阿折地平固体分散体的制备及溶出度的考察(1)
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[摘要] 目的 利用固体分散技术制备阿折地平固体分散体，并检测其体外溶出度。 方法 分别以聚乙二醇4000、聚乙二醇6000、泊洛沙姆188等为载体，用熔融法、溶剂法制备不同比例的阿折地平固体分散体。通过X射线粉末衍射法分析药物在固体分散体中的存在状态。采用紫外分光光度法测定阿折地平固体分散体的溶出度，根据测定结果筛选出两种方法制备的固体分散体进行压片，并比较阿折地平固体分散片的体外溶出特性。 结果 各种方法制备的阿折地平固体分散体均能加快药物溶出，且载体比例愈大，药物溶出越快。最优制备方法为以泊洛沙姆188为载体、药物与载体比例为1∶6，采用熔融法制备。 结论 采用固体分散技术可有效增加阿折地平的体外溶出度。
[关键词] 阿折地平；固体分散体；溶出度
[中图分类号] R971.9 [文献标识码] A [文章编号] 1673-7210(2012)08(c)-0118-03
Investigation on preparation and dissolution of Azelnidipine Solid Dispersions
WANG Yue1 LIU Huan2 WANG Chenggang2 WANG Xinglin2
1.Tianjin University of Traditional Chinese Medicine, Tianjin 300193, China; 2.Tianjin Institute of Pharmaceutical Research Tianjin State Key Laboratory of Drug Delivery Technology and Pharmacokinetics, Tianjin 300193, China
[Abstract] Objective To prepare Azelnidipine Solid Dispersions by the technology of solid dispersion and determine the dissolution of Azelnidipine. Methods Azelnidipine Solid Dispersions were prepared with different proportion by melting method and solvent method which used PEG 4000, PEG 6000, Poloxamer 188 as carriers. The distribution condition by using X-ray diffraction was analyzed. The dissolution of the solid dispersions was detected by UV spectrophotometry, solid dispersions were to be pieces according to the measuring results of the two methods, and the characteristics of dissolution of solid dispersions in vitro were compared. Results The dissolution was significantly improved by Azelnidipine Solid Dispersions with every method in vitro, and the higher carrier of Azelnidipine ratio, the faster drug dissoluted. Using the Poloxamer 188 as the carrier, the ratio of Azelnidipine and carrier of 1∶6, and utilizing fusion method was the best preparation method ......
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