Abstract Title:

Effect of silymarin supplement on the pharmacokinetics of rosuvastatin.

Abstract Source:

Pharm Res. 2008 Aug;25(8):1807-14. Epub 2008 Jan 31. PMID: 18236139

Abstract Author(s):

Jian Wei Deng, Ji-Hong Shon, Ho-Jung Shin, Soo-Jin Park, Chang-Woo Yeo, Hong-Hao Zhou, Im-Sook Song, Jae-Gook Shin

Article Affiliation:

Department of Pharmacology and Pharmacogenomics Research Center, Inje University College of Medicine, 633-165 Gaegum-Dong, Jin-Gu, Busan, 614-735, South Korea.

Abstract:

OBJECTIVES: To evaluate the effect of silymarin on the pharmacokinetics of rosuvastatin in systems overexpressing OATP1B1 or BCRP transporters and in healthy subjects.

MATERIALS AND METHODS: The concentration-dependent transport of rosuvastatin and the inhibitory effect of silymarin were examined in vitro in OATP1B1-expressing oocytes and MDCKII-BCRP cells. For in vivo assessment, eight healthy male volunteers, divided into two groups, were randomly assigned to receive placebo or silymarin (140 mg) three times per day for 5 days. On day 4, all subjects received rosuvastatin (10 mg, 8 AM: ) 1 h after the placebo or silymarin administration. A series of blood samples were collected for 72 h, and the plasma concentration of rosuvastatin was determined using LC-MS/MS.

RESULTS: Based on the concentration dependency of rosuvastatin transport in the OATP1B1 and BCRP overexpression systems, rosuvastatin is a substrate for both transporters. Silymarin inhibited both OATP1B1- and BCRP-mediated rosuvastatin transport in vitro (K (i) 0.93 microM and 97 microM, respectively). However, no significant changes in AUC, half-life, Vd/F, or Cl/F of rosuvastatin were observed in human subjects following pretreatment with silymarin.

CONCLUSIONS: Silymarin does not appear to affect rosuvastatin pharmacokinetics in vivo, suggesting that silymarin, administered according to a recommended supplementation regimen, is not a potent modulator of OATP1B1 or BCRP in vivo.

Study Type : Human Study

Print Options


Disqus

Login to Comment

Commenting is limited to Members only. If you are already a member, please login to post a comment. If you do not have a member account and would like to become a member, please click here to begin the process to become a member.

Key Research Topics

Popular Threads

This website is for information purposes only. By providing the information contained herein we are not diagnosing, treating, curing, mitigating, or preventing any type of disease or medical condition. Before beginning any type of natural, integrative or conventional treatment regimen, it is advisable to seek the advice of a licensed healthcare professional.

© Copyright 2008-2016 GreenMedInfo.com, Journal Articles copyright of original owners, MeSH copyright NLM.