EFFECT OF MICROSPHERONIZATION ON THE RELEASE AND ULCEROGENIC ACTIVITY OF SULINDAC | ||||
| Bulletin of Pharmaceutical Sciences Assiut University | ||||
| Article 7, Volume 21, Issue 2, December 1998, Page 161-170 PDF (513.81 K) | ||||
| Document Type: Original Article | ||||
| DOI: 10.21608/bfsa.1998.67981 | ||||
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| Author | ||||
| A. Abd-Elmageed | ||||
| Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt | ||||
| Abstract | ||||
| Sulindac (SUL) NSAIDS has irritation and ulcerogenic activity on the human stomach. Sulindac microspheres were prepared adopting the solvent evaporation method, using cellulose acetate butyrate as coating polymer with 1-2 drug : polymer ratio. The influence of microsphere particle size and pH of the dissolution medium on the release profile of the drug was investigated. In all cases the drug release mechanism followed Higuchi diffusion model with sustained release profile of sulindac from SUL-CAB microspheres. The smaller particle size gave significantly higher release rate of the drug. The release rate was slower in acidic medium (pH 1.2) than that at pH 7.4. The effect of microspheronization on the ulcerogenic activity of the drug in the stomach of rabbits was studied. It was observed that the ulcerogenic activity of the drug was disappeared and the mucosal surfaces showed free of hemorrhage and inflammations when the drug is used as microspheres. | ||||
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