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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 of ketoprofen (KPF) liposome gel in rats and the distribution of its local tissue in the skin. METHODS: SD rats were selected as animal models and compared with the oral administration of KPF to study the in vivo pharmacokinetics of KPF liposome gel in plasma and skin after topical application. Results: The plasma concentrations of C_ (max) and AUC_ (0 → 24) after oral administration of KPF liposome gel were (1.255 ± 0.54) μg · ml -1 and (59.388 ± 3.76) Cmax and AUC 0 ~ 24 of local skin tissue were (28.019 ± 1.98) μg · ml -1 and (602.21 ± 2.84) μg · ml -1 ~ (-1) · h. Compared with oral KPF, KPF liposome gel reduced the blood distribution, but had obvious skin accumulation ability (P <0.05). Conclusion: The topical administration of KPF liposome gel can obtain higher dermal tissue concentration while avoiding the adverse effect of higher plasma concentration, which is superior to oral administration.