Rapid pharmacokinetics screening of drug candidates in vitro and in vivo.
- Author:
Xiao-na DONG
1
;
Xiao-xia ZHU
;
Zhi-yun MENG
;
Jiang-lin LIU
;
Ying-lin CAO
;
Gui-fang DOU
Author Information
1. Institute of Transfusion Medicine, Academy of Military Medical Sciences, Beijing 100850, China.
- Publication Type:Journal Article
- MeSH:
Animals;
Chromatography, Liquid;
methods;
Drug Evaluation, Preclinical;
methods;
Female;
High-Throughput Screening Assays;
methods;
Male;
Microsomes, Liver;
metabolism;
Pharmaceutical Preparations;
administration & dosage;
blood;
metabolism;
Pharmacokinetics;
Random Allocation;
Rats;
Rats, Sprague-Dawley;
Spectrometry, Mass, Electrospray Ionization;
methods
- From:
Acta Pharmaceutica Sinica
2009;44(11):1309-1312
- CountryChina
- Language:Chinese
-
Abstract:
The paper is to report the pharmacokinetic character of a series of chemical compounds in vitro and in vivo. Metabolism stability of a series of chemical compounds was screened by using rat liver microsomes. The samples of different chemical compounds were combined and then simultaneously detected by LC-MS/MS. Compounds y13, y12 and y11 were screened out by microstability assay in vitro. The pharmacokinetics of compounds y11, y12 and y13 was evaluated by using SD rat. The plasma samples were pooled at the same time. The plasma concentrations were determined by LC-MS/MS. The pharmacokinetic character of two compounds y13, y11 was good by screening in vivo, so they were developed for further research. High-throughput screening of drug candidates in vitro and in vivo was effective, to provide information for the chemical structure information and lower the drug development risk.
