盐酸舍曲林固体分散体的制备及体外溶出度研究  

Preparation and in vitro dissolution of Sertraline hydrochloride solid dispersion

作　　者：郑碧莹 张佳欢 石森林[1] 吴素香[1] ZHENG Biyin;ZHANG Jiahuan;SHI Senlin;WU Suxiang(College of Pharmaceutical Science,Zhejiang Chinese Medical University,Hangzhou,Zhejiang,311402 P.R.China)

机构地区：[1]浙江中医药大学药学院,浙江杭州311402

出　　处：《华西药学杂志》2020年第6期604-607,共4页West China Journal of Pharmaceutical Sciences

摘　　要：目的制备盐酸舍曲林固体分散体,并评价其体外溶出度。方法分别以泊洛沙姆188(p188)、聚乙烯吡咯烷酮K30(PVPK30)、聚乙二醇6000(PEG6000)为载体,用溶剂法制备固体分散体,考察载体种类、药物-载体比例以及不同溶出介质对盐酸舍曲林溶出的影响。结果以p188为载体,药载比为1:2,制备的固体分散体溶出速率最佳,5 min累积溶出度达90%,显著高于原料药和物理混合物(药物-载体)。结论固体分散体技术可以显著提高盐酸舍曲林的溶出速率。在p188、PVPK30、PEG6000载体中,p188对盐酸舍曲林溶出度的改善效果最佳,适合作为盐酸舍曲林固体分散体的载体。OBJECTIVE To prepare Sertraline hydrochloride solid dispersion(SHSD)for increasing the dissolution rate of Sertraline hydrochloride(SH).METHODS The solid dispersions were prepared by solvent method with poloxamer 188(p188),povidone K30(PVPK30)and polyethylene glycol 6000(PEG6000)as carriers.The effects of carrier type,drug-carrier ratio and different dissolution media on the dissolution of SH were investigated.RESULTS With poloxamer188 as the carrier,the drug loading ratio was 1:2,and the solid dispersion prepared had the best dissolution rate.The solid dispersion prepared with p188,in which the mass ratio of the sertraline hydrochloride and p188 was 1:2,exhibited optimal dissolution.The cumulative dissolution rate reached 90%within 5 minutes which was significantly higher than the rate of drug substance and physical mixture(drug-carrier).CONCLUSION Solid dispersion technology can significantly increase the dissolution rate of SH.P188,PVPK30 and PEG6000 all can improve the dissolution of SH,and p188 is especially suitable as a carrier for a SHSD.

关 键 词：盐酸舍曲林 固体分散体 泊洛沙姆188 聚乙烯吡咯烷酮K30 聚乙二醇6000 溶剂法 差示扫描量热法 粉末X-射线衍射分析 体外溶出度 

分 类 号：R94[医药卫生—药剂学]