Lack of metabolic racemisation of ropivacaine, determined by liquid chromatography using a chiral AGP column.

Abstract:

:Ropivacaine hydrochloride monohydrate (ropivacaine) is a new local anaesthetic agent which is administered exclusively as the (-)-(S)-form. The aim of the study was to determine whether metabolic racemisation of (-)-(S)-ropivacaine occurs. This was tested in man, rat, dog, and sheep after different routes of administration. The enantiomers of ropivacaine and two of the major metabolites, 3-hydroxy-ropivacaine and 2',6'-pipecoloxylidide (PPX), were determined in urine samples by liquid chromatography on a Chiral AGP column after liquid-liquid extraction. It was possible to detect < 1% of the (+)-(R)-enantiomer of both ropivacaine and the two major metabolites. In the samples examined, no trace of metabolic racemisation was observed. In pharmacokinetic, pharmacodynamic, toxicological, and metabolic studies, therefore, nonchiral assays are considered to be adequate.

journal_name

Chirality

journal_title

Chirality

authors

Arvidsson T,Bruce HF,Halldin MM

doi

10.1002/chir.530070414

subject

Has Abstract

pub_date

1995-01-01 00:00:00

pages

272-7

issue

4

eissn

0899-0042

issn

1520-636X

journal_volume

7

pub_type

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