Pharmacokinetic Study of Letrozole Polymorphs in Rats

VernacularTitle:大鼠灌胃不同晶型来曲唑的药动学
Author: Junke SONG ¹ ; Cheng XING ; Ningbo GONG ; Wen ZHANG ; Jialin SUN ; Yang LYU ; Guanhua DU
Author Information

1. 中国医学科学院北京协和医学院药物研究所天然药物活性物质与功能国家重点实验室
Keywords: Letrozole; Crystal form; Pharmacokinetics; Chromatography,high-performance liquid
From: Herald of Medicine 2019;38(2):183-187
CountryChina
Language:Chinese
Abstract: Objective To study the gastrointestinal absorption process of three letrozole polymorphs in rats, and evaluate the different pharmacokinetics parameters of different polymorphs. Methods A total of 18 SD rats were given the different letrozole polymorphs. Then the high-performance liquid chromatographic method was used for the determination of plasma concentration of letrozole in these SD rats.Finally the pharmacokinetic parameters among the different polymorphs were calculated. Results Cmax of letrozole crystal form I, crystal form II and crystal form III were (9.247± 4.612) ,(23.387± 9.049) and (15.682±1.589) mg·L-1, respectively, and AUC0→t were(198.115±47.014) ,(476.641±125.467) and (271.817±41.068) mg·L-1·h,respectively. Conclusion The different crystal forms of letrozole result in different plasma concentration in SD rats. Crystal form II may be its preponderant polymorphs which deserves further research and development.