新型天然酪氨酸酶抑制剂UP302乳膏的大鼠透皮吸收和排泄研究  

Percutaneous absorption and excretion of a novel natural tyrosinase inhibitor UP302 emulsion in rats

作　　者：张双庆[1] 于敏[1] 闻镍[1] 朱凌[1] 李佐刚[1] 

机构地区：[1]中国食品药品检定研究院食品药品安全评价研究所药物代谢动力学实验室,北京100176

出　　处：《药物分析杂志》2012年第11期1919-1922,1928,共5页Chinese Journal of Pharmaceutical Analysis

摘　　要：目的:研究新型天然酪氨酸酶抑制剂UP302乳膏经皮给予大鼠后的吸收和排泄。方法:大鼠经皮给予10 mg.cm-2UP302乳膏(以UP302计为0.2 mg.cm-2),收集血液、尿液、粪便和皮肤生物样品,用LC-MS/MS法测定UP302浓度,HPLC法测定乳膏中未吸收的UP302量。大鼠尾静脉同时给予5 mg.kg-1UP302用于计算经皮给药的绝对生物利用度。结果:UP302乳膏绝对生物利用度为8.07%,皮肤中UP302的量为透皮给药量的0.087%±0.025%,粪便中UP302排泄量为透皮给药量的0.091%±0.026%,尿液中未发现UP302,皮肤上残留的UP302量为78.96%±5.88%。结论:为评价UP302乳膏在动物体内的吸收动力学及为毒性安全性评价提供参考。Objective：To investigate percutaneous absorption and excretion of a novel natural tyrosinase inhibitor UP302 emulsion applied to rats. Methods： Samples of blood, urine, feces and treated skin were collected after the emulsion was applied to rats at a dose of 10 mg cm-2（equivalent to 0.2 mg cm-2 of UP302） in which the con- tents of UP302 were determined by LC - MS/MS, and the residual UP302 on the skin surface of rats was measured by HPLC. Absolute bioavailability of UP302 which was injected in rats via the tail vein by 5 mg kg -1 was calculated Results： Absolute bioavailability of UP302 emulsion was 8.07% ,and the contents of UP302 in skin,feces and urine were 0. 087% ± 0. 025% ,0. 091% ± 0. 026% and 0 of the applied dose, respectively. Residual amount of UP302 on the surface of skin was 78.96% ± 5.88%. Conclusion： Useful information was obtained for pharmacoki- netics and safety evaluation of UP302 emulsion in rats.

关 键 词：酪氨酸酶抑制剂UP302乳膏 透皮吸收 排泄酪氨酸酶 生物利用度 吸收动力学 

分 类 号：R917[医药卫生—药物分析学]