摘要
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C_(max)、AUC_(0→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C_(max)、AUC_(0→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。
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.
出处
《中国药师》
CAS
2010年第12期1704-1707,共4页
China Pharmacist
