case of these solid dispersions. The DE60 was also increased from 36.83% to 56.31% and 54.92 %.
The dispersion with skimmed milk powder (1:7) by Rota evaporation Method and Lyophilization Method
(1:5) showed faster dissolution rate (96.1 % and 94.88 % respectively). The tablets were formulated from
the final and stable solid dispersions. These solid dispersions were selected to prepare tablets using Ac-do-
sol as superdisintegrant and Avicel PH102 as diluents. Tablets were characterized for hardness, friability,
disintegration time, percent drug release studies. Tablet T2 showed highest dissolution rate and best
dissolution efficiency at (DE 60) minutes. The similarity factor was calculated for comparison of the
dissolution profile before and after stability studies. The f2 value was found to be more than 50 (~ 94.00)
thereby indicating a close similarity between both the dissolution profiles.
Keywords: Carvedilol (CAR), Skimmed milk powder (SM), Solid dispersions, Rota-evaporation
Method, Lyophilisation method.
INTRODUCTION
Several techniques are commonly used to
improve dissolution and bioavailability of poorly
water-soluble drugs, such as size reduction, the
use of surfactants and the formation of solid
dispersions. The latter are defined as dispersions
of one or more active ingredients in an inert
carrier in the solid state. Mechanisms involved
include increased wettability, solubilisation of the
drug by the carrier at the diffusion layer and
reduction or absence of aggregation and
agglomeration. Moreover, transformation of the
crystalline drug to the amorphous state upon solid
dispersion formulation increases the dissolution
rate since no lattice structure has to be broken
down for dissolution to take place.1
Carvedilol
(CAR), an antihypertensive agent, is used in the
treatment of hypertension, congestive heart
failure, cardiac arrhythmias and angina pectoris.
It is a nonselective β-adrenergic blocker with
selective α-adrenergic blocking. However, drug
2. Shivangi Madhok et al. International Journal of Drug Research and Technology 2015, Vol. 5 (2), 81-102
http://www.ijdrt.com 82
bioavailability is very limited (25-30%), since it
is practically insoluble in water and its dissolution
is rate limiting for its absorption from gastro-
intestinal tract.2
Also CAR is poorly flowable and
compressible drug. Carvedilol is practically
insoluble in water and exhibits pH-dependant
solubility. Its solubility is <1 μg/ml above pH 9.0,
23 μg/ml at pH 7, and about 100 μg/mL at pH 5 at
room temperature. However, up to fourfold
improvement of carvedilol bioavailability could
be achieved by increasing the carvedilol
solubility.3
The solubility of carvedilol in aqueous
solutions with pH ranging from 1 to 4 is limited
due to its protonation, resulting in “in situ”
hydrochloride salt formation, which exhibits
lower solubility in media containing chlorine ions
due to the common-ion effect. It’s extremely low
solubility at alkaline pH levels may prevent the
drug from being available for absorption in the
small intestine and colon, thus making it a poor
candidate for an extended-release dosage form.
Carvedilol undergoes significant stereoselective
first-pass metabolism, resulting in low absolute
bioavailability (30% or less). However, some
sources suggest that this low bioavailability is the
result of poor aqueous solubility.4
The objective
of the present study was enhancement of
solubility of poorly soluble carvedilol with
Skimmed milk powder by solid dispersion. The
solid binary systems were prepared by
maintaining constant drug concentration and
increasing carrier concentrations using physical
mixing and solvent evaporation techniques. The
skimmed milk is a colloidal suspension of casein
micelles, globular proteins and lipoprotein
particles. The principal casein fractions are ɑ-s1,
ɑ-s2, β-casein and k-casein. β-casein is
amphiphilic and acts as a detergent molecule with
surfactant property. The milk also contains whey
proteins with principle fractions of β-lactoglo-
bulin, ɑ-lactalbumin, bovine serum albumin and
immunoglo- bulins. These molecules were found
to be surface active with superior solubility than
caseins. The lyophilisation procedure was chosen
because it provides protection against heat
denaturation of protein molecules. The objective
of the present study was enhancement of
solubility of poorly soluble carvedilol with
skimmed milk powder by solid dispersion.5
The
dissolution characteristics of SDs were evaluated
and compared with pure.
MATERIALS AND METHODS
Materials
Carvedilol (gift sample from Sun pharmaceutical
industries Ltd, India), skimmed milk powder was
purchased from Uttam’s diary (Punjab, India),
sodium hydroxide pellets, methanol, acetone,
methanol LR, TBA, monobasic potassium
phosphate, n-octanol, avicel pH 102, Ac-Di-Sol,
magnesium stearate, Talc. Solid dispersions were
prepared by Rota-evaporation and Lyophilization
methods in four different ratios. Carvedilol and
skimmed milk powder were weighed according to
different weighed ratios.
Methods
Preparation of solid dispersions by rota-
evaporation method
Various ratios of carvedilol (1:1, 1:3, 1:5 and 1:7)
with skimmed milk were prepared. The selected
amount of drug were taken and dissolved in a
minimum amount of acetone. Different ratios of
polymer were taken in pestle mortar. Drug
solution was added in mortar to form a
suspension. The suspension obtained was
transferred in RBF and evaporated in a rotary
evaporator (Heidolph Heivap Advantage ML/GB,
Germany) at a rotation speed of 50 rpm at 50°C
for about 15 min. Passed the dried solid
dispersions through sieve no. # 60 so as to form
uniform granules. The cooled granules were
stored in sealed bags in desiccators for their
evaluation. The prepared samples were compared
for their solubility and dissolution rate studies.
