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ENANTIOSELECTIVE PHARMACOKINETICS OF VERAPAMIL IN EIGHT HEALTHY CHINESE MALE VOLUNTEERS
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- Author:
- No author available
- Journal Title:
- ACTA PHARMACEUTICA SINICA
- Issue:
- 1
- DOI:
- 10.3321/j.issn:0513-4870.1999.01.004
- Key Word:
- 维拉帕米;去甲维拉帕米;对映体;药代动力学;毛细管电泳
Abstract： 目的: 考察维拉帕米(VPM)和去甲维拉帕米(NVPM)对映体的药代动力学特性. 方法: 8名汉族男性健康志愿者分别po外消旋VPM 80 mg和静滴5 mg,以三甲基-β-环糊精为手性选择剂,毛细管电泳法同时测定VPM和NVPM对映体的血浆浓度,用二房室开放模型拟合药-时曲线.结果: po VPM的R/S(AUC),R/S(CL)和R/S(Cmax)比率分别为3.66±1.86,0.3±0.053和4.82±0.58;NVPM的R/S(Cmax)和R/S(AUC)比率为2.58和2.36.iv VPM的R/S(AUC),R/S(CL)和R/S(Cmax)比率分别为1.04±0.29,1.01±0.3和1.36±0.12.R-(+)-VPM和S-(-)-VPM的绝对生物利用度为30.3±19和9.8±5.9.结论: VPM有较大的对映体特异性首过代谢,选择优对映体S-(-)-VPM为监测对象有利于临床合理使用外消旋VPM.
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