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黄秋葵胶和海藻酸钠的聚合物微球用于奥卡西平的控制释放:体外和体内评价。

Polymeric microspheres of okra mucilage and alginate for the controlled release of oxcarbazepine: In vitro &in vivo evaluation.

机构信息

Faculty of Pharmacy, University of Sargodha, Sargodha 40100, Pakistan.

Faculty of Pharmacy, University of Sargodha, Sargodha 40100, Pakistan.

出版信息

Int J Biol Macromol. 2018 May;111:1156-1165. doi: 10.1016/j.ijbiomac.2018.01.058. Epub 2018 Jan 12.

Abstract

Oxcarbazepine-loaded alginate/okra pods mucilage microspheres were prepared through inotropic gelation technique for the sustained release of oxcarbazepine. The drug encapsulating efficiency of these microspheres was found 76.22 ± 0.01% to 90.57 ± 0.02% and their average particle sizes were 496 μm ± 0.41 to 692 μm ± 0.22. These microspheres were characterized in terms of swelling capacity, FTIR, DSC and SEM analysis. The in vitro drug release from these microspheres was followed sustained release (Korsemeyer - Peppas model) pattern (R = 0.9552-0.9906) and value of n > 1 showed that drug released by anomalous (non-Fickian) diffusion. The in vivo studies showed that there were highly significant difference with p < 0.001 in the pharmacokinetic parameters (C t AUC K), when oxcarbazepine was formulated in form of polymeric microspheres as compared to pure drug.

摘要

载有奥卡西平的海藻酸钠/黄秋葵荚粘液微球通过向心凝胶化技术制备,用于奥卡西平的缓释。这些微球的药物包封效率为 76.22±0.01%至 90.57±0.02%,平均粒径为 496μm±0.41 至 692μm±0.22。这些微球在溶胀能力、FTIR、DSC 和 SEM 分析方面进行了表征。这些微球的体外药物释放遵循持续释放(Korsemeyer-Peppas 模型)模式(R=0.9552-0.9906),n 值大于 1 表明药物通过异常(非菲克)扩散释放。体内研究表明,与纯药物相比,奥卡西平制成聚合物微球后,药代动力学参数(C t AUC K)有高度显著差异(p<0.001)。

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