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RAJIV GANDHI UNIVERSITY OF HEALTH SCIENCES, KARNATAKA,
BANGALORE.
M. PHARM SYNOPSIS
YEAR OF ADMISSION-MAY 2009
TITLE OF THE SYNOPSIS
DESIGN AND CHARACTERIZATION OF SUSTAINED RELEASE ACECLOFENAC MATRIX TABLETS CONTAINING TAMARIND SEED POLYSACCHARIDE
BY
BASAVARAJ
M. Pharm., PART-I
DEPARTMENT OF PHARMACEUTICS
UNDER THE GUIDANCE OF
Mr. B. SOMESHWARA RAO. M. Pharm.
ASSOCIATE PROFESSOR
DEPARTMENT OF PHARMACEUTICS
INSTITUTION
SREE SIDDAGANGA COLLEGE OF PHARMACY
B. H. ROAD, TUMKUR-572 102
KARNATAKA
RAJIV GANDHI UNIVERSITY OF HEALTH SCIENCES, KARNATAKA, BANGALORE.
ANNEXURE-II
PROFORMA FOR REGISTRATION OF SUBJECTS FOR DISSERTATION
1. / NAME OF THE CANDIDATEAND ADDRESS / Mr. BASAVARAJ
S/O PRABHAKAR
AT & POST - MATALA
TALUKA - BASAVA KALYAN
DIST. - BIDAR
PIN - 585 419
STATE – KARNATAKA.
2. / NAME OF THE INSTITUTION / SREE SIDDAGANGA COLLEGE OF PHARMACY
B. H. ROAD, TUMKUR- 572 102,
KARNATAKA.
3. / COURSE OF STUDY AND SUBJECT / MASTER OF PHARMACY IN PHARMACEUTICS.
4. / DATE OF ADMISSION / 23-05- 2009.
5. TITLE OF THE TOPIC
“DESIGN AND CHARACTERIZATION OF SUSTAINED RELEASE ACECLOFENAC MATRIX TABLETS CONTAINING TAMARIND SEED POLYSACCHARIDE”
6.0 / BRIEF REVIEW OF THE INTENDED WORK
6.1- Need for the study
Oral route is the most preferred route for administration of drugs. Tablets are the most popular oral formulation available in the market and preferred by the patients and physicians alike. In long term therapy for the treatment of chronic disease conditions, Conventional formulations are required to be administered in multiple doses and therefore have several disadvantages1.
The primary benefit of a sustained release dosage form compared to a conventional dosage form is the uniform drug plasma concentration and therefore uniform therapeutic effect. Over the past two decades, sustained release dosage forms have made significant progress in terms of clinical efficacy and patient compliance. Matrix devices due to their chemical inertness, drug embedding ability and drug release character have gained steady popularity for sustaining the release of a drug2.
Hydrophilic matrices are interesting option when developing an oral sustained release formulation. The drug release from such matrices can be controlled through their physical properties. Polysaccharides are the choice of materials among the hydrophilic polymers used, because they are nontoxic and acceptable by the regulating authorities. The various polysaccharides used in drug delivery applications are cellulose ethers, xanthan gum, locust bean gum and guar gum. Another natural polysaccharide Tamarind seed polysaccharide (TSP) obtained from the seed kernel of Tamarindus indica, possesses properties like high viscosity, broad pH tolerance, noncarcinogenicity, mucoadhesive nature, and biocompatibility. It is used as stabilizer, thickener, gelling agent, and binder in food and pharmaceutical industries. The tamarind seed polysaccharide constitutes about 65% of the tamarind seed components3.
Aceclofenac is a non-steroidal anti-inflammatory drug used extensively in the treatment of rheumatoid arthritis, osteoarthritis and ankylosing spondylitis. Aceclofenac is one of the emerging NSAID molecules. Aceclofenac is a newer derivative of diclofenac and has less GIT complications, short biological half-life of 4 hours and dosing frequency
More than one per day make acelofenac an ideal candidate for modified release multiple unit preparation to reduce the frequency of administrations and to improve patient compliances, aceclofenac is suitable for making sustain release dosage form4.
The aim of the present study is to design and characterize sustained release matrix tablet of aceclofenac containing tamarind seed polysaccharide and to study their release kinetics in comparison with the marketed sustained release tablets.
6.2 - Review of Literature
1. Study of release behaviour of drugs from TSP tablets with water soluble and insoluble model drugs such as acetoaminophen, caffeine, theophylline, salicylic acid and indomethacin.They concluded that the mechanism of release of soluble drugs was found to be anomalous. Zero order release can be achieved taking sparingly soluble drug like indomethacin from TSP. For water soluble drugs, the release amount can also be controlled by partially cross linking the matrix. The extent of release can be varied by controlling the degree of cross linking5.
