不同渗透促进剂对复方盐酸多塞平乳膏体外经皮的促渗作用研究

目的研究不同浓度油酸和氮酮及其复合物对复方盐酸多塞平乳膏透皮吸收的影响,提高乳膏中两种主要有效成分盐酸多塞平和醋酸曲安奈德的渗透效果.方法选用1%氮酮(aonze,AZ)、2%AZ、1%油酸(oleic acid,OA)、2%OA、1%OA-AZ 5种渗透吸收促进剂,采用离体小鼠皮为皮肤模型,在Franz扩散池上进行促渗实验.结果 5种渗透吸收促进剂对复方盐酸多塞平乳膏中盐酸多塞平促渗能力为2%AZ＞1%OA-AZ＞2%OA＞1%AZ＞1%OA;对醋酸曲安奈德促渗能力为2%AZ＞1%OA-AZ＞1%AZ＞2%OA＞1%OA.结论在所选的5种渗透促进剂中,选用2%AZ渗透促进剂对复方盐酸多塞平乳膏体外经皮促渗作用最显著,油酸、氮酮联合应用有协同作用,比单用氮酮或油酸促渗能力强.

Transdermal delivery effect of different penetration enhancers on compound doxepin cream

OBJECTIVE To determine the effect of different concentrations of aonze(AZ),oleic acid(OA)and complex penetration enhancers on the transdermal delivery of compound doxepin cream.The excised mouse skin was used.METHODS 1%AZ,2%AZ,1%OA,2%OA,and 1%OA AZ were used as five penetration enhancers,the in vitro transdermal permeation experiment via the mouse skin was carried out.RESULTS The five penetration enhancers could increase the permeability of the drug.The order of enhancement for doxepin hydrochloride was 2%AZ>1%OA AZ>2%OA>1%AZ>1%OA,and the order of enhancement for triamcinolone acet onide was 2%AZ>1%OA AZ>1%AZ>2%OA>1%OA.CONCLUSIONS The permeability of compound doxepin cream was most significantly increased by 2%AZ penetration enhancer.The combination of AZ and OA synergistically enhanced the drug transdermal flux of compound doxepin cream,compared with using AZ or OA alone.