Effects of Zhenyuan capsule on the pharmacokinetics comparison of simvastatin and its active metabolites in rats

doi:10.5246/jcps.2020.07.047

Abstract

Abstract:

The total ginsenosides of ginseng fruit are the main constituents of Zhenyuan capsule, which is mainly used for the treatment of cardiovascular diseases. It has been reported that ginsenoside can affect the activity of CYP450 enzymes. Zhenyuan capsule and simvastatin may interact with each other through CYP3A4 mediation, then affect the efficacy and even produce adverse reactions. However, no studies have investigated the effects of Zhenyuan capsule on the pharmacokinetics of simvastatin and its active metabolites. In this study, liquid chromatography–electrospray ionization–mass spectrometry (LC-MS/MS) was used to detect the pharmacokinetics of simvastatin and its active metabolites-simvastatin acid with or without Zhenyuan capsule in rats. Compared with the simvastatin alone, the pharmacokinetic parameters of simvastatin and simvastatin acid were significantly different in AUC₀_–₂₄ and AUC₀_–_∞, and they were decreased in varying degrees (P<0.05). It appeared that the Zhenyuan capsule might increase the activity of CYP3A4 to some extent.

Key words: Zhenyuan capsule, Simvastatin, Simvastatin acid, LC-MS/MS, Pharmacokinetics

CLC Number:

R942

Supporting:

Ye Yuan, Bo Yu, Xueqin Zhang, Yanan Li, Shumei Wang. Effects of Zhenyuan capsule on the pharmacokinetics comparison of simvastatin and its active metabolites in rats[J]. Journal of Chinese Pharmaceutical Sciences, 2020, 29(7): 494-503.

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