MODIFICATION OF THE RELEASE OF DIPYRIDAMOLE FROM CERTAIN POLYMERIC SYSTEMS | ||||
| Bulletin of Pharmaceutical Sciences Assiut University | ||||
| Article 3, Volume 27, Issue 1, June 2004, Page 19-24 PDF (479.58 K) | ||||
| Document Type: Original Article | ||||
| DOI: 10.21608/bfsa.2004.65386 | ||||
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| Authors | ||||
| Ahmed E. Aboutaleb; Ali A. Abdel-Rhaman; Mahrous Ahmed* ; Amany A. Abdel-Rheem | ||||
| Department of Industrial Pharmacy, Faculty of Pharmacy, Assiut University, Assiut, Egypt | ||||
| Abstract | ||||
| The objective of the present study is to modify the release of dipyridamole (DIP); which has a pH dependant solubility in order to overcome its irregular and incomplete absorption from the gastrointestinal tract. This was achieved by incorporation of a dissolution retarder such as cellulose acetate phthalate CAP and a dissolution enhancer such as cyclodextrins; (dimethyl beta cyclodextrin DM-βCD and hydroxypropyl betacyclodextrin HP-βCD). This was an effective mean of moderating the drastic dissolution behaviour of that basic drug at acidic pH. Coevaporates of DIP with DM-βCD and DIP with HP-βCD in 1:2 molar ratio were prepared, followed by coating of these coevaporates by an enteric polymer (cellulose acetate phthalate, CAP) in 1: 3 drug : polymer weight ratio. In vitro release study was performed for capsules containing the modified granules at pH values of 1.3, 5 and 6.8. It was found that the drug release from the modified granules was decreased in a simulated gastric fluid and was enhanced in a simulated intestinal fluid and reached up to 100%. This could be attributed to the protecting effect of CAP for the drug granules in the acidic medium, followed by dissolving of CAP coat in the intestinal fluids which lead the drug to be released easily from the granules. | ||||
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