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Article

Effects of Silymarin on the In Vivo Pharmacokinetics of Simvastatin and Its Active Metabolite in Rats

National Clinical Drug Monitoring Center, Department of Pharmacy, Hebei Province General Center, Shijiazhuang 050051, China
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Author to whom correspondence should be addressed.
Academic Editor: Jesus Simal-Gandara
Molecules 2019, 24(9), 1666; https://doi.org/10.3390/molecules24091666
Received: 12 April 2019 / Revised: 23 April 2019 / Accepted: 25 April 2019 / Published: 28 April 2019
(This article belongs to the Special Issue Modern Analytical Techniques in Metabolomics Analysis)
Herein, the effect of silymarin pretreatment on the pharmacokinetics of simvastatin in rats was evaluated. To ensure the accuracy of the results, a rapid and sensitive UPLC–MS/MS method was established for simultaneous quantification of simvastatin (SV) and its active metabolite simvastatin acid (SVA). This method was applied for studying the pharmacokinetic interactions in rats after oral co-administration of silymarin (45 mg/kg) and different concentrations of SV. The major pharmacokinetic parameters, including Cmax, tmax, t1/2, mean residence time (MRT), elimination rate constant (λz) and area under the concentration-time curve (AUC0–12h), were calculated using the non-compartmental model. The results showed that the co-administration of silymarin and SV significantly increased the Cmax and AUC0–12h of SVA compared with SV alone, while there was no significant difference with regards to Tmax and t1/2. However, SV pharmacokinetic parameters were not significantly affected by silymarin pretreatment. Therefore, these changes indicated that drug-drug interactions may occur after co-administration of silymarin and SV. View Full-Text
Keywords: herb-drug interaction; silymarin; simvastatin; simvastatin hydroxyacid; pharmacokinetics herb-drug interaction; silymarin; simvastatin; simvastatin hydroxyacid; pharmacokinetics
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MDPI and ACS Style

Li, Y.; Wu, Y.; Li, Y.-J.; Meng, L.; Ding, C.-Y.; Dong, Z.-J. Effects of Silymarin on the In Vivo Pharmacokinetics of Simvastatin and Its Active Metabolite in Rats. Molecules 2019, 24, 1666. https://doi.org/10.3390/molecules24091666

AMA Style

Li Y, Wu Y, Li Y-J, Meng L, Ding C-Y, Dong Z-J. Effects of Silymarin on the In Vivo Pharmacokinetics of Simvastatin and Its Active Metabolite in Rats. Molecules. 2019; 24(9):1666. https://doi.org/10.3390/molecules24091666

Chicago/Turabian Style

Li, Ying, Yin Wu, Ya-Jing Li, Lu Meng, Cong-Yang Ding, and Zhan-Jun Dong. 2019. "Effects of Silymarin on the In Vivo Pharmacokinetics of Simvastatin and Its Active Metabolite in Rats" Molecules 24, no. 9: 1666. https://doi.org/10.3390/molecules24091666

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