不同透皮促进剂对双氯芬酸钾凝胶体外透皮效果的影响研究

Effect of Different Penetration Enhancers on the Transdermal Permeation of Diclofenac Potassium Gel in Vitro

目的:考察氮酮(Azone)、丙二醇(PG)、油酸(OA)3种透皮促进剂一元、二元、三元联合对双氯芬酸钾凝胶的体外促透作用。方法:配制以下13种含不同透皮促进剂的双氯芬酸钾凝胶处方:空白,3%Azone,5%OA,12%PG,6%PG+2.5%OA,12%PG+5%OA,1.5%Azone+2.5%OA,1.5%Azone+6%PG+5%OA,1.5%Azone+12%PG,3%Azone+5%OA,3%Azone+6%PG,3%Azone+6%PG+5%OA,3%Azone+12%PG,以透皮速率J等为指标,采用改良的Franz扩散池,以离体人皮肤为透皮屏障,测定并计算双氯芬酸钾凝胶加入上述不同透皮促进剂处理后药物的透皮性能。结果:与空白组比较,其它各组J值均升高,其中以3%Azone+12%PG组的J值最高,达10.253 0μg.cm-2.h-1。结论:3种透皮促进剂对双氯芬酸钾凝胶均有不同程度促透效果,但以Azone和PG二元联用效果最佳。

OBJECTIVE： To study the effects of Azone, propylene glycol （PG）, oleic acid （OA） alone or in combination of two or three as penetration enhancers on the in vitro transdermal efficacy of dielofenae potassium（DP） gels. METHODS： Thirteen formulations of DP gels containing the following different penetration enhancers at different concentrations were prepared： blank, 3% Azone, 5% OA, 12% PG, 6% PG＋2.5% OA, 12% PG＋5% OA, 1.5% Azone＋2.5% OA, 1.5% Azone ＋ 6% PG ＋ 5% OA, 1.5 % Azone ＋ 12% PG, 3% Azone ＋ 5o/00A, 3% Azone ＋ 6% PG, 3% Azone ＋ 6% PG ＋ 5% OA, and 3% Azone ＋ 12% PG. The in vitro permeation test was performed on a modified Franz - type diffusion cell with human skin as transdermal barrier taking transdermal velocity （J） as index to determine and compute the transdermal properties of the DP gels after treated respectively by the above 13 penetration enhancers. RESULTS： Compared with the blank control group, all the penetration enhancer-treated formulations showed significant higher J value, with the formulation treated by 3% Azone＋ 12% PG enhancer showing the highest J value of 10.253 μg · cm ^-2· h^-1. CONCLUSION： All the three penetration enhancers could promote the transdermal permeation DP gels, much as in the combination of Azone and propylene.