Enantioselective analysis of etodolac in human pla... - BV FAPESP
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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Enantioselective analysis of etodolac in human plasma by LC-MS/MS: Application to clinical pharmacokinetics

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Author(s):
Silva, Carolina de Miranda [1] ; Rocha, Adriana [1] ; Tozatto, Eduardo [1] ; da Silva, Lucienir Maria [2] ; Donadi, Eduardo Antonio [2] ; Lanchote, Vera Lucia [1]
Total Authors: 6
Affiliation:
[1] Univ Sao Paulo, Fac Ciencias Farmaceut Ribeirao Preto, Dept Anal Clin Toxicol & Bromatol, Ave Cafe Sn, Campus USP, BR-14040903 Ribeirao Preto, SP - Brazil
[2] Univ Sao Paulo, Fac Med Ribeirao Preto, Dept Clin Med, BR-14040903 Ribeirao Preto, SP - Brazil
Total Affiliations: 2
Document type: Journal article
Source: Journal of Pharmaceutical and Biomedical Analysis; v. 120, p. 120-126, FEB 20 2016.
Web of Science Citations: 5
Abstract

Etodolac is a non-steroidal anti-inflammatory drug with preferential inhibition of cyclooxigenase-2 and is widely used in the management of pain in patients with inflammatory arthritis. Etodolac is available as a racemic mixture of (-)-(R)-Etodolac and (+)-(S)-Etodolac; cyclooxigenases inhibition is attributed to (+)-(S)-Etodolac. According to our knowledge, this is the first method for determination of etodolac enantiomers in plasma using LC-MS/MS. Plasma extraction were performed with 25 mu L of plasma and 1 mL of n-hexane:ethyl acetate (95:5); racemic ibuprofen was used as internal standard. Resolution of enantiomers were performed in a Chiralcel (R) OD-H column; deprotonated {[}M-H](-) and their respective ion products were monitored at transitions of 286>242 for etodolac enantiomers and 205>161 for ibuprofen. The quantitation limit was 3.2 ng/mL for both enantiomers in plasma. The method was applied to study the pharmacokinetics of etodolac enantiomers after the administration of a 300 and 400 mg dose of racemic drug to a healthy volunteer. Analysis of plasma samples showed higher plasma concentration of (-)-(R)-Etodolacfor both doses (300 mg dose: AUC(0-infinity)49.80 versus 4.55 ug h/mL;400 mg dose: AUC-(0-infinity) 63.90 versus 6.00 ug h/mL) with an (R)-(+)/(S)-(-) ratio of approximately 11. (C) 2015 Elsevier B.V. All rights reserved. (AU)

FAPESP's process: 10/12922-1 - POPULATION PK-PD (PHARMACOKINETIC-PHARMACODYNAMIC) OF ETODOLAC IN HEALTHY VOLUNTEERS TREATED WITH RACEMIC DRUG AND ITS PURE EUTOMER.
Grantee:Carolina de Miranda Silva
Support Opportunities: Scholarships in Brazil - Post-Doctoral