Composition of various solid dispersions prepared
by rota-evaporation enlisted in table 1.6
Preparation of solid dispersions by
lyophilisation technique
Solid dispersions of carvedilol using skimmed
milk powder were prepared by lyophilisation
method. Carvedilol (100 mg) was dissolved in
TBA (20 ml) and required stoichiometric amount
of skimmed milk powder was dissolved in water
(5 ml), both above mentioned solutions were
3. Shivangi Madhok et al. International Journal of Drug Research and Technology 2015, Vol. 5 (2), 81-102
http://www.ijdrt.com 83
mixed to obtain a homogenous carrier and drug
co-solvent system. Various complexes of
carvedilol with skimmed milk powder were
prepared in ratios of 1:1, 1:3, 1:5, 1:7 as enlisted
in table 2. The resulting solutions were frozen at -
20°C in a deep freezer for 1 h. The resulting
solution (25 ml) was taken into round bottom
flask (RBF) and frozen for 2 h followed with a
condenser temperature of -78.5°C. When
complete freezing was achieved the RBF’s were
removed from freezing chamber, vacuum was
applied and samples were subjected to
lyophilisation for 4 h with vacuum of 0.02 mbar.
A complete sublimation of solvents occurred and
a dried mass (the hydrophobic drug-SM complex
lyophilized powder) remained in the RBF. Dried
powder was removed from the freeze- drier and
placed in the desiccators until used. Composition
of various solid dispersions prepared by
lyophilisation technique has enlisted in table 2.7,8
Experimental Studies
Characterization of solid dispersions
Determination of Percentage Yield and Drug
Content
Drug content of the carvedilol solid dispersions
was calculated by dissolving solid dispersions
equivalent to 12.5 mg of carvedilol in a suitable
quantity of methanol (20 ml), filtered using 45
µm Whattman filter paper, suitably diluted with
methanol and analyzed by using UV
spectrophotometer against methanol as blank.
Similarly, the percentage yield of each
formulation was determined according to the
recoverable final weight of solid dispersions and
the total original weight of carvedilol and carrier.
% Yield = ………………1
In equation 1 a is the weight of the solid
dispersion, b is the weight of carvedilol taken for
solid dispersion preparation, and c is the weight
of skimmed milk powder taken for solid
dispersion preparation.9
Solubility of solid dispersions
Solid dispersions equivalent to 12.5 mg were
added to 20 ml of phosphate buffer pH 6.8 in
screw capped vials. The vials were capped
properly and shaken at 37 ◦
C in a temperature
controlled water bath for 48 h. Resultant samples
were centrifuged and filtered, suitably diluted
with phosphate buffer pH 6.8 and analyzed by
UV spectrophotometer at 285.5 nm.
In vitro dissolution studies
Dissolution studies were conducted by using USP
XXIV paddle method (apparatus 2) official in
USP. The stirring rate was 100 rpm. Phosphate
buffer pH 6.8 was used as dissolution medium
(900 ml) and was maintained at 37±0.5◦
C.7
A 5
ml aliquot of sample was withdrawn at 5, 10, 15,
20, 25, 30, 35, 40, 45, 50, 55, 60 min. The
samples were filtered using Whatman filter paper.
The collected samples were suitably diluted and
analyzed for carvedilol content by UV
spectrophotometric method at 285.5 nm. The
volume withdrawn at each time interval was
replaced with equal volume of fresh dissolution
media. Dissolution studies were performed in
triplicate and mean values were taken. A model
independent approach, dissolution efficiency
(DE) was employed to evaluate the dissolution
rate of carvedilol from solid dispersion. DE is
defined as the area under the dissolution curve up
to the time t, (measured using trapezoidal rule)
expressed as a percentage of the area of the
rectangle described by 100 % dissolution in the
same time. DE60 was calculated from the
dissolution data from equation 2 and used for
comparison.
DE % = …………….. 2
Infrared spectroscopy
The infrared spectra (IR) of the samples was
performed on fourier transformed infrared
spectrophotometer (Perkin Elmer 400 spectrum
USA). The pellets of the drug and KBr were
prepared on KBr press. The spectra were scanned
over wave number range of 4000 to 400 cm-1
at
ambient temperature.
X-Ray Diffraction (XRD)
The X-ray diffraction patterns were recorded
using XPERT-PRO diffractometer with Cu Kα
filter generated at 45kV voltage and 40mA
current over a diffraction angle of 2θ.
4. Shivangi Madhok et al. International Journal of Drug Research and Technology 2015, Vol. 5 (2), 81-102
http://www.ijdrt.com 84
Differential Scanning Calorimetry (DSC)
A differential scanning calorimeter (4000 Perkin
Elmer, USA) was used to determine the degree of
drug crystallinity in solid dispersions. About 2-4
mg of sample in open aluminium standard pan
was heated at a scanning rate of 20 /min from a
temperature -50 to 220 under nitrogen gas
flow.
Scanning Electron Microscopy (SEM)
The morphology of carvedilol, skimmed milk
powder and solid dispersions were determined
using a scanning electron microscope (SEM)
(Jeol model JSM-6610, JAPAN) operated at an
accelerating voltage of 3 kV. Samples were
prepared by mounting powder on to a brass stub
using graphite glue and coated with gold under
vacuum before use.
Preparation of Tablets
Formulation of blends
The selected solid dispersions of carvedilol CAR
4, CAR 7 and excipients such as superdisintegrant
(Ac-Di-Sol) and Avicel PH 102 as diluents were
co-grounded in a pestle mortar and passed
through sieve no. 60. Finally talc and magnesium
stearate were added and mixed for 5 min.
Characterization of Blend
Bulk density
The bulk density (ρb) of the blend was determined
by pouring the blend into a graduated cylinder.
The bulk volume (Vb) and weight of powder (M)
was determined. The bulk density was calculated
using the (equation 3).
