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坎地沙坦固体分散体的制备及溶出度、稳定性研究
引用本文:王美荣,王利珍,林建英.坎地沙坦固体分散体的制备及溶出度、稳定性研究[J].中国现代应用药学,2011,28(7):654-658.
作者姓名:王美荣  王利珍  林建英
作者单位:太原理工大学化学化工学院制药工程系,太原 030024;太原理工大学化学化工学院制药工程系,太原 030024;太原理工大学化学化工学院制药工程系,太原 030024
摘    要:目的利用固体分散技术提高坎地沙坦的溶解性。方法以体外溶出度为指标,通过单因素试验,考察处方和工艺因素对坎地沙坦固体分散体中药物溶出的影响,运用正交试验选定坎地沙坦固体分散体的最优处方;采用FTIR、DSC、XRD分析技术对药物与载体间的相互作用及药物在固体分散体中的存在状态进行鉴定,探讨固体分散体的增溶机制,考察固体分散体的稳定性。结果以聚乙烯吡咯烷酮(PVPK30)为载体,二氯甲烷:甲醇:乙醇-2:2:l为混合溶剂制备的固体分散体溶出度lh可达99%;红外分析表明坎地沙坦与PVPK30间有氢键形成;DSC及XRD表征表明坎地沙坦以微晶或无定形态分散于PVPK30中;稳定性加速试验显示固体分散体经过30d后XRD显示药物无明显的团聚,仍以微晶或无定形态存在。结论固体分散技术能有效提高坎地沙坦的溶出度。制得的坎地沙坦固体分散体为一稳定体系,具有实际应用价值。

关 键 词:坎地沙坦  固体分散体  正交实验  溶出度  稳定性
收稿时间:2010/9/29 0:00:00

Studies on Preparation of Candesartan Solid Dispersion and Its Dissolution and Stability
WANG Meirong,WANG Lizhen and LIN Jianying.Studies on Preparation of Candesartan Solid Dispersion and Its Dissolution and Stability[J].The Chinese Journal of Modern Applied Pharmacy,2011,28(7):654-658.
Authors:WANG Meirong  WANG Lizhen and LIN Jianying
Affiliation:Department of Pharmaceutical Engineering, College of Chemistry and Chemical Engineering, Taiyuan University of Technology, Taiyuan 030024, China;Department of Pharmaceutical Engineering, College of Chemistry and Chemical Engineering, Taiyuan University of Technology, Taiyuan 030024, China;Department of Pharmaceutical Engineering, College of Chemistry and Chemical Engineering, Taiyuan University of Technology, Taiyuan 030024, China
Abstract:OBJECTIVE To improve the solubility of candesartan by using solid dispersion(SD) technology.METHODS Single factor method and orthogonal experimental method were adopted to obtain the optimal formula by using the in vitro dissolution as an index.FTIR,DSC,XRD were used to study the existing status of candesartan in SD and bond between candesartan and carriers,so as to study solubilizing mechanism and the stability.RESULTS The ideal candesartan SD was prepared under the condition as follows,carrier was PVPK30 ...
Keywords:candesartan  solid dispersion  orthogonal design  dissolution  stability
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