【摘要】 目的探讨不同促渗剂对右旋酮洛芬氨丁三醇(DKT)水凝胶贴剂透皮吸收的影响。方法采用改良Franz扩散池,以高效液相色谱法检测一元促渗剂及多元促渗剂对DKT水凝胶贴剂累积渗透量的影响。比较无促渗剂组和含促渗剂组在比格犬体内的药代动力学(简称药动学)参数,考察其体内促渗效果。结果体外透皮试验中,以4%氮酮联用10%丙二醇的效果最好,其促渗倍率提高至无渗透促进剂的3.22倍。在药动学试验中,含促渗剂组与无促渗剂组的药动学参数0～24 h药时曲线下面积(AUC0→24 h)分别为(26.22±1.17)mg·h/L和(10.56±0.32) mg·h/L,两者比值为2.48。结论 4%氮酮联用10%丙二醇的促渗作用最好,可作为DKT水凝胶贴剂的促渗剂。更多还原

【Abstract】 Objective To investigate the effect of penetration enhancers on the transdermal permeability of dexketoprofen( DKT) trometamol hydrogel patch.Methods Modified Franz diffusion cell was used.HPLC method was adopted to detect the effect of a penetration enhancer and multiple penetration enhancers on accumulative permeation quantity of DKT trometamol in the hydrogel patch.The pharmacokinetic parameters in vivo in beagle dogs were compared between the non-penetration enhancer group and the penetration enhancer group,and the transdermal permeability of dexketoprofen trometamol hydrogel patch in vivo was studied.Results In vitro transdermal test showed that 4% azone combined with 10% propylene glycol had the best penetrative effect,and its penetration rate was the 3.22-fold enhancement of the no-penetration enhancer group.In the pharmacokinetic experiment,AUC0→24 hof DKT hydrogel patch included transdermal penetration and without transdermal penetration were( 26.22 ± 1.17) mg·h/L and( 10.56 ± 0.32) mg·h/L with the ratio of 2.48.Conclusion 4% azone combined with 10% propylene glycol has the best penetrative effect,which can be used as the enhancer for DKT trometamol hydrogel patch.更多还原