ρb = M/ Vb …………………………...3
Tapped density
The tapped density was determined by tapping the
measuring cylinder containing a known mass of
blend 100 times using density apparatus. Vt i.e.
the minimum volume occupied in the cylinder
and the weight (M) of the blend was determined.
The tapped density (ρt) was calculated by the
given formula (equation 4)
ρt = M/ Vt …………………………… 4
Compressibility index
The simplest way for measurement of flow of the
powder is its compressibility, an indication of the
ease with which a material can be induced to
flow. It is expressed as compressibility index (I)
which can be calculated as follows (equation 5)
I= ρt-ρb/ρt × 100 ………………….. 5
Where, ρt = tapped density
ρb = bulk density
Angle of repose
It was determined by the funnel method in which
the blend was poured through a funnel that can be
raised vertically until a specified cone height (h)
was obtained. Radius (r) and the height of the
heap formed was measured and angle of repose
(θ) was calculated using the formula (equation 6)
tan θ= h/r ; θ= tan-1
(h/r) …………….. 6
Hausner’s ratio
Hausner ratio (Hr) is an indirect index of ease of
powder flow. It is calculated by the following
formula (equation 7)
Hr = ρt/ρb ………………………….. 7
Where, ρt is tapped density and
ρb is bulk density
Low Hausner’s ratio i.e < 1.25 indicates better
flow properties
Preparation of Tablets
The tablets of selected solid dispersion CAR 4
AND CAR 7 weighing 200 mg were prepared by
direct compression method by using 8 mm
concave die punch set with single punch machine.
Each tablet contained solid dispersions equivalent
to 10 mg of carvedilol. The formula for tablet is
as follows in table 3.
Characterization of tablets
After compression of powder the tablets were
evaluated for organoleptic properties such as
colour, odour, taste, thickness, hardness,
friability, content uniformity, disintegration time
and in vitro dissolution studies.
General Appearance
The general appearance of a tablet, its visual
identification and over all elegance is essential for
consumer acceptance. This includes tablet’s size,
shape, colour, presence or absence of an odour,
taste, surface texture, physical flaws etc.
5. Shivangi Madhok et al. International Journal of Drug Research and Technology 2015, Vol. 5 (2), 81-102
http://www.ijdrt.com 85
Tablet Thickness
Thickness of the tablet is an important
characteristic in reproducing appearance and also
in counting by suing filling equipment. Some
filling equipment utilizes the uniform thickness of
the tablets as a counting mechanism. Ten tablets
were taken and their thickness was recorded using
micrometer (Mityato, Japan).
Weight Variation
In this case twenty tablets were taken and their
weight was determined individually and
collectively on a digital weighing balance. The
average weight of one tablet was determined from
the collective weight. The weight variation of
each tablet was determined. The weight variation
test would be satisfactory method of determining
the drug content uniformity.
Friability
Friability of the tablets was determined using
Roche friabilator. In this the tablets were
subjected to the combined effect of abrasions and
shock in a plastic chamber revolving at 25 rpm
and dropping the tablets at the height of 6 inches
in each revolution. Pre-weighed sample of tablets
are placed in the friabilator and were subjected to
100 revolutions. The friability (% F) was
determined by the formula (equation 8)
% F = (1-W°/W) × 100 ………………. 8
Where, %F is percentage friability
W° is initial weight of the tablets before test
W is the final weight of the tablets after test
Hardness
Hardness of tablet is defined as the force applied
across the diameter of the tablet in order to break
the tablet. The resistance of the tablet to chipping,
abrasion or breakage under conditions of storage,
transportation and handling before usage depends
on its hardness. Hardness of the tablet of each
formulation was determined using Pfizer hardness
tester.
Content Uniformity
Ten tablets were randomly selected, weighed and
powdered in a glass mortar pestle. The weight of
the powder equivalent to 10 mg of carvedilol was
weighed and dissolved in 20 ml of methanol in
volumetric flask. 10 ml of this solution was taken
and volume was made upto 100 ml with methanol
and the solution was filtered. An aliquot of 1.0 ml
of solution were diluted to 10 ml methanol in
separate volumetric flask. The content uniformity
in each formulation was determined
spectrophotometrically at 286 nm.
In Vitro Disintegration Test
In vitro disintegration time was determined using
disintegration test apparatus. In this case, one
tablet was placed in each of six tubes of apparatus
and a disc was added to each tube i.e. 3 inches
long, opens at the top, and held against a 10 mesh
screen at the bottom end of the basket rack
assembly. The basket rack assembly was
positioned in a 1 litre of phosphate buffer pH 6.8.
The time taken for the tablet to disintegrate
completely and pass through the screen was
measured.
In Vitro Dissolution Test
In vitro dissolution studies of tablets were
performed in phosphate buffer pH 6.8 using
rotating paddle method. A tablet was added to
900 ml of phosphate buffer pH 6.8 at 100 rpm at
37 C ± 0.5 C. 5 ml of aliquots were withdrawn at
5, 10, 15, 20, 25, 30, 35, 40, 45, 50, 55, 60 min
and immediately filtered through Whatmann filter
paper no. 41. At each sampling, an equal volume
of fresh medium was added. The concentration of
carvedilol was measured spectrophotometrically
at 285.5 nm. The dissolution efficiency (% DE60)
of the tablets was determined in order to compare
with the marketed tablet.
Stability Studies
Carvedilol tablets were kept in ambered coloured
bottles and the stability studies of CAR tablets
were checked as per ICH guidelines at 40 ± 2◦
C
and 75 ± 5% RH up to 3 months. During the
study period the formulations were withdrawn at
predetermined time intervals of 0, 15, 30, 45, 60,
75, and 90 days for change in physical
characterization, drug content and in vitro
dissolution studies. FDA has placed more
emphasis on a dissolution profile comparison in
the area of post- approval changes. Among
several methods investigated for dissolution
6. Shivangi Madhok et al. International Journal of Drug Research and Technology 2015, Vol. 5 (2), 81-102
http://www.ijdrt.com 86
profile comparison, f2 (similarity factor) is the
simplest. Moore and Flanner proposed a model
independent mathematical approach to compare
the dissolution profile using similarity factor (f2).
