5－单硝基异山梨醇酯片在正常人体的药代动力学和生物利用度的研究  

A PHARMACOKINETIC AND BIOAVAILABILITY STUDY IN HEALTHY VOLUNTEERS BEING GIVEN ORAL DOSE ON ISOSORBIDE 5-MONONITRATE

作　　者：赵奕[1] 周莹[1] 袁虹 阮邹荣[1] 单江[1] 

机构地区：[1]浙江医科大学临床药理研究所

出　　处：《中国临床药理学杂志》1995年第1期33-37,共5页The Chinese Journal of Clinical Pharmacology

摘　　要：本文报道了应用毛细管气相色谱法以ＥＣＤ（Ｎｉ－６３）为检测器，采用外标法测定人血浆中的５－单硝基异山梨醇酯（ＩＳ－５－ＭＮ）．结果表明该方法精密度好，灵敏度高，线性关系良好；ｒ＝０．９９９９（ｎ＝６），最低检测限为０．０３ｎｇ，日内和日间平均变异系数＜６％。１０名健康志愿者口服国产和进口ＩＳ－５－ＭＮ片所得的药时曲线均符合二室模型，其药代动力学参数无显著性差异。吸收速率常数分别为４．６９，４．９１ｈ￣－１；达峰时间为０．８９，０．８１ｈ；峰浓度为２２５．１８，２２２．８０μｇ／ｌ；半衰期Ｔ１／２β为５．６０，５．６１ｈ；表观分布容积为０．０６３和０．０７０１；平均总体清除率为１３．０１和１２．４０１／ｈ，生物利用度Ｆ＝９８．２８±９．７６％。The concentration of isosorbide 5-minonitrate in human plasma were determined by capillary column gas-liquid chromatography. This method has high selectivity and reproducibility. The relation between hight and concentration was very good r=0.9999. The limit of detection was 0.03 ng. The average of within-day and without-day CV was<5 %.The curve of concertration-time fitted a two-compartment open model after oral dose of 1 tablet of Chinese-made and Holland-made of isosorbide 5-minonitrate (20 mg/tablet) in the healthy, The result of pharmacokinetics of them has no difference. Ka were 4. 69, 4. 91 h-1 respectively, Cmax were 225.18,222.80μg/l, T1/2βwere 5.60and 5.61; Vd were 0.063 and 0.070 L; Cls were 13.01 and 12.401/h . The bioequivalence F= 98.28 ±9.76%.

关 键 词：异山梨醇酯 气相色谱法 药代动力学 生物利用度 

分 类 号：R972.3[医药卫生—药品]