PHARMACOKINETICS AND PHARMACODYNAMICS EVALUATION OF PREPARED ZINC ASPIRIN SUPPOSITORIES | ||||
Bulletin of Pharmaceutical Sciences Assiut University | ||||
Article 8, Volume 26, Issue 2, December 2003, Page 187-199 PDF (589.76 K) | ||||
Document Type: Original Article | ||||
DOI: 10.21608/bfsa.2003.65483 | ||||
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Authors | ||||
Fergany A. Mohamed1; Saida A. Aly2; Hamdy M. Abdel-Rahman3 | ||||
1Department of Pharmaceutics, Faculty of Pharmacy, Assiut University, Assiut, Egypt | ||||
2Department of Pharmacology, Faculty of Medicine, Assiut University, Assiut, Egypt | ||||
3Department of Pharmaceutical Medicinal Chemistry, Faculty of Pharmacy, Assiut University, Assiut Egypt | ||||
Abstract | ||||
In an attempt to reduce the gastrointestinal side effects of aspirin, zinc aspirin complex was prepared and formulated into suppositories. The prepared suppositories were evaluated invitro for their hardness, melting range, uniformity of weight and drug content and in-vivo drug release. The pharmacokinetic and pharmacodynamic properties of zinc aspirin were evaluated in comparison with that of aspirin and aspirin lysinate (aspegic) following rectal and oral administration in experimental animals. Blood samples were collected at different time intervals after adminstration of drugs under evaluation. Salicylic acid (main metabolite of aspirin) was determined in plasma by using high performance liquid chromatography (HPLC). The antiinflammatory activity was studied in albino rats using carrageenan oedema model; and the analgesic activity was studied using hot plate and writhing methods. The results revealed that following rectal administration, the bioavailability of zinc aspirin was significantly (P<0.05) greater than that of aspirin and aspirin Lysinate. The absolute bioavailabilities were 94, 88.89 and 83.63 for zinc aspirin; aspirin lysinate and aspirin respectively. The peak plasma concentration (Cmax) were 54.5188, 50.271.68 and 48.091.15 ugl-1 for zinc aspirin, aspirin lysinate and aspirin, respectively. There was significant difference in the tmax. The area under the plasma concentration-time curve (AUC) values were 148.932.79, 140.832.3 and 132.493.56 ug.h/ml for zinc aspirin, aspirin lysinate and aspirin, respectively. There were significant differences in the Cmax, tmax and AUC following oral administration. The anti-inflammatory and analgesic studies revealed that zinc aspirin administered rectally or orally was more effective as anti-inflammatory and analgesic. The invivo studies were correlated with the in-vitro release studies of aspirin from the prepared suppositories. Based on the obtained results, the authors recommend the possible use of zinc aspirin as a substitute of aspirin containing products. | ||||
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