The similarity factor (f2) is a logarithmic
reciprocal square root transformation of the sum
of square errors and is a measurement of the
similarity in the percent (%) dissolution between
the curves. Generally similarity factor in the
range of 50-100 is acceptable according to US
FDA and it was determined by the formula
(equation 9).10
f2 = 50 log {[1+ 2]-0.5 *100 …..9
Where, n is the no. of time points, Rt is the
dissolution value of the reference batch
(prechange) at time t and Tt is the dissolution
value of the test batch (postchange) at time t.
RESULTS AND DISCUSSION
Percentage Yield
The % yield was calculated to know about %
yield or efficiency of any method which helps in
selection of appropriate method of production.
The decrease in % yield which is attributed to
difficulty of sieving (table 4 and figure 1).
Drug Content
The drug content of the prepared solid dispersions
was found to be in the range of 96.29-99.13 %
indicating the application of present methods for
the preparation of solid dispersions with high
content uniformity (table 4).
Solubility Studies
Solubility of drug increased with the increase in
the ratio of polymer. But in case of CAR 7 molar
ratio of 1:7 solid dispersion the solubility of drug
decreased due to less drug-polymer entrapment
(table 5 and figure 2).
Dissolution Studies
The in vitro release profile of carvedilol and all
solid dispersions CAR 1, CAR 2, CAR 3, CAR 4,
CAR 5, CAR 6, CAR 7 and CAR 8 are shown in
table 6 and table 7. Figure 3 and figure 4 showed
the comparison of cumulative percent drug
released versus time. In all the cases, cumulative
percent released was much greater than pure
carvedilol. The dissolution rates were enhanced
with increasing concentration of polymer. Higher
dissolution rates were shown by the solid
dispersions of drug with skimmed milk powder as
compared to the pure drug.
Pure carvedilol yielded the slowest percent
release due to its hydrophobic property causing
the powder to float on the surface of the
dissolution media and prevented its surface to
make contact with the medium for initial time
intervals. Hence the enhancement of the
carvedilol dissolution rate by solid dispersion
technique compared with that of the pure drug
could presumably be explained by the following
factors: 1) surfactant properties of the carrier 2)
low viscosity of the carrier 3) a decrease in
crystallinity and size of the drug crystals in the
solid dispersions 4) increased solubility of the
drug.
When the mixture comes in contact with the
media, the polymer particles might have hydrated
rapidly into polymer solution solubilises the
adjacent drug particles and subsequently releases
the drug into the medium.
Dissolution Efficiency
Dissolution efficiency of pure carvedilol, solid
dispersions prepared with skimmed milk powder
by different methods at 60 min were calculated
which is shown in table 8 and comparison of %
DE60 of different formulations is shown in figure
5.
FTIR Studies: FTIR (Fourier Transform
Infrared Spectroscopy)
The IR spectra of SDs were compared with the
standard spectrum of carvedilol. FTIR spectrum
of carvedilol, skimmed milk powder and their
solid dispersions are shown in figure 6, figure 7,
figure 8, figure 9, and figure 10. From the FTIR
study it was found that some of the peaks of the
drugs were shifted broadened, some present with
reduced intensity and some vanished. This was
referred to formation of a complex between the
drug and carrier. Complexation was leading to
formation of an amorphous form of drug with
skimmed milk powder by solid dispersion leading
to improve the dissolution rate of drug.
7. Shivangi Madhok et al. International Journal of Drug Research and Technology 2015, Vol. 5 (2), 81-102
http://www.ijdrt.com 87
X-RD (X-Ray Diffraction) Studies
X-RD pattern of CAR (figure 11) showed several
sharp high intensity peaks at diffraction angle 2θ
of 5.9666, 17.546, 17.7051 and 18.5126, which
suggested CAR as crystalline material. Table 5.7
shows XRD data of CAR and physical mixture.
XRD pattern of skimmed milk powder (figure 12)
showed its amorphous nature. XRD pattern of
physical mixture (figure 13) showed several
characteristic sharp peaks of CAR at diffraction
angles of 2θ of 5.9884, 17.1862, 17.7061 and
18.6132. Significant peaks of both carvedilol and
skimmed milk powder were present in physical
mixture and slight significant shift in the peaks
was observed, which suggested very less to no
chemical interaction between drug and polymer.
A total drug amorphization were observed in the
XRD diffractogram of CAR-SM rota evaporated
solid dispersion in drug/ polymer ratio 1:7 (CAR
4) and lyophilized solid dispersion in drug/
polymer ratio 1:5 (CAR 7) only two broad peaks
at diffraction angle 2θ of 16.54°, 19.34° and
16.54°, 27.67° respectively corresponding to the
diffraction pattern of drug were recorded while
other peaks of carvedilol crystals were completely
disappeared thus suggesting that CAR 4 and CAR
7 inhibited the crystallization of carvedilol
through the formation of complex. XRD of solid
dispersions are shown in fig 14 and figure 15.
SEM (Scanning Electron Microscopy)
SEM images of pure carvedilol, skimmed milk
powder, physical mixture and solid dispersions
are shown in figure 16, figure 17, figure 18,
figure 19, figure 20 and figure 21. The pure
carvedilol shown in figure 16, figure 17 at
different magnifications showed blunt crystals.
