促渗剂对消喘巴布剂中白芥子体外透皮吸收特性的影响

Effects of different penetration enhancers on percutaneous absorption of sinapis alba of Xiaochuan cataplasmin vitro

目的:探讨不同的透皮促渗剂对消喘巴布剂中白芥子体外透皮吸收特性的影响。方法:采用Franz扩散池和离体大鼠皮肤进行体外透皮实验,计算出含不同促渗剂的消喘巴布剂中芥子碱硫氰酸盐的累积渗透量和渗透速率。结果:芥子碱硫氰酸盐体外透皮吸收符合零级动力学方程,不同的促渗剂对芥子碱透皮吸收影响的顺序为:月桂氮芯卓酮>丙二醇>薄荷脑,同种促渗剂的不同浓度对消喘巴布剂透皮吸收影响的顺序为:月桂氮芯卓酮1%>3%>5%;丙二醇5%>7%>3%;薄荷脑1%>3%>2%。结论:不同的透皮促渗剂都能促进消喘巴布剂中芥子碱的透皮吸收,但是不同的浓度促渗效果却不同,其中以1%月桂氮芯卓酮促渗效果最好。

OBJECTIVE To investigate the effect of different preparation enhancers on percutaneous absorption of Xiaochuan Cataplasm in vitro. METHODS Using Franz-type diffusion cell and excised big mouse skin in vitro as transdermal barrier, the content of sinapine thiocyanate in different kinds and concentration enhancers was determined by HPLC, then cumulative per- meation quantity（Q） and the penetration rate（J） of Xiaochuan Cataplasm was calculate. RESULTS The releasing permeated amount of sinapine thiocyanate in vitro complied with the zero releasing equation. The ordering of the effects of different pene- tration enhancers on permeation quantity（Q） and the penetration rate（J） of Xiaochuan Cataplasm was azone〉propylene glycol- glycol〉menthol. The ordering of the effects of the different concentration of same penetration enhancers was azone 1% 〉3 % 〉 5% Propylene glycol 5% 〉7% 〉3%, menthol 1% 〉3% 〉2%. CONCLUSION Azone, propylene glycol and menthol can all enhance transdermal absorption of sinapine thiocyanate, but only in the appropriate concentrations can they best act their effective of permeation enhancing. The effect ofpromoting penetration of 1 % azone is the best.