2. Development and evaluation of xyloglucan matrix tablets containing naproxen by using xyloglucan (XGL), hydroxyproplymethylcellulose (HPMC), cellulose acetate phthalate (CAP) and ethyl cellulose (EC) were prepared by conventional wet granulation technique and concluded that, the tablets containing XGL in combination with CAP had released 98.08% drug and release was extended over a period of 10 hours of dissolution study, hence it is a good combination for the controlled release of drugs6.
3. Evaluation of TSP as a mucoadhesive and sustained release component of nifedipine mucoadhesive tablet in comparison with HPMC and sodium corboxymethylcellulose. Best mucoadhesive performance and in vitro drug release profile were exhibited by the tablet containing carbopol and TSP in the ratio of 1:1. This formulation was more comfortable to the user due toless erosion, faster hydration rate, and optimum pH of surrounding medium7.
4. Formulation of sustained release matrix tablets of tramadol HCl using natural gums such as xanthan and guar gum by direct compression method. Guar gum alone could not efficiently control the drug while xanthan gum and all combinations of natural gums
with HPMC could retard tramadol HCl release. Tablets with only xanthan gum had the highest mean dissolution time and released the drug following a zero order model via swelling, diffusion and erosion mechanisms8.
5. Xanthan gum based sustained release matrix tablets of diclofenac sodium by using xanthan gum, polyethylene glycol (PEG 6000) and concluded that xanthan gum can be used as an effective matrix former, to retard the release of diclofenac sodium for extended period of time9.
6. Formulation and in vitro evalution of sustained release matrix tablets of metoprolol succinate by using ethanolic solution of EC and polyvinylpyrollidine were used as a granulating agent along with hydrophyllic matrix materials like HPMC, gaur gum and concluded that the hydrophyllic matrix of HPMC alone could not control the metoprolol succinate effectively for 16 hours. It is evident from the result that matrix tablet prepared with HPMC and granulating agent of EC (4%w/v) is better system for once daily sustained release of highly water soluble drug like metoprolol succinate10.
7. Formulation of sustained release lithium carbonate (LC) matrix tablets: influence of hydrophyllic materials by using different ratios of polymers including carbopol (CP), sodium carboxy methylcellulose and HPMC concluded that release of lithium carbonate from all formulated sustained release matrix tablets were generally sustained. Sodium CMC, CP and HPMC can therefore, be used to modify release rates of lithium carbonate in hydrophilic matrix tablets11.
8. In vitro release characteristics of matrix tablets study of karaya gum and guar gum as release modulators. Tablets were evaluated for physical characteristics like hardness, weight variation, friability, swelling index and drug content. The effect of water soluble
(lactose) and water insoluble (dicalcium phosphate ) excipients on drug release was evaluated. Incorporation of lactose or dicalcium phosphate influenced drug release, but at lower levels only. A combination of karaya gum and guar gum exhibited more sustained release than individual gum12.
9. Formulation and evaluation of tamulosoin hydrochloride as a sustained release matrix tablets by using HPMC K 100M, HPC K 15M, HPMC K 100-LV, EC. Tablets were prepared by direct compression method and wet granulation method. The in vitro release of the trial batch XII complies with the tolerance limit and matches with a
reputed sustained release product in the market. The evaluation for drug release kinetics reveals that the drug release from the tablet follows first-order kinetics. The stability study of the tablets of trial batch XII revealed that it was stable at the end of 1st month at 40°C/75% RH 13.
10. Formulation and optimization of directly compressible isoniazid modified release matrix tablet using low viscosity grade hydroxymethylcellulose (HMC) and medium viscosity grade HMC and high viscosity grade HPMC, matrix tablets were prepared by direct compression. The results of this investigation enabled to fabricate hydrophilic matrices containing isoniazid. It was also demonstrated that the release of isoniazid from directly compresed matrix tablets could be modified by changing the type and amount of polymer in the matrix tablets14.
6.3 - Objective of the Study
Following are the objectives of the present study
1. To carry out preformulation studies for possible drug polymer interaction.
2. To develop analytical method for the estimation of the drug in formulation.
3. To develop and formulate sustained release matrix tablets of aceclofenac.
4. To carry out short term stability studies on the most satisfactory formulation.
7.0 / MATERIALS AND METHODS
Material:
Drug: Aceclofenac.
Polymers: Tamarind seed polysaccharide, Guar gum, HPMC etc.
Excipients: Lactose, Avicel pH101, Starch, Magnesium stearate and Talc.
Methods:
Development of sustained release matrix tablets by wet granulation method/ by suitable method.
7.1 - Source of Data
Review of Literature from
a) Journals such as,
1) Indian Journal of Pharmaceutical Sciences
2) International Journal of Pharmaceuticals
3) Brazilian Journal of Pharmaceutical Sciences
4) Asian journal of pharmaceutics
5) Journal of pharmacy pharmaceutical sciences
b) AAPS Pharmaceutical Science and Technology
c) World Wide Web
d) J-gate@Helinet
e) Library: Sree Siddaganga College of Pharmacy
f) E-library: Sree Siddaganga College of Pharmacy
7.2 - Method of collection of data
1) Pre-formulation studies for possible drug/polymer interaction by IR/DSC analysis.
