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布阿加呋喃固体分散体的制备及体外研究

[Preparation and in vitro study of buagafuran solid dispersions].

作者信息

Xia Xue-Jun, Tao Zhong-Hua, Ren Yi, Wang Ren-Yun, Liu Yu-Ling

机构信息

Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing 100050, China.

出版信息

Yao Xue Xue Bao. 2008 May;43(5):548-52.

Abstract

Solid dispersions technique was used to solidify buagafuran and improve buagafuran in vitro dissolution and stability. Buagafuran solid dispersions were prepared separately using PVPK30, PEG6000 and Poloxamer188 at various weight ratios as carriers. The status of buagafuran in solid dispersions was determined by using DSC and IR. The solubility, content and in vitro dissolution of pure drug and the solid dispersions were detected by using HPLC. When buagafuran/carrier was 1:5 or less, the drug existed in a solid dispersion form. Three kinds of carriers all can improve buagafuran dispersibility and in vitro dissolution. Accelerating experiment showed that buagafuran/PVPK30 < or = 1:10 solid dispersions was ageing-resistant, and the aspect, content and in vitro dissolution did not change after storaged over 3 months, but PEG6000, Poloxamer188 and a lower ratio PVPK30 solid dispersions became aged. Buagafuran/PVPK30 < or = 1:10 solid dispersions can be developed as buagafuran oral drug delivery carrier.

摘要

采用固体分散技术固化布地奈德,提高其体外溶出度和稳定性。分别以不同重量比的聚乙烯吡咯烷酮K30(PVPK30)、聚乙二醇6000(PEG6000)和泊洛沙姆188(Poloxamer188)为载体,制备布地奈德固体分散体。采用差示扫描量热法(DSC)和红外光谱法(IR)确定布地奈德在固体分散体中的状态。用高效液相色谱法(HPLC)检测纯药物及固体分散体的溶解度、含量和体外溶出度。当布地奈德与载体比例为1:5或更低时,药物以固体分散体形式存在。三种载体均能提高布地奈德的分散性和体外溶出度。加速试验表明,布地奈德/PVPK30≤1:10的固体分散体具有抗老化性,储存3个月以上后外观、含量和体外溶出度均未改变,但PEG6000、Poloxamer188及较低比例PVPK30的固体分散体发生老化。布地奈德/PVPK30≤1:10的固体分散体可开发为布地奈德口服给药载体。

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