The parent carvedilol crystals were in the form of
rod shaped crystals, which is in confirmation with
the earlier report. This rod shaped form of
carvedilol leads to very poor flow and
compression difficulties. The prepared solid
dispersion agglomerates were spherical to larger
extent and remaining was irregular in shape with
smooth surface, which enabled them flow very
easily. In case of solid dispersions figure 18,
figure 19, figure 20 and figure 21. It was difficult
to distinguish the presence of carvedilol crystals
appeared to be incorporated into particles of the
skimmed milk powder.
DSC (Differential Scanning Calorimetry)
The characteristic endothermic peak,
corresponding to drug melting point disappeared
in solid dispersions. This might be due to higher
polymer concentration and uniform distribution of
drug in the crust of polymer, resulting in complete
miscibility of molten drug in polymer. Absence of
peak for the drug indicates that the drug is
distributed homogenously in an amorphous state
within the solid dispersions without any
interaction. No characteristic melting peak of
CAR i.e. 119.17 °C was found in DSC curves of
CAR 4 as shown in figure 25 and CAR 7 as
shown in figure 26 solid dispersions. The peaks in
the solid dispersions (CAR4 and CAR 7)
appeared at 95.42°C, 149.59°C and 95.42°C,
136.36°C respectively. Thus clearly indicated that
drug was in an amorphous state which confirmed
the results obtained from XRD.
Formulation and Characterization of Tablets
The tablets were made of the final and stable
formulation CAR 4 and CAR 7. Total two
formulations were formulated and designated as
T1and T2. The characterization of mixed blend
was performed for the flow property of powder
which includes bulk density, tapped density,
hausner’s ratio, compressibility index, angle of
repose as shown in table 9 for quality control
parameters like hardness, thickness, friability,
disintegration time, in vitro dissolution studies
and drug content are shown in table 10. Drug
content in the selected solid dispersions as shown
in table 11. Dissolution efficiency of all the
tablets were calculated at 60 min and data is
shown in table 12. Flowability of CAR and its
tablet blend was determined. HR and angle of
repose was much improved compared to those of
original powder (untreated carvedilol). In case of
pure CAR powder couldnot pass through the
funnel during the angle of repose experiment. The
poor flow of CAR could be due to the irregular
shape and high fineness of the powder, which
posed hurdles in the uniform flow from the
funnel. It is obvious from CI value that the flow
of untreated CAR is extremely poor due to high
8. Shivangi Madhok et al. International Journal of Drug Research and Technology 2015, Vol. 5 (2), 81-102
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cohesivity and adhesivity. Because of poor
flowability and compatibility of untreated CAR
powder. The micrometric properties of CAR can
be improved forming tablet blends using
magnesium stearate (antiadherent) and talc
(glidant, lubricant). All tablet blends showed
lower CI than untreated CAR, which is an
identical improvement in flow behaviour of the
particles could be due to an increase in true
density of CAR powders as shown in table 9. The
difference in the bulk density of CAR samples
may be related to their markedly different crystal
habbits, leading to different contact points and
frictional, cohesive forces between the crystals.
These are in good agreement morphology of CAR
4 and CAR 7 tablet blends. Dissolution was
carried out on the tablets and marketed
preparation. The in vitro release data in table 12
indicated that the maximum drug release was
found in T2. Dissolution profile of carvedilol
from marketed tablet and best formulations (T1
and T2) are shown in figure. 27. In vitro release
studies reveal that there is marked increase in
dissolution efficiency of carvedilol from all the
solid dispersions when compared to marketed
tablet. From the in vitro drug release profile, it
can be seen that formulation CAR 4 containing
SM (1:7 ratio of drug : SM) and CAR 7
containing SM (1:5 ratio of drug : SM) showed
higher dissolution efficiency compared with
marketed tablet i.e., 54.25 % and 58.61%
respectively in 60 min. The results in vitro drug
release of CAR solid dispersion tablets (T1 and
T2) indicated that no dissolution was achieved for
marketed tablet with only 57.66 % dissolved after
60 min. Results in table 13 showed that the
dissolution of marketed tablet was slowest as
compared to solid dispersion tablets (T1 and T2)
which showed significant enhancement in CAR
dissolution because as the soluble carrier
dissolves the insoluble drug gets exposed to
dissolution media in the form of very fine
particles which dissolves quickly. The
disintegrant Ac-Di-Sol shows the faster
disintegration and thus enhances the dissolution
rate of tablets. The evident improvement obtained
with rota evaporated products was a consequence
of the closer contact between the components and
the better dispersion of the drug into the
hydrophilic carrier obtained through rota
evaporated technique.
Stability Studies
The T2 formulation showed no significant
variation in all the parameters under the test
period at different conditions i.e. (40 ± 2°C and
75 ± 5 % RH). The results are shown in table 14
and in vitro release studies has enlisted in table
14. There was no significant variation in the in
vitro drug release profile over a period of three
months as shown in figure 28. The similarity
factor was calculated for comparison of the
dissolution profile before and after stability
studies. The f2 value was found to be more than
50 (~ 94.00) which indicated a close similarity
between both the dissolution profiles (T2 and S2)
dissolution profile of T2 and S2 tablets were
shown in table 15.
