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The effect of herbal medicine baicalin on pharmacokinetics of rosuvastatin, substrate of organic anion-transporting polypeptide 1B1.
Clin Pharmacol Ther. 2008 Mar; 83(3):471-6.CP

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-infinity) 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-infinity) 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.

Authors+Show Affiliations

Pharmacogenetics Research Institute, Central South University, Changsha, Hunan, People's Republic of China.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article
Randomized Controlled Trial
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

17851565

Citation

Fan, L, et al. "The Effect of Herbal Medicine Baicalin On Pharmacokinetics of Rosuvastatin, Substrate of Organic Anion-transporting Polypeptide 1B1." Clinical Pharmacology and Therapeutics, vol. 83, no. 3, 2008, pp. 471-6.
Fan L, Zhang W, Guo D, et al. The effect of herbal medicine baicalin on pharmacokinetics of rosuvastatin, substrate of organic anion-transporting polypeptide 1B1. Clin Pharmacol Ther. 2008;83(3):471-6.
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. (2008). The effect of herbal medicine baicalin on pharmacokinetics of rosuvastatin, substrate of organic anion-transporting polypeptide 1B1. Clinical Pharmacology and Therapeutics, 83(3), 471-6.
Fan L, et al. The Effect of Herbal Medicine Baicalin On Pharmacokinetics of Rosuvastatin, Substrate of Organic Anion-transporting Polypeptide 1B1. Clin Pharmacol Ther. 2008;83(3):471-6. PubMed PMID: 17851565.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - The effect of herbal medicine baicalin on pharmacokinetics of rosuvastatin, substrate of organic anion-transporting polypeptide 1B1. AU - Fan,L, AU - Zhang,W, AU - Guo,D, AU - Tan,Z-R, AU - Xu,P, AU - Li,Q, AU - Liu,Y-Z, AU - Zhang,L, AU - He,T-Y, AU - Hu,D-L, AU - Wang,D, AU - Zhou,H-H, Y1 - 2007/09/12/ PY - 2007/9/14/pubmed PY - 2008/3/14/medline PY - 2007/9/14/entrez SP - 471 EP - 6 JF - Clinical pharmacology and therapeutics JO - Clin Pharmacol Ther VL - 83 IS - 3 N2 - 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-infinity) 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-infinity) 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. SN - 1532-6535 UR - https://www.unboundmedicine.com/medline/citation/17851565/The_effect_of_herbal_medicine_baicalin_on_pharmacokinetics_of_rosuvastatin_substrate_of_organic_anion_transporting_polypeptide_1B1_ L2 - https://doi.org/10.1038/sj.clpt.6100318 DB - PRIME DP - Unbound Medicine ER -