不同骨架型乌头总生物碱贴片的经皮渗透性比较研究  

Study on different matrix style of transdermal delivery system in total alkaloids patches

作　　者：李文兰[1] 徐栋[1] 王艳萍[1] 季宇彬[1] 赵培[1] 

机构地区：[1]哈尔滨商业大学生命科学与环境科学研究发展中心,哈尔滨150076

出　　处：《中国新药杂志》2008年第2期138-142,共5页Chinese Journal of New Drugs

基　　金：哈尔滨市科学计划项目(2004AA3CS173-2)

摘　　要：目的:对比研究4种不同骨架型乌头总碱贴片的透皮吸收行为,筛选最佳贴片并对其进行体外释放度实验。方法:采用改良的Franz扩散池,以生理氯化钠溶液为接收介质,以大鼠离体背部皮肤为透皮屏障,计算4种骨架型贴片中乌头总碱及新乌头碱的稳态流量及滞后时间。结果:4种经皮给药制剂(TDS)中,黏胶剂骨架型贴片(P-3)稳态流量最高,其中乌头总碱的稳态流量9.2μg.cm-2.h-1,滞后时间1.413 h;新乌头碱的稳态流量0.243 6μg.cm-2.h-1,滞后时间1.172 h。该贴片体外释放符合回归方程,Higuchi方程为S(t)=13.32t1/2+18.428,r=0.980 1,体外释药机制为药物扩散和骨架溶蚀的综合效应。结论:黏胶剂骨架型是乌头总碱经皮给药制剂的理想设计模型。Objective：To choose the optimal patch and determine the releasing rate in vitro by comparing transdermal profile of four matrix styles of total alkaloids patches. Methods ： Using modified Franz diffusion cells, isolated rear mice skin as transdermal barrier and saline isotonic solution as receptor fluid,the steady flux of total alkaloids and mesaconine permeated across mice skin per unit area and lag time were evaluated. Results：Among the four matrix styles of patches, the steady flux of total alkaloids and mesaconine in the viscose patch （ P-3 ） were the highest, they were 9.2 and 0. 243 6μg· cm ^- 2 · h^-1 respectively. And the lag time of total alkaloids and mesaconine in the patches were 1. 413 and 1. 172 h. The in vitro releasing curve of total alkaloids in vitro from Patch-3 followed the Higuchi equation which was S（t） = 13.32t1/2 ＋ 18. 428,r = 0. 980 1. The in vitro release was decided by the effect of diffusion of drug and erosion of skeleton materials. Conclusion：Viscose skeletoned-type patch is the ideal mode of the transdermal delivery system for total alkaloids.

关 键 词：乌头总碱 骨架型贴片 经皮渗透 

分 类 号：R943.41[医药卫生—药剂学]