2) Preparation of the sustained release matrix tablets by wet granulation process/ by suitable method.
3) Evaluation of the various properties of sustained release matrix tablets:
Physical properties:
a) Evaluation of granules:
a) Angle of repose
b) Bulk density
c) Compressibility index
d) Total porosity
b) Evaluation of tablets:
a) Thickness
b) Weight variation test
c) Drug content
d) Hardness & friability
4) Drug in-vitro release studies by using suitable in-vitro model.
5) To carry out short term stability studies on the most satisfactory formulation.
/ 7.3 - Dose the study require any investigation or investigation to be conducted on patients or other humans or animals?
“ NOT APPLICABLE”
7.4 - Has ethical clearance been obtained from your institution in case of 7.3?
“ NOT APPLICABLE ”
8.0 / REFERENCES
1. Ravi PR, Ganga S, Saha RN. Design and study of lamivudine oral controlled release tablets. AAPS PharmSciTech 2007;8(4):1-9.
2. Basak SC, Kumar KS, Ramalingam M. Design and release characteristics of sustained release tablet containing metformin HCl. Brazilian J Pharm Sci 2008;44(3):477-82.
3. Deveswaran R, Abraham S, Bharath S, Basavaraj BV, Furtado S, Madhavan V. Design and characterization of diclofenac sodium tablets containing tamarind seed polysaccharide as release retardant. Int J Pharm Tech Res 2009;1(2):191-5.
4. Trivedi P, Verma AML, Garud N. Preparation and characterization of aceclofenac microspheres. Asian J Phrmaceutics 2008;2(2):110-5.
5. Sumathi S, Ray AR. Release behaviour of drugs from tamarind seed polysaccharide tablets. J Pharm pharmaceut Sci 2002;5(1):12-8.
6. Kulkarni RV, Shah A, Boppana R. Development and evaluation of xyloglucan matrix tablets containing naproxen. Asian J of pharmaceutics 2008;2(2):102-5.
7. Patel B, Patel P, Bhosale A, Hardikar S, Mutha S, Chaulang G. Evaluation of tamarind seed polysaccharide as a mucoadhesive and sustained release component of nifedipine buccoadhesive tablet and comparison with HPMC and Na CMC. Int J Pharm Tech Res 2009;1(3):404-10.
8. Varshosaz J, Tavakoli N, Kheirolahi F. Use of hydrophilic natural gums in formulation of sustain release matrix tablets of tramadol hydrochloride. AAPS PharmSciTech 2006;7(1):1-7.
9. Yeole PG, Galgatte UC, Babla IB, Nakhat PD. Design and evaluation of xanthan gum based sustained release matrix tablets of diclofenac sodium. Indian J Pharm Sci
2006;68(2):185-9.
10. Jha AK, Bhattacharya A, Verma P. Formulation and in vitro evaluation of sustained release matrix tablets of metoprolol succinate using hydrophilic polymers. Int J Pharm Tech Res 2009;1(4):972-7.
11. Emami J, Tavakoli N, Movahedian A. Formulation of sustained-release lithium carbonate matrix tablets: influence of hydrophilic materials on the release rate and in vitro-in vivo evaluation. J Pharm Pharmaceut Sci 2004;7(3):338-44.
12. Senapati MK, Srinatha A, Pandit JK. In vitro release characteristics of matrix tablets study of karaya gum and guar gum as release modulators. Indian J Pharm Sci 2006;68(6):824-6.
13. Nithiyananthan TS, Shankarananth V, Rajasekhar KK, Hareesh G. Formulation and evaluation of tamulosoin hydrochloride as a sustained release matrix tablet. Int J Chemtech Res 2009;1(4):1278-90.
14. Gohel MC, Parikh RK, Padshala MN, Sarvaiya KG, Jena DG. Formulation and optimization of directly compressible isoniazid modified release matrix tablet. Indian J Pharm Sci 2007;69(5):640-5.
9.0 /
SIGNATURE OF THE CANDIDATE
10 / REMARKS OF THE GUIDE / Recommended
11 / NAME AND DESIGNATION OF
11.1 Guide / Mr. B. SOMESHWARA RAO, M.Pharm.
Associate professor
Department of pharmaceutics
11.2 Signature
11.3 Co-Guide ( If any) / ------
11.4 Signature / ------
11.5 Head of the Department / Dr. SURESH V. KULAKARNI, M. Pharm., Ph. D.
Professor & Head
Department of Pharmaceutics
11.6 Signature
12 / 12.1 Remarks of the Chairman
Principal / Forwarded to the University for approval
12.2 Signature
/
(Dr.S.BADAMI)
PrincipalSree Siddaganga College of Pharmacy
B. H. Road, Tumkur-572 102.
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