Development of an enantiomer selective microsampling assay for the quantification of ketorolac suitable for paediatric pharmacokinetic studies.
Biopharm Drug Dispos
; 34(7): 377-86, 2013 Oct.
Article
em En
| MEDLINE
| ID: mdl-24251328
ABSTRACT
BACKGROUND:
Ketorolac, a potent nonsteroidal anti-inflammatory drug used for pain control in children, exists as a racemate of inactive R (+) and active S (-) enantiomers.AIM:
To develop a microsampling assay for the enantioselective analysis of ketorolac in children.METHODS:
Ketorolac enantiomers were extracted from 50 µl of plasma by liquidliquid extraction and separated on a ChiralPak AD-RH. Detection was by a TSQ quantum triple quadrupole mass spectrometer with an electrospray ionisation source operating in a positive ion mode. Five children (age 13.8 (1.6) years, weight 52.7 (7.2) kg), were administered intravenous ketorolac 0.5mg/kg (maximum 10mg) and blood samples were taken at 0, 0.25, 0.5, 1, 2, 4, 6, 8 and 12 h post administration. CL, VD and t1/2 were calculated based on non-compartmental methods.RESULTS:
The standard curves for R (+) and S (-) ketorolac were linear in the range 02000 ng/ml. The LLOQs of the method were 0.15 ng on column and 0.31 ng on column for R (+) and S (-) ketorolac, respectively. The median (range) VD and CL of R (+) and S (-) ketorolac were 0.12 l/kg (0.070.17), 0.017 l/h/kg (0.120.29) and 0.17 (0.090.31) l/kg, 0.049 (0.020.1) l/h/kg, p = 0.043), respectively. The median (range) elimination half-life (t1/2) of the R (+) and S (-) ketorolac was 5.0 h (2.55.8) and 3.1 h (1.84.4), p = 0.043), respectively.CONCLUSION:
The development of a simple, rapid and reliable ketorolac assay suitable for paediatric PK studies is reported.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Anti-Inflamatórios não Esteroides
/
Cetorolaco
Limite:
Adolescent
/
Child
/
Humans
Idioma:
En
Revista:
Biopharm Drug Dispos
Ano de publicação:
2013
Tipo de documento:
Article