长春西汀固体分散体的制备及体外溶出特性

目的:制备长春西汀固体分散体,提高其溶出速度和程度。方法:以泊洛沙姆188(F68)为载体,用溶剂-熔融法制备固体分散体;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;并考察载体的用量、溶出介质和转速对药物体外溶出特性的影响。结果:长春西汀的固体分散体中药物部分以分子状态分散,部分以微晶分散。固体分散体VIN-F68(1∶6,w/w)的溶出参数t50t、d与相应物理混合物、原料药粉末和市售片剂间差异存在显著性(P<0.01),溶出介质和转速的选择对药物的溶出有一定影响。结论:长春西汀的固体分散体能显著提高药物的溶出速度和程度。

Study on the preparation and in vitro evaluation of vinpocetine solid dispersion

OBJECTIVE To prepare vinpocetine solid dispersion and improve the dissolution of vinpocetine.METHODS Vinpocetine solid dispersion was prepared with poloxamer188(F68) as carrier by solvent-melting methods.Differential thermal analysis and powder X-ray diffraction were used to determine the status of drug in carriers,the dissolution characteristics in vitro and the effects of carrier ratios,different dissolution media and rotational speeds for dissolution tests were studied.RESULTS Drug in vinpocetine solid dispersion partly existed as molecule and partly as fine crystal.The parameters of t_(50)and t_(d)of vinpocetine solid dispersion were greatly reduced,compared with vinpocetine physical mixture,drug substance and marketed tablets.The dissolution of drug was inflenced by differenr dissolution media and rotational speeds.CONCLUSION VIN-F68 solid dispersion can improve the dissolution of vinpocetine.