盐酸格拉司琼微乳的制备及其体外经皮渗透研究  

Study on preparation of granisetron hydrochlorid microemulsion and its percutem permeation in vitro

作　　者：张雪梅[1] 余瑜[1] 赵领[1] 钟晓东[1] 梁艳[1] 李必波[1] 

机构地区：[1]重庆医科大学药学院药物化学与生物材料研究室重庆高校药物工程研究中心,重庆400016

出　　处：《重庆医科大学学报》2009年第6期735-739,共5页Journal of Chongqing Medical University

基　　金：国家自然科学基金(30772595)

摘　　要：目的:研制新型盐酸格拉司琼(Granisetron hydrochloride,GH)水包油(O/W)型微乳透皮剂。方法:利用伪三元相图方法研究微乳中十四酸异丙酯(Isopropyl myristate,IPM)、卵磷脂(Phosphatidyl choline,PC)、吐温80(Tween80,T80)、乙醇(Ethanol,Eth)、水的组成及配比;采用正交设计实验,以影响微乳质量的原辅料为考察因素,以各种原辅料的不同用量为考察水平,以经皮渗透稳态流量、时滞和累积渗透量为指标,经体外经皮渗透实验,筛选出最佳处方。结果:GH微乳的最佳处方为A2B1C2,即IPM/Km为1∶6、Km为3∶1、GH为5.0%。结论:微乳具有较强的促进GH经皮渗透作用,有望成为GH的新型透皮给药制剂。Objective：To prepare O/W granisetron hydrochloride （GH）microemulsion of a new type transdermal delivery system. Methods： The microemulsion was prepared with the formulation containing isopropyl myristate-phosphatidyl choline-tween80-ethanol-water by the pseudo-ternary phase diagram.Quality of feedstock and adjuvant was selected as investigation factor.Dosage was selected as investigation level.The permeation steady state flux,lag time and cumulative permeation quantity of GH were selected as indices, Orthogonal tests were carried out to obtain the optimum formulation. Results：The optimum formulation of GH was A2B1C2 that IPM/Km, Km and GH were 1： 6,3：1,5.0%. Conclusion：These results indicated that the studied microemulsion system with high osmosis acoss nude rabbits skin could be a potential vehicle for the transdermal delivery of GH.

关 键 词：盐酸格拉司琼 微乳 伪三元相图 经皮渗透 

分 类 号：R94[医药卫生—药剂学]