酮洛芬脂质体凝胶在大鼠体内的药物动力学及皮肤组织分布研究

目的：研究酮洛芬（KPF）脂质体凝胶在大鼠体内的药物动力学及其皮肤局部组织分布。方法：选择SD大鼠为动物模型，与KPF口服给药相对照，研究KPF脂质体凝胶局部用药后在血浆和皮肤中的体内药动学行为。结果：KPF脂质体凝胶大鼠局部给药后的血药浓度Cmax、AUC0→24分别为（1．255±0．54）μg·ml^-1和（59．388±3．76）μg·ml^-1·h，局部皮肤组织的Cmax、AUC0→24分别为（28．019±1．98）μg·ml^-1和（602．21±2．84）μg·ml^-1·h。与口服KPF相比，KPF脂质体凝胶降低了血液中的分布，而具有明显的皮肤蓄积能力（P〈0．05）。结论：KPF脂质体凝胶局部给药在获得较高的皮肤组织浓度的同时，避免了较高的血药浓度的不良反应，疗效优于口服．

Study on Pharmacokinetics and Skin Accumulation of Ketoprofen Lipogel in vivo in Rats

Objective ： To study the pharmacokinetics and skin accumulation of ketoprofen （KPF） lipogel in vivo in rats. Method ： SD mouse was used as model, the KPF concentration in plasma and skin of the lipogel were detected and Cmax and AUC0→24 in plasma and skin were calculated when compared with the common gel. Result： Cmax and AUC0→24 in plasma of KPF lipogel were （ 1. 255 ± 0. 54） μg.ml^-1 and （59. 388 ±3.76） μg.ml ^-1.h,respectively. Cmax and AUC0→24 in skin of the lipogel were （28. 019± 1.98）μg. ml^- 1 and （602. 21 ± 2. 84） μg.ml^- 1 . h ,respectively. Compared with the KPF common gel, KPF lipogel could decrease the drug concentration in blood while increase drug concentration in skin（ P 〈 0. 05 ）. Conclusion： KPF lipogel could enhance the drug accumulation in skin while decrease the concentration in plasma,which could increase the effect in local tissue while decrease the side effects.