https://scholars.lib.ntu.edu.tw/handle/123456789/565070
標題: | Interaction between red yeast rice and CYP450 enzymes/P-glycoprotein and its implication for the clinical pharmacokinetics of lovastatin | 作者: | Chen C.-H. Uang Y.-S. Wang S.-T. JYH-CHIN YANG CHUN-JUNG LIN |
公開日期: | 2012 | 卷: | 2012 | 起(迄)頁: | 127043 | 來源出版物: | Evidence-based Complementary and Alternative Medicine | 摘要: | Red yeast rice (RYR) can reduce cholesterol through its active component, lovastatin. This study was to investigate the pharmacokinetic properties of lovastatin in RYR products and potential RYR-drug interactions. Extracts of three registered RYR products (LipoCol Forte, Cholestin, and Xuezhikang) were more effective than pure lovastatin in inhibiting the activities of cytochrome P450 enzymes and P-glycoprotein. Among CYP450 enzymes, RYR showed the highest inhibition on CYP1A2 and CYP2C19, with comparable inhibitory potencies to the corresponding typical inhibitors. In healthy volunteers taking the RYR product LipoCol Forte, the pharmacokinetic properties of lovastatin and lovastatin acid were linear in the dose range of 1 to 4 capsules taken as a single dose and no significant accumulation was observed after multiple dosing. Concomitant use of one LipoCol Forte capsule with nifedipine did not change the pharmacokinetics of nifedipine. Yet, concomitant use of gemfibrozil with LipoCol Forte resulted in a significant increase in the plasma concentration of lovastatin acid. These findings suggest that the use of RYR products may not have effects on the pharmacokinetics of concomitant comedications despite their effects to inhibit the activities of CYP450 enzymes and P-gp, whereas gemfibrozil affects the pharmacokinetics of lovastatin acid when used concomitantly with RYR products. Copyright ? 2012 Chia-Hao Chen et al. |
URI: | https://www.scopus.com/inward/record.uri?eid=2-s2.0-84871447117&doi=10.1155%2f2012%2f127043&partnerID=40&md5=20785a52eeae904a5968e0ed992b2e55 https://scholars.lib.ntu.edu.tw/handle/123456789/565070 |
ISSN: | 1741427X | DOI: | 10.1155/2012/127043 | SDG/關鍵字: | acid; cholestin; cytochrome P450; cytochrome P450 1A2; cytochrome P450 2B6; cytochrome P450 2C19; cytochrome P450 2C9; cytochrome P450 2D6; cytochrome P450 3A4; drug metabolite; gemfibrozil; lipocol forte; lovastatin acid; mevinolin; multidrug resistance protein; nifedipine; unclassified drug; xuezhikang; adult; area under the curve; article; controlled study; drug blood level; drug clearance; drug distribution; drug dose escalation; drug half life; drug potency; enzyme inhibition; evening dosage; human; maximum plasma concentration; mean residence time; morning dosage; normal human; plasma concentration-time curve; priority journal; randomized controlled trial; single drug dose; time to maximum plasma concentration |
顯示於: | 藥學系 |
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