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In VitroandIn VivoEvaluation of Oxatomideβ-Cyclodextrin Inclusion Complex

机译:Oxatomideβ-环糊精包合物的体外和体内评价

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The objective of this study was to evaluate the influence of oxatomideβ-cyclodextrin inclusion complex on the physicochemical properties and bioavailability of the drug. Oxatomideβ-cyclodextrin solid complex was prepared with equimolar ratio of both oxatomide andβ-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 withβ-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.
机译:这项研究的目的是评估oxatomideβ-环糊精包合物对药物的理化性质和生物利用度的影响。使用不同的技术,在存在或不存在水溶性聚合物的情况下,以等摩尔比的草酸酯和β-环糊精制备草酸酯-β-环糊精固体复合物。与纯草酮相比,在PVP-K15存在下制备的共蒸发复合物显示出快速的药物释放和%溶解效率的显着提高(P <0.05)。此外,与市售药品相比,该复合物在兔子中的生物利用度评估结果表明,草履虫的口服生物利用度增加了73.15%。综上所述,在PVP-K15存在下,共蒸发制得的草酮与β-环糊精的包合物,不仅增加了草酸酯的溶出度,而且提高了草酸酯的生物利用度。

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