• 首页期刊简介编委会刊物订阅专栏专刊电子刊学术动态联系我们English
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.
WANG Meirong,WANG Lizhen,LIN Jianying.Studies on Preparation of Candesartan Solid Dispersion and Its Dissolution and Stability[J].Chin J Mod Appl Pharm(中国现代应用药学),2011,28(7):654-658.
【打印本页】   【HTML】   【下载PDF全文】   查看/发表评论  【EndNote】   【RefMan】   【BibTex】
←前一篇|后一篇→ 过刊浏览    高级检索
本文已被:浏览 3141次   下载 3060 本文二维码信息
码上扫一扫!
分享到: 微信 更多
坎地沙坦固体分散体的制备及溶出度、稳定性研究
王美荣, 王利珍, 林建英
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︰1为混合溶剂制备的固体分散体溶出度1 h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30 d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
DOI:
分类号:
基金项目:
Studies on Preparation of Candesartan Solid Dispersion and Its Dissolution and Stability
WANG Meirong, WANG Lizhen, LIN Jianying
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 and the solvent volume ratio was methylene chloride : methanol : ethanol=2︰2︰1. The dissolution of the candesartan SD is up to 99% in one hour. XRD and DSC results showed that drug exists in crystallite or amorphous form in SD. FTIR results indicated that hydrogen bonds were formed between drug and PVPK30. Accelerated stability tests demonstrated that stability of SD was well in 30 days. CONCLUSION SD technology can obviously improve dissolution of candesartan. Candesartan SD is a stabilizing system which having actual applied value.
Key words:  candesartan  solid dispersion  orthogonal design  dissolution  stability
扫一扫关注本刊微信