马钱子碱与士的宁体外经皮渗透性质的考察

Percutaneous permeation of brucine and strychnine in vitro

目的:考察马钱子碱、士的宁游离药物体外经皮渗透性质及相互影响。方法:测定马钱子碱及士的宁在pH值7.4的磷酸盐缓冲液(PBS)、含10%乙醇的PBS、含20%乙醇的PBS及含20%乙醇的生理氯化钠溶液中的溶解度。用改良的Franz扩散池法考察马钱子碱溶液、士的宁溶液以及混合溶液中马钱子碱与士的宁体外透皮渗透性质。结果:根据溶解度实验结果选择含20%乙醇的PBS作为溶剂;以含20%乙醇的生理氯化钠溶液为接受液。马钱子碱与士的宁混合溶液中马钱子碱的体外经皮渗透速率比单用马钱子碱显著提高了近1.5倍(P<0.05),累积透过百分率也明显提高(P<0.01);而士的宁没有显著变化。结论:士的宁可显著促进马钱子碱的体外经皮渗透速度和程度。

Objective：To evaluate the permeability and interaction of brucine and strychnine in vitro Methods：The solubility of brucine and strychnine in PBS, 10% alcohol PBS,20% alcohol PBS and 20% alcohol NS were determined by HPLC. The permeability of the solution of brucine,strychnine and their mixed solution was determined in vitro using Franz diffusion cell with mice skin. Results：According to the solubility,20% alcohol PBS was as the solvent,20% alcohol NS as the reception. Compared to the solution of brucine, the permeability of the mixed solution was almost increased by 1.5 times,and accumulated permeation dose ratio of brucine was also ele- rated. No effect of brucine on the permeability of the strychnine was found. Conclusions：Strychnine can increase the permeability and cumulative permeation of brucine in vitro .