N-三甲基壳聚糖对盐酸奥昔布宁凝胶透皮促进作用的体外研究

Transdermal permeation enhancement effect of N-trimethyl chitosan on oxybutynin hydrochloride gels in vitro

目的研究季铵化程度为60%的N-三甲基壳聚糖(TMC60)对盐酸奥昔布宁(OXY)凝胶体外透皮吸收的影响。方法以含5%氮酮的OXY凝胶为阳性对照,以不含透皮促进剂的OXY凝胶为阴性对照,分别考察含3%、5%及8%TMC60的OXY凝胶的体外透皮特性,得到各组累积透过量Q,并求出稳态透皮速率J。结果阳性对照组及三种TMC60组的Q和J均显著大于阴性组(P<0.05),氮酮及TMC60均能较好地促进OXY的体外透皮效果;与阳性对照组相比,3%的TMC60促进效果明显较弱(P<0.05),而5%TMC60的促进效果与同浓度氮酮无统计学差异(P>0.05),8%TMC60的促进效果最佳(P<0.05)。结论 TMC60可以显著促进OXY凝胶的体外透皮,其中5%TMC60的促进效果与同浓度氮酮相当。

Objective To explore the transdermal permeation enhancement of N-trimethyl chitosan with a degree of quatemization of 60％ （TMC60） on oxybutynin hydrochloride （OXY） gels in vitro.Methods OXY gels containing 5 ％ Azone were chosen as the positive control and OXY gels without any enhancers as the negative control,and the transdermal permeation of OXY gels was studied with 3％,5％ and 8％ TMC60 as the enhancer.The cumulative penetration amount（Q） and the steady penetration rate（J） in vitro were obtained and compared among the above groups.Results The cumulative penetration amount and the steady penetration rate were higher in positive control group and three TMC60 groups than those in negative control group （P ＜ 0.05）.The transdermal permeation enhancement was lower in 3％ TMC60 group than that in positive group （P ＜ 0.05）,while that in 5％ TMC60 group showed no significant difference between the two groups（P ＞ 0.05）,but the transdermal permeation enhancement in 8％ TMC60 group was the best （P ＜ 0.05）.Conclusion TMC60 can enhance the transdermal permeation of OXY gels in vitro,and the enhancement is similar to that of Azone at the same concentration.