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萘哌地尔自微乳化释药系统的制备
引用本文:江兴龙,贾运涛,张良珂,田睿,滕永真. 萘哌地尔自微乳化释药系统的制备[J]. 中国医药工业杂志, 2012, 43(9): 756-759
作者姓名:江兴龙  贾运涛  张良珂  田睿  滕永真
作者单位:1. 重庆医科大学药学院,重庆400016;重庆医科大学生命科学研究院,重庆400016
2. 重庆医科大学附属儿童医院药剂科,重庆,400010
3. 重庆医科大学药学院,重庆,400016
4. 重庆医科大学生命科学研究院,重庆,400016
基金项目:重庆市渝中区科委科技三费资助项目,重庆市教育委员会科学技术研究项目,重庆市卫生局课题资助
摘    要:通过萘哌地尔在不同辅料中的平衡溶解度和伪三元相图筛选了空白自微乳化释药系统(SMEDDS)的组分,并继续用正交设计和单因素试验优化载萘哌地尔SMEDDS的处方。所得优化处方中萘哌地尔的溶解度显著高于水中溶解度,稀释后能形成平均粒径约23 nm的微小乳滴。体外释放试验表明,萘哌地尔SMEDDS及其混悬液在pH 6.8磷酸盐缓冲液中8 h累积释放率均低于20%;但在0.1 mol/L盐酸中,前者释放较快且完全。

关 键 词:萘哌地尔  自微乳化释药系统  伪三元相图  制备

Preparation of Naftopidil Self-microemulsifying Drug Delivery System
JIANG Xinglong , JIA Yuntao , ZHANG Liangke , TIAN Rui , TENG Yongzhen. Preparation of Naftopidil Self-microemulsifying Drug Delivery System[J]. , 2012, 43(9): 756-759
Authors:JIANG Xinglong    JIA Yuntao    ZHANG Liangke    TIAN Rui    TENG Yongzhen
Affiliation:1.School of Pharmacy,Chongqing Medical University,Chongqing 400016;2.Institute of Life Sciences,Chongqing Medical University,Chongqing 400016;3.Dept.of Pharmacy,Children’s Hospital of Chongqing Medical University,Chongqing 400010)
Abstract:The components of the blank self-microemulsifying drug delivery system(SMEDDS) were screened by the results of equilibrium solubility of naftopidil in different excipients and pseudo-ternary phase diagrams.The formulation of SMEDDS loaded with naftopidil was optimized by orthogonal design and single factor experiment.The solubility of naftopidil in the optimal SMEDDS was significantly higher than in water.The mean particle size was about 23 nm after self-microemulsification.The results of the in vitro release test showed that the cumulative amount at 8 h of naftopidil SMEDDS and its suspension in pH 6.8 phosphate buffer were lower than 20% while the former released faster and more completely in 0.1 mol/L HCl.
Keywords:naftopidil  self-microemulsifying drug delivery system  pseudo-ternary phase diagram  preparation
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