Hence, the results of the stability studies
confirmed that the developed formulation is very
stable.11
CONCLUSION
The objective of the present study was to improve
the solubility and dissolution behaviour of the
poorly water soluble drug Carvedilol by solid
dispersion technique using skimmed milk powder
as carrier. Results from the present study suggest
that the low oral bioavailability of CAR could be
well circumvented by lyophilisation monophase
solution technology and rota evaporation
technique. Complexation with SM significantly
improved the dissolution rate of CAR through a
number of factors such as drug amorphization and
increased drug high degree of porosity. The
present results showed that the solid dispersion
and the solvent evaporation (rota evaporation
method and lyophilisation method) seem to
possess great potential to significantly enhance
the solubility and dissolution rate of poorly
soluble drugs. Results showed that in rota
evaporation technique carvedilol was absorbed
after equilibrium in acetone solution. Thus this
method was suitable to produce dispersions with
best distribution of drug within the carrier in thin
9. Shivangi Madhok et al. International Journal of Drug Research and Technology 2015, Vol. 5 (2), 81-102
http://www.ijdrt.com 89
layer and as a consequent best possible drug
release. TBA was found to be an excellent freeze-
drying medium. It is miscible with water in any
proportion. It possesses a very high vapour
pressure (41.25 mmHg at 25°C), a high melting
point (24°C) and has a low toxicity. Moreover,
adding TBA to water results in formation of
larger needle- shaped ice crystals with a higher
surface area and porosity than round ice crystals
that can facilitate sublimation. All these factors
contribute TBA as an ideal freeze- drying
medium that could be removed rapidly and
completely by freeze- drying. Among all the
prepared formulations, the rota evaporates i.e.
CAR 4 solid dispersion prepared by SM and
lyophilized dispersion i.e. CAR 7 prepared by SM
showed marked increase in the solubility as well
as dissolution when compared to pure drug and
marketed formulation. Physical characterization
of prepared solid dispersions have also been
performed by DSC, FTIR, XRD and SEM to find
the evidence of interaction and XRD analysis
showed that there was a considerable decrease in
the crystallinity of the drug which increased the
surface area thereby increasing the dissolution
and enhancement in the drug release. Freeze dried
solid dispersions in 1:7 ratios (CAR-SM) and rota
evaporated solid dispersions 1:8 ratios (CAR-SM)
were proven to be advantageous in context of
enhancing carvedilol dissolution characteristics in
basic medium. SEM photograph of solid
dispersions (CAR-SM) clearly revealed a change
in the morphology of the drug particles. The
formation of amorphous aggregates was observed
in CAR 4 and CAR 7 solid dispersions. The
selected solid dispersion with the best ratio from
each method were formulated into tablets using
Avicel PH102 (diluents), Ac-Di-Sol
(superdisintegrant), talc and magnesium stearate
as excipients. In vitro results demonstrated that
rotaevaporated and lyophilized solid dispersion
tablets (T1 and T2) containing carvedilol can
result in rapid dissolution of carvedilol at
intestinal pH.
The developed tablets (T1 and T2) may be an
alternative to conventional oral tablets of
carvedilol which usually suffers from a slow
dissolution and poor solubility and low oral
bioavailability. The physical stability of the final
formulations proved to be unchanged after the
storage upto 3 months at accelerated stability
condition (40 ± 2 C and 75 ± 5 % RH).
AKNOWLEDGEMENT
The author’s wishes to thank Ankur Laboratories
Pvt. Ltd. and Sun Pharma, Mumbai for gift
sample of Carvedilol. The author also offers
special thanks to Loba Chemie Pvt. Ltd. for
providing various chemicals without which the
present work would not have been completed.
Table 1: Compositions of S.D containing CAR and SM with rota-evaporation method
Table 2: Composition of S.D containing CAR and SM with lyophilization method
S. No. Formulation code Drug : Carrier ratio
1 CAR1 1:1
2 CAR 2 1:3
3 CAR 3 1:5
4 CAR 4 1:7
S. No. Formulation code Drug : Carrier ratio
1 CAR 5 1:1
2 CAR 6 1:3
3 CAR 7 1:5
4 CAR 8 1:7
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Table 3: Composition of optimized solid dispersion tablets
Ingredients Weight (mg) Weight (mg)
SD 1:5 (T1) 60 -
SD 1:7 (T2) - 80
Ac-Di-Sol 8 8
Avicel pH 102 120 100
Talc 6 6
Magnesium stearate 6 6
Table 4: Percent yield and percent drug content of S.D with rota-evaporation method
and lyophilization method
Formulation code % Yield % Drug Content
CAR 1 83.2% 97.12±0.385
CAR 2 82.6% 98.18±0.669
CAR 3 79.03% 96.29±0.266
CAR 4 80.38% 99.13±0.259
CAR 5 84.2% 97.12±0.385
CAR 6 83.6% 98.18±0.669
CAR 7 78.03% 96.29±0.266
CAR 8 79.01% 98.15±0.259
All results were calculated as mean ± SD, n=3
Figure 1: Percentage yield of different solid dispersions of carvedilol.
Table 5: Solubility of S.D with rota-evaporation method and lyophilization method
All results were calculated as mean ± SD, n=3
Formulation code Solubility (µg/ml)
CAR 1 43.43±0.010
CAR 2 117.5±0.021
CAR 3 150.62±0.019
CAR 4 224.68±0.017
CAR 5 66.56±0.010
CAR 6 186.75±0.021
CAR 7 205.31±0.019
CAR 8 65.98±0.017
11. Shivangi Madhok et al. International Journal of Drug Research and Technology 2015, Vol. 5 (2), 81-102
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Figure 2: Solubility studies of different solid dispersions of carvedilol
Table 6: Dissolution profile of pure CAR AND SM with rota-evaporation method
Cumulative Mean Percent Released ± S.D.
