透皮促渗剂对双乌跌打损伤药方体外透皮吸收和体内药效的影响

Influence of Penetration Enhancers on in Vitro Transdermal Permeation and in Vivo Pharmacodynamics of Shuangwu Fractures Prescription

目的考察透皮促渗剂对双乌跌打损伤药方体外透皮吸收和体内药理效应的影响。方法采用Franz扩散池,以小鼠离体皮肤为渗透屏障,比较不同透皮促渗剂对双乌跌打损伤复方中指标成分胡椒碱透皮吸收的影响,并在此基础上筛选最佳透皮促渗剂的比例和浓度。采用小鼠热板法和二甲苯致小鼠耳肿胀实验,平行比较了含与不含透皮促渗剂药方的消炎镇痛作用。结果月月月月酮和NMP合用促透效果最好,稳态渗透速率达到4.1712μg·cm-2·h-1。NMP与月月月月酮比为7:3,浓度为3%时,对胡椒碱的促透作用最强。双乌跌打损伤药方有明显的消炎镇痛作用,促透剂的加入可以进一步加强药效(P<0.1)。结论采用浓度为3%,以此月月月月酮复合促透剂可取得对胡椒碱的最大促透效果,并提高药方消炎镇痛的作用。

OBJECTIVE To study the influence of penetration enhancers on the transdermal absorption in vitro and explore in vivo pharmacodynamic responses of Shuangwu fractures prescription with or without enhancers. METHODS Skin permeation of piperine, the main constituent of Shuangwu fractures prescription, was evaluated by the Franz diffusion cell method with isolated rat skin. Different kinds, percentages and concentrations of penetration enhancers were applied. Furthermore, the analgesic and anti-inflammatory effects of the formula suspension with and without penetration enhancers were evaluated by hot-plate pain trial and xylene-induced ears edema method. RESULTS Azone combined with NMP was found to be the optimal penetration enhancer with the steady state flux up to 4.171 2 μg·cm^-2h^-1. The greatest penetration efficiency of piperine can be achieved by the compound enhancer Azone and NMP （3 ： 7） at 3%. Shuangwu fractures prescription showed positive effect on analgesis and anti-inflammatory, and the effect was enhanced with the added penetration enhancers（P〈0.l）. CONCLUSION 3% Compoud penetration enhancer, Azone and NMP （3：7）, can achieve the best enhancerment on transdermal penetration of piperine in vitro. Shuangwu fractures perscription containing this enhancer can get increased anti-inflammatory and analgesic effect in vivo.