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水飞蓟宾固体分散体的制备及体外溶出研究
http://www.100md.com 《第二军医大学学报》2000年第10期
水飞蓟宾|固体分散体|泊洛沙姆188|体外溶出度
     作者:邓莉 邹豪 蒋雪涛

    单位:邓莉(第二军医大学药学院药剂学教研室,上海 200433);邹豪(第二军医大学药学院药剂学教研室,上海 200433);蒋雪涛(第二军医大学药学院药剂学教研室,上海 200433)

    关键词:水飞蓟宾;固体分散体;泊洛沙姆188;体外溶出度

    第二军医大学学报001019 [摘要] 目的:制备了水飞蓟宾的固体分 散体,并检测其体外溶解度及溶出速度。方法:选择尿素、聚乙烯吡 咯烷酮(PVP)、泊洛沙姆188等3种载体,用熔融法和共沉淀法制备水飞蓟宾固体分散体,并 进行差热分析、X-射线粉末衍射分析以鉴别药物在载体中的存在状态,最后进行了体外溶 出研究。结果:水飞蓟宾在PVP中以无定型存在,在泊洛沙姆188中以 微细结晶存在,在尿素中大部分仍以晶体形式存在,少量以分子状态存在。溶出研究结果表 明泊洛沙姆188载体的水飞蓟宾固体分散体的溶解度最大,溶出速度最快。结论: 泊洛沙姆是提高水飞蓟宾溶解度及溶出速度的理想载体。

    [中图分类号] R 283.6 [文献标识码] A

    [文章编号] 0258-879X(2000)10-0961-04

    Preparation and evaluation of silibinin solid dispersions in vitro

    DENG Li, ZOU Hao, JIANG Xue-Tao

    (Department of Pharmaceutics, College of Pharm acy, Second Military Medical University, Shanghai 200433, China)

    [ABSTRACT]Objective: To prepare silibinin solid dispersion a nd measure its dissolution in vitro.Methods: Silibinin solid dispersions were obtained with urea, PVP and poloxamer188 as carriers by meltin g and coevaporation methods. Differential thermal analysis and powder X-ray dif fraction were used to determine the status of drug in carriers, and the dissolut ion characteristics in vitro were studied in simulated gastric juice. Results: In PVP- silibinin solid dispersions drug was amorphous; in p oloxamer188-silibinin solid dispersions, drug existed as fine crystal, while in urea-silibinin solid dispersions most of silibinin existed as crystal, only a little as molecule. Poloxamer188 was the better carrier in improving the solutio n and dissolution rate of the drug. Conclusion: Poloxamer188 is a very useful carrier in improving the solubility and dissolution of silibinin. ......

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