Effect of quercetin on the pharmacokinetics of oral cyclosporine
Effect of quercetin on the pharmacokinetics of oral cyclosporine
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DOI：
10.1093/ajhp/61.22.2406
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发表时间：
2004-11-15
影响因子：
2.7
通讯作者：
Choi, KE
中科院分区：
文献类型：
--
作者：
Choi, JS;Choi, BC;Choi, KE
为了研究槲皮素对口服环孢素[环孢素]药代动力学的影响，对8名根据病史、心电图、实验室检测和体检确定为健康的男性志愿者（来自韩国）进行了测试。治疗包括：对照（单次口服剂量300 mg环孢素），服用5 mg槲皮素/kg后30分钟施用环孢素（预处理A），每天两次施用槲皮素，持续3天，然后单次口服剂量环孢素（预处理B）。在0、0.5、1、2、3、4、8、12和24小时时抽取血样。在静脉注射中。组单剂量环孢素（100mg溶于50ml 0.9%氯化钠注射液）静脉滴注30分钟，测定药物绝对生物利用度。在输注结束后立即0、15和30分钟以及输注开始后1、2、4、8、12和24小时采集血样。两个预处理组的环孢素浓度均高于对照组。预处理B组环孢素的半衰期明显长于对照组。预处理组达到环孢素最大浓度所需的时间并不明显长于对照组。对照组环孢素的平均绝对生物利用度为 36.3%，预处理 A 组为 49.4%，预处理 B 组为 54.2%。
To investigate the effect of quercetin on the pharmacokinetics of oral cyclosporine [ciclosporin], 8 male volunteers (from Korea Republic) determined as healthy based on medical history, electrocardiography, laboratory testing and physical examination were tested. Treatments comprised: control (single oral dose of 300 mg cyclosporine), administration of cyclosporine 30 minutes after taking 5 mg quercetin/kg (pretreatment A), administration of quercetin twice daily for 3 days followed by a single oral dose of cyclosporine (pretreatment B). Blood samples were withdrawn at 0, 0.5, 1, 2, 3, 4, 8, 12 and 24 h. In the i.v. group, a single dose of cyclosporine (100 mg in 50 ml of 0.9% sodium chloride injection) was infused intravenously for 30 minutes to determine the drug absolute bioavailability. Blood samples were obtained at 0, 15 and 30 minutes immediately after the end of infusion and 1, 2, 4, 8, 12 and 24 h after the start of infusion. Cyclosporine concentrations in both pretreatment groups were higher than in the control group. The half life of cyclosporine in pretreatment group B was significantly longer than in the control group. The time needed to reach the maximum concentration of cyclosporine in the pretreatment groups was not significantly longer than in the control group. The mean absolute bioavailability of cyclosporine was 36.3% in the control group, versus 49.4% in the pretreatment group A and 54.2% in pretreatment group B.