As a potent drug used to improve the neurodegenerative conditions, there is few information about the brain tissue distribution of tranilast by now. In this study, a novel sensitive LC-MS/MS method has been developed and validated to determine tranilast in rat brain tissue samples. The calibration curve showed good linearity ranged from 2.140 to 428.0ng·mL-1. The method was fully validated and successfully applied in the brain tissue distribution study of tranilast in rats, which had never been reported in detail by now. Furthermore, a rapid LC-MS/MS method with a short run time of 3min was developed and validated for the determination of tranilast in rat plasma and the application to a pharmacokinetic study of tranilast in rats. After oral dosage of 10.5mg·kg-1 tranilast, the maximum plasma concentration (Cmax1) of tranilast was (18.59±5.40) μg·mL-1 at (0.667±0.408) h while the area under the curve (AUC0-24) was (54.87±14.13) μg·h·mL-1 with the elimination half-life of (2.93±0.41) h. The ratio calculated by dividing the concentration of tranilast in brain with the concentration of tranilast in the plasma, was (0.6042

作者：Wen, Yang；Eboka Majolene B, Sabi-Mouka；Lei, Wang；Chang, Shu；Yan, Wang；Juefang, Ding；Li, Ding

来源：Journal of pharmaceutical and biomedical analysis 2017 年