Analysis of hydrochloride 4-methyl-piperazine-1-carbodithioc acid 3-cyano-3,3-diphenyl-propyl ester and its metabolites in rats by HPLC-ESI/ITMSn.
- Author:
Xiao-mei JIANG
1
;
Xiao-mei LING
;
Run-tao LI
;
Jing-rong CUI
Author Information
- Publication Type:Journal Article
- MeSH: Animals; Antineoplastic Agents; blood; metabolism; urine; Chromatography, High Pressure Liquid; methods; Feces; chemistry; Male; Molecular Structure; Piperazines; blood; metabolism; urine; Rats; Rats, Sprague-Dawley; Reproducibility of Results; Spectrometry, Mass, Electrospray Ionization; methods
- From: Acta Pharmaceutica Sinica 2006;41(11):1084-1089
- CountryChina
- Language:Chinese
-
Abstract:
AIMTo identify the main metabolites of hydrochloride 4-methyl-piperazine-1-carbodithioc acid 3-cyano-3,3-diphenyl-propyl ester (TM208) in rats.
METHODSRat feces, urine and plasma samples were collected after ig 500 mg x kg(-1) TM208, then the samples were extracted and concentrated using ethyl acetate. The treated samples were analyzed by HPLC-ESI/ITMSn. The structures of metabolites were elucidated according to the rules of drug metabolism and disposition in vivo and the characteristic fragmentation behaviors of TM208 in ESI-ITMSn.
RESULTSEight phase I metabolites were identified existing in rat feces, five of them were also found in rat urine and plasma, but no phase II metabolite was found.
CONCLUSIONThe HPLC-ESI/ITMSn method is rapid, highly sensitive and specific and it is suitable for the identification of TM208 and its metabolites in rats.