Time (min) Pure Drug CAR 1 CAR 2 CAR 3 CAR 4
5 10.8±0.265 20.85±0.422 20.48±0.23 27.23±0.215 23.18±0.225
10 11.69±0.240 27.62±0.340 22.73±0.225 30.38±0.225 33.39±0.127
15 12.82±0.220 30.83±0.450 25.14±0.225 33.76±0.225 33.99±0.23
20 13.72±0.225 31.74±0.22 31.26±0.230 36.54±0.132 39.76±0.127
25 16.03±0.155 34.36±0.341 33.71±0.225 38.11±0.132 42.66±0.098
30 17.55±0.225 38.41±0.345 37.81±0.132 41.11±0.127 44.16±0.132
35 18.69±0.23 39.39±0.225 41.28±0.178 58.6±0.132 67.36±0.132
40 19.8±0.225 40.81±0.341 42.36±0.121 67.98±0.225 69.95±0.250
45 21.6±0.220 41.41±0.225 44.95±0.23 77.88±0.21 88.40±0.127
50 22.93±0.196 49.45±0.346 60.08±0.210 88.11±0.414 90.48±0.215
55 25.03±0.240 54.40±0.853 72.98±0.121 91.71±0.161 94.45±0.127
60 27.23±0.215 65.85±0.127 73.7±0.167 92.86±0.121 96.1±0.215
All results were calculated as mean ± SD, n=3
Table 7: Dissolution profile of pure CAR and SM with lyophilization method
Cumulative Mean Percent Released ± S.D.
Time (min) Pure Drug CAR 5 CAR 6 CAR 7 CAR 8
5 10.8±0.265 22.73±0.225 20.27±0.2 22.28±0.225 22.73±0.225
10 11.69±0.240 27.91±0.23 22.73±0.225 30.16±0.22 27.91±0.23
15 12.82±0.220 30.18±0.368 25.13±0.341 33.54±0.22 30.01±0.568
20 13.72±0.225 30.61±0.389 31.96±0.225 37.74±0.132 30.9±0.469
25 16.03±0.155 31.74±0.22 37.81±0.225 38.4±0.236 31.96±0.593
30 17.55±0.225 35.48±0.127 40.21±0.127 43.89±0.225 35.56±0.225
35 18.69±0.23 36.76±0.345 42.54±0.225 67.31±0.23 36.76±0.345
40 19.8±0.225 41.26±0.341 45.02±0.23 70.01±0.225 41.26±0.341
45 21.6±0.220 48.62±0.675 49.97±0.225 86.09±0.121 48.62±0.675
50 22.93±0.196 49.82±0.341 65.88±0.127 90.02±0.255 49.96±0.226
55 25.03±0.240 63.56±0.564 67.46±0.132 92.5±0.215 63.56±0.564
60 27.23±0.215 69.56±0.45 76.72±0.127 94.88±0.121 69.56±0.45
All results were calculated as mean ± SD, n=3
12. Shivangi Madhok et al. International Journal of Drug Research and Technology 2015, Vol. 5 (2), 81-102
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Figure 3: In vitro dissolution profile of pure CAR and SM with rota-evaporation method
Figure 4: In Vitro dissolution profile of pure CAR and SM with lyophilization method
Table 8: Dissolution efficiency of solid dispersions prepared by different methods
Formulation
code
% DE60
CAR 1 36.83±0.353
CAR 2 39.13±0.191
CAR 3 53.15±0.276
CAR 4 56.31±0.167
CAR 5 37.82±0.356
CAR 6 40.59±0.190
CAR 7 54.92±0.202
CAR 8 39.94±0.409
All results were calculated as mean ± SD, n=3
Figure 5: Comparison of % DE60 of different formulations
14. Shivangi Madhok et al. International Journal of Drug Research and Technology 2015, Vol. 5 (2), 81-102
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Figure 9: FTIR spectrum of CAR 4
Figure 10: FTIR spectrum of CAR 7
Figure 11: X-RD pattern of Carvedilol
RC SAIF PU, Chandigarh
Spectrum Name: Shivangi Madhok-4.sp Description: SD-1:5 L
Date Created: fri may 31 13:17:55 2013 India Standard Time (GMT+5:30)
4000.0 3600 3200 2800 2400 2000 1800 1600 1400 1200 1000 800 600 450.0
11.0
14
16
18
20
22
24
26
28
30
32
34
36
38
40
42
44
46
48
50
53.0
cm-1
%T
3526
3382
3342
2932
2900 1655
1607
1505
1454
1440
1394
1345
1305
1255
1221
1167
1115
1095
1072
1058
1036
1020
915
899
876
754
722
672
631
605
552
469
RC SAIF PU, Chandigarh
Spectrum Name: Shivangi Madhok-5.sp Description: SD-1:7 R
Date Created: fri may 31 13:25:55 2013 India Standard Time (GMT+5:30)
4000.0 3600 3200 2800 2400 2000 1800 1600 1400 1200 1000 800 600 450.0
2.5
4
6
8
10
12
14
16
18
20
22
24
26
28
30
32
34
36
36.9
cm-1
%T
3526
3382
3344
2976
2933
2900
2067
1656
1607
1585
1538
1506
1454
1440
1393
1359
1344
1305
1257
1221
1202
1168
1142
1116
1095
1072
1058
1035
1019
988
915
899
875
843
779
755
721
671
631
604
566
551
468
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Figure 12: X-RD pattern of skimmed milk powder
Figure 13: X-RD pattern of physical mixture
Figure 14: X- Ray diffraction of S.D. CAR 4
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Figure 15: X- Ray diffraction of S.D. of CAR 7
Figure 16: SEM image of CAR at 1,000 X
Figure 17: SEM image of CAR at 1,500 X
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Figure 18: SEM image of S.D. of CAR 4 with rota evaporation method at 750 X
Figure 19: SEM image of S.D. of CAR 4 WITH rota evaporation method at 3,000 X
Figure 20: SEM image of S.D. of CAR 7 with lyophilization method at 1,300X
Figure 21: SEM image of S.D. of CAR: SM (1:5) with lyophilization method at 1500 X
