食物-药物相互作用：辣椒素对辛伐他汀及其在大鼠体内的活性代谢物药代动力学的影响。
Food-drug interactions: effect of capsaicin on the pharmacokinetics of simvastatin and its active metabolite in rats.
机构信息
Department of Pharmacy, Union Hospital, Huazhong University of Science and Technology, Wuhan 430022, People's Republic of China.
出版信息
Food Chem Toxicol. 2013 Mar;53:168-73. doi: 10.1016/j.fct.2012.11.045. Epub 2012 Dec 5.
Capsaicin (trans-8-methy-N-vanilly-6-nonenamide, CAP), the main ingredient responsible for the hot pungent taste of chilli peppers. However, little is known about the metabolic interactions between CAP and clinically used drugs. This study attempted to investigate the effect of CAP on the pharmacokinetics of simvastatin (SV), a cytochrome P450 (CYP) 3A substrate and an important cholesterol-lowering agent. CAP (3, 8 or 25 mg/kg), ketoconazole, dexamethasone or 5% CMC-Na was given to rats for seven consecutive days and on the seventh day SV (80 mg/kg) was administered orally. The results showed that when a single dose of SV was administered to rats fed with CAP over one week, AUC(0→∞), C(max) of SV and its acid metabolite was significantly decreased in comparison to the control treatment. Pretreatment of rats with CAP resulted in an decrease in the AUC(0-∞) of SV of about 67.06% (CAP 3 mg/kg, P<0.05), 73.21% (CAP 8 mg/kg, P<0.01) and 77.49% (CAP 25 mg/kg, P<0.01) compared with the control group. The results demonstrate that chronic ingestion of high doses of CAP will decrease the bioavailability of SV to a significant extent in rats.
辣椒素（反式-8-甲基-N-香草基-6-壬酰胺，CAP）是导致辣椒辛辣味的主要成分。然而，关于 CAP 与临床使用的药物之间的代谢相互作用知之甚少。本研究试图探讨 CAP 对辛伐他汀（SV）药代动力学的影响，SV 是细胞色素 P450（CYP）3A 的底物，也是一种重要的降胆固醇药物。CAP（3、8 或 25mg/kg）、酮康唑、地塞米松或 5%CMC-Na 连续 7 天给予大鼠，第 7 天给予 SV（80mg/kg）口服。结果表明，当单剂量 SV 给予 CAP 喂养一周的大鼠时，与对照处理相比，SV 的 AUC（0→∞）、C（max）及其酸代谢物显著降低。CAP 预处理大鼠使 SV 的 AUC（0-∞）减少约 67.06%（CAP 3mg/kg，P<0.05）、73.21%（CAP 8mg/kg，P<0.01）和 77.49%（CAP 25mg/kg，P<0.01）与对照组相比。结果表明，大鼠长期摄入高剂量 CAP 会显著降低 SV 的生物利用度。
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