促渗剂对青藤碱脂质体透皮贴剂经皮渗透的影响

Effect of Penetration Enhancers on the Transdermal Penetration of Sinomenine Liposome Patch

目的:研究促渗剂对青藤碱透皮贴剂经皮渗透行为的影响。方法:建立离体经皮渗透试验方法,并作方法学考察。分别在贴剂中加入单一及复合促渗剂5%氮酮、10%油酸、1%丙二醇+4%氮酮、2%丙二醇+8%油酸,在相同条件下进行离体经皮渗透试验,测定不同时间的药物累积透过量。离体试验结束后,测定皮肤层中药物的滞留量。结果:在贴剂处方中加入促渗剂后,药物累积透过量增加,而皮肤层中的滞留药量减少。结论:促渗剂可使贴剂内药物穿透角质层进入真皮层,而不能增加药物在角质层内的积累。故可推测,在脂质体贴剂中加入促渗剂可能导致脂质体双分子层结构的破坏,引起药物渗漏,从而不利于药物在皮肤及局部组织的蓄积。故作用于局部的脂质体贴剂中不宜加入促渗剂。

Objective: To study the effect of penetration enhancers on the transdermal penetration of sinomenine liposome patch. Methods: We firstly established the experimental method of transdermal penetration, and the methodology study was carried out at the same time. Furthermore, we added 5% Azone, 10% Oleic acid, 1% PG+4%Azone, 2%PG+8%Oleic acid into the patch. The cumulative penetration amounts were determined during the test of transdermal penetration and the part lagged in the skin was determined after the test. Results: The cumulative penetration amounts released from the patch increased, while the part lagged in the skin decreased at the same time. Conclusions: The results indicate that penetration enhancers can facilitate drug through corneum into dermis, but can't enhance the drug's accumulation in the corneum. It is concluded that penetration enhancers can destroy the two-molecule structure of liposomes and cause drug leakage, so penetration enhancers should not be added into liposome patch of part functions.