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dc.date.accessioned 2011-12-28T17:52:11Z
dc.date.available 2011-12-28T03:00:00Z
dc.date.issued 2011 es
dc.identifier.uri http://sedici.unlp.edu.ar/handle/10915/8385
dc.description.abstract Substrate-dependent inhibition of CYP3A4 might influence the extrapolation of drug interactions from the in vitro to in vivo situation. The aim of the present study is to investigate reversible and time-dependent inhibition of CYP3A4-mediated nifedipine oxidation by noscapine. Furthermore, in vitroin vivo extrapolation (IVIVE) was performed using in vitro parameters. The results showed that CYP3A4- mediated nifedipine oxidation activity was strongly inhibited with an IC50 of 25.7 ± 5.4 μM. Kinetic analysis showed that inhibition of CYP3A4-mediated nifedipine oxidation by noscapine was best fit to a noncompetitive manner with Ki value of 10.9 μM. IC50 shift experiment showed that IC50 was significantly decreased from 25.7 ± 5.4 μM to 0.34 ± 0.07 μM after pre-incubation with noscapine for 30 min, which indicated that time-dependent inhibition existed for inhibition of CYP3A4 by noscapine. The AUC of (R)- warfarin was predicted to increase by 0.5 % using Cmax or 0.2 % using unbound Cmax with reversible inhibition prediction equation, while the AUC of (R)-warfarin was estimated to increase by 23.1 % using Cmax or 10.4 % using unbound Cmax with TDI prediction equation. Inhibition of CYP3A4 by noscapine showed substrate-dependent inhibition behaviour. However, the results obtained from IVIVE are very similar using testosterone or nifedipine as probe substrates. es
dc.format.extent 1854-1857 es
dc.language en es
dc.subject Warfarina es
dc.subject Sustratos es
dc.subject Noscapina es
dc.subject Nifedipino es
dc.subject Interacciones de Drogas es
dc.title Reversible and time-dependent inhibition of CYP3A4-mediated nifedipine oxidation by noscapine es
dc.type Articulo es
sedici.identifier.uri http://www.latamjpharm.org/resumenes/30/9/LAJOP_30_9_2_2.pdf es
sedici.creator.person Wang, Li-Ming es
sedici.creator.person Yang, Ling es
sedici.creator.person Li, Ming es
sedici.creator.person Sun, De-Guang es
sedici.creator.person Tang, Bo es
sedici.creator.person Gao, Zhen-Ming es
sedici.creator.person Liang, Rui es
sedici.creator.person Qu, Yan-Qing es
sedici.creator.person Fang, Zhong-Ze es
sedici.creator.person Tang, Shu-Hong es
sedici.creator.person Jin, Xue Li es
sedici.subject.materias Farmacia es
sedici.description.fulltext false es
mods.originInfo.place Colegio de Farmacéuticos de la Provincia de Buenos Aires es
sedici.subtype Comunicacion es
sedici2003.identifier ARG-FARM-ART-0000001873 es
sedici.relation.journalTitle Latin American Journal of Pharmacy es
sedici.relation.journalVolumeAndIssue vol. 30, no. 9 es


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