DESIGN AND EVALUATION OF COLON TARGETED DOSAGE FORM CONTAINING MESALAZINE USING PH DEPENDENT POLYMERS
Abstract
Colonic drug delivery has gained importance not just for the delivery of the drugs for the treatment of local diseases associated with the colon like Crohn’s disease, ulcerative colitis and irritable bowel syndrome but also for the potential it holds for the systemic delivery of proteins and therapeutic peptides. The aim of the study was to develop colon targeted tablets of Mesalazine by wet granulation method using 33 response surface method with design of experiment software and HPMC K4M, Eudragit RL100, Ethyl cellulose and PVP K-30 used as pH dependent polymers. All the formulations (F1 to F27) were evaluated for the physicochemical parameters and were subjected to in vitro drug release studies. The amount of Mesalazine released from tablets at different time intervals was estimated by UV spectrophotometer. The formulation F26 released 98.16% of Mesalazine after 24 h. The results of the study showed that formulation F26 is the best formulation based on the evaluation parameters which provides targeting of Mesalazine for local action in the colon owing to its minimal release of the drug in the first 4 h. The pH dependent tablet system is a promising vehicle for preventing rapid hydrolysis in gastric environment and improving oral bioavailability of Mesalazine for the treatment of disease at colon region.
Keywords:
Mesalazine, Colon specific, Eudragit RL 100, pH dependent polymers.DOI
https://doi.org/10.25004/IJPSDR.2017.090604References
2. Aurora J, Talwar N, Pathak V. Colonic drug delivery challenges and opportunities an overview. European Gastroenterology Review. 2006; 1-6.
3. Nugent SG, Kumar D, Rampton DS, Evans DF. Intestinal luminal pH in inflammatory bowel disease: possible determinants and implications for therapy with aminosalicylates and other drugs. Journal of Gastroenterology. 2001; 48(4): 571–577.
4. Ewe K, Schwartz S, Petersen S, Andreas G. Inflammation does not decrease Intraluminal pH in Chronic Inflammatory Bowel Disease. Digestive Diseases and Sciences. 1999; 44 (7): 1434-1439.
5. Patel P, Roy AK. Formulation and evaluation of colon targeted tablets of Ornidazole for the treatment of amoebiasis. International journal of drug delivery & research. 2011; 3(1): 52-61.
6. Montgomery, Douglas C. Design and Analysis of Experiments: Response surface method and designs, John Wiley and Sons, Inc. New Jersey. 2005, pp. 210-256.
7. Schwartz BJ, Connor RE, Optimization technique in pharmaceutical formulations and processing. J Drugs Pharm Sci Modern Pharm. 1996; 72:727-54.
8. Nair R, Sevukarajan M, Vishnu Priya K, Arun Kumar KS. Response Surface Methodology for the Optimization of Ethylcellulose Microspheres. International Journal of PharmTech Research. 2011; 3(2): 775-783.
9. Asghar LF, Chandran S. Design and evaluation of matrices of Eudragit with polycarbophil and carbopol for colon-specific delivery. Journal of Drug Targeting. 2008; 16(10): 741-57.
10. Yehia SA, Elshafeey AH. Optimization of budesonide compression-coated tablets for colonic delivery. AAPS pharmaceutical Sciences and Technology. 2009; 10(1): 147-156.
11. Nykanen P, Kragars K, Sakkinen M. Organic acids as excipients in matrix granules for colon-specific drug delivery. International Journal of Pharmaceutics. 1999; 184: 251-261.
12. Małgorzata W, Marcin Z, Aleksandra A. Tasting cetirizine-based microspheres with an electronic tongue. Sensors and Actuators B Chemical. 2016; 238: 1190-1198.
13. Harris SM, Jaweria T, Merchant HA, Yousuf RI. Evaluation of Drug Release Kinetics from Ibuprofen Matrix Tablets Using HPMC. Pakistan Journal of Pharmaceutical Sciences. 2006; 19(2): 119-124.
14. Dash S, Murthy PN, Nath L, Chowdhary P. Kinetic modeling on drug release from controlled drug delivery systems. Acta Poloniae Pharmaceutical. Drug research. 2010; 67(3):217-23.
15. Bayomi MA. Geometric approach for zero-order release of drugs dispersed in an inert matrix. Pharm Res. 1994; 11: 914-916.
16. Janssen M, Timur UT, Woike N. Celecoxib-loaded PEA microspheres as an auto regulatory drug-delivery system after intra-articular injection. Journal of Controlled Release. 2016; 244: 30-40.
17. Tyagi LK, Kori ML. Stability Study and In-vivo Evaluation of Lornoxicam Loaded Ethyl Cellulose Microspheres. International Journal of Pharmaceutical Sciences and Drug Research. 2014; 6(1): 26-30.
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