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

Texto completo
Autor(es):
Silva, Carolina de Miranda [1] ; Rocha, Adriana [1] ; Tozatto, Eduardo [1] ; da Silva, Lucienir Maria [2] ; Donadi, Eduardo Antonio [2] ; Lanchote, Vera Lucia [1]
Número total de Autores: 6
Afiliação do(s) autor(es):
[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
Número total de Afiliações: 2
Tipo de documento: Artigo Científico
Fonte: Journal of Pharmaceutical and Biomedical Analysis; v. 120, p. 120-126, FEB 20 2016.
Citações Web of Science: 5
Resumo

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)

Processo FAPESP: 10/12922-1 - PK-PD (farmacocinética-farmacodinâmica) populacional do etodolaco em voluntários sadios tratados com o fármaco racêmico e seu eutômero puro.
Beneficiário:Carolina de Miranda Silva
Modalidade de apoio: Bolsas no Brasil - Pós-Doutorado