靖博宇,王志远,李燕,孙进,何仲贵
JING Bo-yu,WANG Zhi-yuan,LI-Yan,SUN-Jin,HE Zhong-gui(School of Pharmacy

• 1:沈阳药科大学药学院

摘要(Abstract)：

目的应用固体分散技术,提高非洛地平的体外溶出度。方法以PVPK30、Lutrol F68、Tween80(与吸附剂,如PVPP)为载体,分别采用溶剂法、熔融法、溶剂蒸发-沉积等技术制备非洛地平固体分散体,考察不同载体对固体分散体溶出度的影响。并着重考察以Tween 80为增溶剂,不同种类吸附剂为载体对固体分散体外观、溶出度的影响。应用差示热分析和X射线衍射鉴别药物在载体中的存在状态。结果采用不同载体和方法制备的非洛地平固体分散体均能明显促进药物的溶出,溶出速度依次为Tween 80>Lutrol F68>PVPk30。其中m(药物)∶m(Tween 80)∶m(PVPP)=1∶4∶5时,溶出速度最快,1 h累积释放率达90%以上。差示热分析固体分散体中药物吸热峰前移或消失,X射线衍射固体分散体中药物的结晶衍射峰消失,推测药物在载体中以无定形或分子形式存在。结论制备非洛地平固体分散体可以提高其体外溶出度,尤其是含有表面活性剂的固体分散体可进一步提高药物的溶出。
Objective To improve the solubility and dissolution of felodipine by preparing its solid dispersions.Methods PVPk30,Lutrol F68 and Tween 80(with absorbent,such as crospovidone)were used as carriers to prepare the solid dispersions of felodipine by the methods of solvent,melt and solvent evaporation-deposition.When Tween80 was applied as solubilizer,the effect of different absorbents on the appearance and dissolution of solid dispersions were the focus of study.The state of felodipine in carriers was identified by DSC.Results The dissolution rate test demonstrated that all the solid dispersions could improve the dissolution rate of felodipine and the sequence was that:Tween 80>Lutrol F68>PVPk30.Among of this,when weight ratio of felodipine,Tween 80 and PVPP was 1∶4∶5,the dissolution rate was the most fast and the accumulative release rate was up to more than 90% in 1 h.The results of differential scanning calorimetry(DSC) indicated that the drug was in the amorphous state.Conclusions Surfactant is useful in preparing felodipine solid dispersion and significantly improves the dissolution rate of felodipine.

关键词(KeyWords)： 非洛地平;固体分散体;表面活性剂;溶出度;差示扫描量热法
felodipine;solid dispersion;surfactant;dissolution;differential scanning calorimetry(DSC)

Abstract:

Keywords:

基金项目(Foundation): 973国家重大科学研究计划(2009CB930300)

作者(Author): 靖博宇,王志远,李燕,孙进,何仲贵
JING Bo-yu,WANG Zhi-yuan,LI-Yan,SUN-Jin,HE Zhong-gui(School of Pharmacy

DOI: 10.14066/j.cnki.cn21-1349/r.2010.03.013

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