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Preclinical study of a potent P-glycoprotein and cytochrome P450 enzyme inducer rifampicin changing pharmacokinetic parameters of risperidone and its metabolite, 9-hydroxyrisperidone, using a rat model

Title
Preclinical study of a potent P-glycoprotein and cytochrome P450 enzyme inducer rifampicin changing pharmacokinetic parameters of risperidone and its metabolite, 9-hydroxyrisperidone, using a rat model
Authors
Lee K.S.Park J.H.Lee H.J.Rhie S.
Ewha Authors
이화정이정연
SCOPUS Author ID
이화정scopus; 이정연scopus
Issue Date
2012
Journal Title
Journal of Pharmaceutical Investigation
ISSN
2093-5552JCR Link
Citation
vol. 42, no. 6, pp. 345 - 351
Indexed
SCOPUS; KCI scopus
Abstract
The objective of the present investigation is to examine the effects of rifampicin, which is a P-glycoprotein (P-gp) and cytochrome P450 (CYP)3A4 inducer, on the pharmacokinetics of risperidone and its active metabolite, 9-hydroxyrisperidone, in rats. To determine the plasma levels of risperidone and 9-hydroxyrisperidone in rats, a high performance liquid chromatographic method was developed using a liquid-liquid acid back extraction. After pretreated with rifampicin (600 mg/kg) for 6 days, the mean Cmax and AUC0-10 values of risperidone were significantly decreased and the Clt of the drug was significantly increased compared with control (p < 0.01, <0.05, and <0.05, respectively). The Cmax and AUC0-424 of 9-hydroxyrisperidone were also significantly decreased compared with control (p < 0.01, respectively). Thus, the relative bioavailability of risperidone and 9-hydroxyrisperidone once pretreated with rifampicin (600 mg/kg) was 42.5 and 32.5 %, respectively. The exposure of rifampicin significantly decreased oral bioavailability and affected the pharmacokinetics of risperidone and its active metabolite, 9-hydroxyrisperidone, by the induction of P-gp and CYP3A4 as well. © 2012 The Korean Society of Pharmaceutical Sciences and Technology.
DOI
10.1007/s40005-012-0045-0
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약학대학 > 약학과 > Journal papers
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