摘要
目的 观察反复摄入3种柑桔类果汁对阿托伐他汀（ATV）在健康受试者体内药动学的影响。方法 采用4周期交叉自身对照试验设计，洗脱期为2周。24名健康受试者随机分为4组，每组6人，分别给予220 mL葡萄柚汁，220 mL橙汁，220 mL桔汁和220 mL水，1 d 3次，共服用2 d。于第3天分别用220 mL葡萄柚汁，220 mL橙汁，220 mL桔汁和220 mL水送服单剂量10 mg ATV片，服药后0.5和1.5 h 再分别服用220 mL葡萄柚汁，220 mL橙汁，220 mL桔汁和220 mL水，于服药后48 h内检测ATV血浆浓度。 结果 与对照组水相比，服用葡萄柚汁使阿托伐他汀酸的AUC0-∞增加8％(P>0.05)，ρmax降低8％(P>0.05)；服用橙汁使阿托伐他汀酸的AUC0-∞降低10％（P>0.05），ρmax降低27％（P>0.05）；服用桔汁使阿托伐他汀酸的AUC0-∞降低13％（P>0.05），ρmax降低15％（P>0.05）。 结论 3种果汁未显著影响健康受试者体内ATV的药动学过程。
Abstract
OBJECTIVE To investigate the effects of three kinds of juices of mandarinorange on the pharmacokinetics of atorvastatin in healthy volunteers. METHODS A self-controlled， crossover study was designed with four phases and a washout period of 2 weeks. 24 Healthy volunteers were divided into 4 groups randomly， 6 in each group. For 2 d prior to the study-drug administration， 220 mL of grapefruit juice(GFJ)， sweet orange juice， mandarin orange juice or water was given to volunteers of each group three times daily .On the third day，a single dose of 10 mg atorvastatin was orally administered with GFJ, sweet orange juice， mandarin orange juice or water. The additional 220 mL of GFJ， sweet orange juice， mandarin orange juice or water was taken at 0.5 and 1.5 h after administration of atorvastatin.The plasma concentration of atorvastatin was determined at 48 h after dosing. RESULTS Compared with the water group， the AUC0-∞ of atorvastatin acid was increased by 8％(P>0.05)， ρmax was decreased by 8％(P>0.05)，in the group treated with GFJ；the AUC0-∞and ρmax of atorvastatin acid group were decreased by 10％（P>0.05）and 27％（P>0.05） in the group treated with sweet orange juice; the AUC0-∞and ρmax of atorvastatin acid were decreased by 13％（P>0.05）and 15％（P>0.05） in the group treated with mandarin orange juice. CONCLUSION Three kinds of juice showed no significantly influence on the pharmacokinetics of atorvastatin in healthy subjects.
关键词
柑桔类果汁 /
阿托伐他汀 /
药动学
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Key words
mandarin orange juice /
atorvastatin /
pharmacokinetics
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胡晓玲 梁玉岗 朱荣华 李焕德.
中国产3种柑桔类果汁对阿托伐他汀人体内药动学影响的研究[J]. 中国药学杂志, 2010, 45(3): 206-213
HU Xio-ling;LING Yu-gng;ZHU Rong-hu;LI Hun-de.
Effects of Three Kinds of Juice of Mandarinorange on Pharmacokinetics of Atorvastatin in Healthy Volunteers[J]. Chinese Pharmaceutical Journal, 2010, 45(3): 206-213
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