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- Title
The Effect of Herbal Medicine Baicalin on Pharmacokinetics of Rosuvastatin, Substrate of Organic Anion-transporting Polypeptide 1B1.
- Authors
Fan, L.; Zhang, W.; Guo, D.; Tan, Z-R.; Xu, P.; Li, Q.; Liu, Y-Z.; Zhang, L.; He, T-Y.; Hu, D-L.; Wang, D.; Zhou, H-H.
- Abstract
The aim of this study was to explore potential herb–drug interaction between baicalin and rosuvastatin, a typical substrate for organic anion-transporting polypeptide 1B1 (OATP1B1) related to different OATP1B1 haplotype groups. Eighteen unrelated healthy volunteers who were CYP2C9*1/*1 with different OATP1B1 haplotypes (six OATP1B1*1b/*1b, six OATP1B1*1b/*15, and six OATP1B1*15/*15) were selected to participate in this study. Rosuvastatin (20 mg orally) pharmacokinetics after coadministration of placebo and 50-mg baicalin tablets (three times daily orally for 14 days) were measured for up to 72 h by liquid chromatography–mass spectrometry in a two-phase randomized crossover study. After baicalin treatment, the area under the plasma concentration–time curve (AUC)(0–72) and AUC(0–∞) of rosuvastatin decreased by 47.0±11.0% (P=0.001) and 41.9±7.19% (P=0.001) in OATP1B1*1b/*1b, 21.0±20.6% (P=0.035) and 23.9±8.66% (P=0.004) in OATP1B1*1b/*15, and 9.20±11.6% (P=0.077) and 1.76±4.89% (P=0.36) in OATP1B1*15/*15, respectively. Moreover, decreases of both AUC(0–72) and AUC(0–∞) of rosuvastatin among different haplotype groups were significantly different (P=0.002 and <0.001). Baicalin reduces plasma concentrations of rosuvastatin in an OATP1B1 haplotype–dependent manner.Clinical Pharmacology & Therapeutics (2008) 83, 3, 471–476.doi:10.1038/sj.clpt.6100318
- Subjects
HERBAL medicine; DRUG side effects; PHARMACOKINETICS; THERAPEUTICS; PHYSIOLOGICAL effects of chemicals
- Publication
Clinical Pharmacology & Therapeutics, 2008, Vol 83, Issue 3, p471
- ISSN
0009-9236
- Publication type
Article
- DOI
10.1038/sj.clpt.6100318