Hashem Fahima M, Mostafa Mohamed, Shaker Mahmoud, Nasr Mohamed
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Helwan University, Cairo 11790, Egypt.
Department of Pharmaceutics, Faculty of Pharmacy, Suez Canal University, Ismailia 41522, Egypt.
J Pharm (Cairo). 2013;2013:629593. doi: 10.1155/2013/629593. Epub 2012 Dec 6.
The objective of this study was to evaluate the influence of oxatomide β-cyclodextrin inclusion complex on the physicochemical properties and bioavailability of the drug. Oxatomide β-cyclodextrin solid complex was prepared with equimolar ratio of both oxatomide and β-cyclodextrin in presence or absence of water soluble polymers using different techniques. The coevaporated complex prepared in presence of PVP-K15 showed a prompt drug release and significantly increased % dissolution efficiency (P < 0.05) compared to the pure oxatomide. Moreover, the results of bioavailability evaluation of this complex in rabbits compared to commercial drug product indicated a 73.15% increase in the oral bioavailability of oxatomide. In conclusion, inclusion complex of oxatomide with β-cyclodextrin prepared by coevaporation in presence of PVP-K15 not only results in an enhancement of the oxatomide dissolution rate but also improves the bioavailability of oxatomide.
本研究的目的是评估奥沙米特β-环糊精包合物对药物理化性质和生物利用度的影响。采用不同技术,在有无水溶性聚合物存在的情况下,以等摩尔比的奥沙米特和β-环糊精制备了奥沙米特β-环糊精固体复合物。与纯奥沙米特相比,在PVP-K15存在下制备的共蒸发复合物显示出药物快速释放,且溶出效率百分比显著提高(P < 0.05)。此外,该复合物在兔体内的生物利用度评估结果与市售药品相比表明,奥沙米特的口服生物利用度提高了73.15%。总之,在PVP-K15存在下通过共蒸发制备的奥沙米特与β-环糊精包合物不仅提高了奥沙米特的溶出速率,还改善了奥沙米特的生物利用度。