Determination of S 12024 enantiomers in human plasma by liquid chromatography after chiral pre-column derivatization.

Abstract:

:S 12024-2 is a new drug in phase II development that possesses cognitive enhancing properties. As its molecular structure has a chiral centre, a stereoselective method for the analysis of both enantiomers in human plasma has been developed. The method involves pre-column derivatization of the amine moiety with a homochiral reagent (+)-1-(9-fluorenyl)ethyl chloroformate (FLEC), and chromatographic separation of the two diastereoisomers on an achiral reversed-phase cyanopropyl column, with fluorimetric detection (lambda ex = 260 nm; lambda em = 310 nm). A liquid-liquid extraction procedure with diethyl ether-dichloromethane (70:30, v/v) was used for sample preparation. This technique provides a linear response for both enantiomers over a concentration range of 10-500 ng ml-1 and the quantitation limit was set at 5 ng ml-1 in human plasma. Within-day and between-day precision and accuracy are within 9% limits for all concentrations assessed. This procedure was therefore used for determining both enantiomers in human plasma following oral administration of racemic S 12024-2 to elderly healthy subjects.

journal_name

J Pharm Biomed Anal

authors

Boursier-Neyret C,Baune A,Klippert P,Castagne I,Sauveur C

doi

10.1016/0731-7085(93)80099-m

subject

Has Abstract

pub_date

1993-11-01 00:00:00

pages

1161-6

issue

11-12

eissn

0731-7085

issn

1873-264X

pii

0731-7085(93)80099-M

journal_volume

11

pub_type

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