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.
出处
《药物分析杂志》
CAS
CSCD
北大核心
2012年第11期1919-1922,1928,共5页
Chinese Journal of Pharmaceutical Analysis