18. Shivangi Madhok et al. International Journal of Drug Research and Technology 2015, Vol. 5 (2), 81-102
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Figure 22: DSC Themogram of carvedilol
Figure 23: DSC Themogram of Skimmed Milk Powder
Figure 24: DSC Themogram of physical mixture
Figure 25: DSC Themogram of CAR 4
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Table 9: Characterization of blends of selected SD tablets
Formulation
Code
Bulk Density
(g/cm3
)
Tapped Density
(g/cm3
)
Hausner’s Ratio
(Hr)
Compressibility
Index (%) (CI)
Angle of Repose ( )
T1 0.532 ± 0.62 0.637 ± 0.18 1.079 ± 0.67 12.26 ± 0.53 28.09 ± 0.17
T2 0.567 ± 0.04 0.641 ± 0.03 1.130 ± 0.15 11.54 ± 0.01 27.88 ± 0.01
Data is expressed in mean ± S.D (n=3)
Table 10: Characterization of selected solid dispersion tablets
Formulation
Code
Thickness
(mm)
Hardness
(kg/cm2)
Weight
Variation (mg)
Friability
(%)
Disintegration
Time (minutes)
T1 3.32 ± 0.76 3.4 ± 0.58 193 ± 1.98 0.50 ± 0.19 6 ± 0.01
T2 3.36 ± 0.70 3.3 ± 0.59 191 ± 1.96 0.51 ± 0.12 5 ± 0.01
Data is expressed in mean ± S.D (n=3)
Table 11: Drug content in the selected solid dispersion tablets
Formulation Code Drug Content (mg/tablet) Drug Content (%)
T1 9.72 ± 0.022 97.2
T2 9.85 ± 0.013 98.5
Data is expressed as mean ± S.D (n=3)
Table 12: Dissolution efficiency of selected formulation tablets and marketed tablet
S. No. Formulation code Dissolution efficiency (% DE60)
1 Marketed tablet 28.67
2 T1 54.25
3 T2 58.61
Figure 27: Dissolution profile of carvedilol from marketed tablet and best formulations (T1 AND T2)
20. Shivangi Madhok et al. International Journal of Drug Research and Technology 2015, Vol. 5 (2), 81-102
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Table 13: Dissolution profile of carvedilol from marketed tablet and selected solid
dispersion tablets before stability studies
Data is expressed as mean ± S.D (n=3)
Table 14: Evaluation parameters after stability studies for T2
Parameters Conditions 40 ± 2 C and 75 ± 5 % RH
Time period (days) 0 15 30 45 60 75 90
Color appearance White White White White White White White
Drug content 97.3 98.7 99.1 97.5 98.8 96.9 97.2
Hardness (kg/cm2)
3.5 3.1 3.4 3.1 2.9 3.3 3.5
Disintegration time (mins) 6 6.5 6 6 5 6 6.6
Table 15: Dissolution profile of carvedilol from marketed product and solid dispersion
tablets after stability studies
Data is expressed as mean ± S.D (n=3)
Time (min) Cumulative mean percent released ± S.D.
Marketed Tablet T1 Tablets T2 Tablets
5 20.03 ± 0.230 24.10 ± 0.215 23.86 ± 0.230
10 25.89 ± 0.340 35.66 ± 0.641 34.98 ± 0.589
15 31.08 ± 0.389 40.09 ± 0.220 39.89 ± 0.230
20 35.34 ± 0.127 47.19 ± 0.240 45.76 ± 0.125
25 40.07 ± 0.121 58.19 ± 0.564 56.98 ± 0.161
30 45.98 ± 0.230 68.9 ± 0.220 63.18 ± 0.240
35 48.85 ± 0.568 79.10 ± 0.230 72.19 ± 0.422
40 51.08 ± 0.564 87.58 ± 0.230 80.76 ± 0.220
45 53.76 ± 0.161 90.73 ± 0.121 91.98 ± 0.230
50 55.16 ± 0.422 91.99 ± 0.125 93.88 ± 0.340
55 56.10 ± 0.122 94.12 ± 0.340 94.78 ± 0.240
60 57.66 ± 0.265 96.81 ± 0.215 97.26 ± 0.161
Time (min) Cumulative mean percent released ± S.D.
Marketed
Tablet
T2 Tablets S2 Tablets
5 20.03 ± 0.23 23.86 ± 0.23 23.32 ± 0.34
10 25.89 ± 0.34 34.98 ± 0.589 33.87 ± 0.161
15 31.08 ± 0.389 39.89 ± 0.23 38.9 ± 0.22
20 35.34 ± 0.127 45.76 ± 0.125 45.87 ± 0.126
25 40.07 ± 0.121 56.98 ± 0.161 55.99 ± 0.389
30 45.98 ± 0.23 63.18 ± 0.24 64.17 ± 0.23
35 48.85 ± 0.568 72.19 ± 0.422 73.10 ± 0.48
40 51.08 ± 0.564 80.76 ± 0.22 81.22 ± 0.96
45 53.76 ± 0.161 91.98 ± 0.23 91.84 ± 0.27
50 55.16 ± 0.422 93.88 ± 0.34 94.20 ± 0.58
55 56.10 ± 0.122 94.78 ± 0.24 95.90 ± 0.84
60 57.66 ± 0.265 97.26 ± 0.161 98.66 ± 0.71
21. Shivangi Madhok et al. International Journal of Drug Research and Technology 2015, Vol. 5 (2), 81-102
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Figure 28: Dissolution profile of selected solid dispersion tablets before and after stability studies
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Correspondence Author:
Shivangi Madhok*
Department of Pharmaceutics, ASBASJSM College of Pharmacy, Bela-140 111, Ropar, India
22. Shivangi Madhok et al. International Journal of Drug Research and Technology 2015, Vol. 5 (2), 81-102
http://www.ijdrt.com 102
Cite This Article: Shivangi, Madhok and Akankasha, Madhok (2015), “Enhancement of solubility and
dissolution of carvedilol by solid dispersion technique using rota-evaporation and lyophilization methods”,
International Journal of Drug Research and Technology, Vol. 5 (2), 81-102.