国产注射用盐酸米诺环素人体药动学研究.doc

1 国产注射用盐酸米诺环素人体药动学研究作者: 王华丽黄文祥盛家琦【关键词】注射用盐酸米诺环素; ,, 药动学; , 反相高效液相色谱法摘要: 目的研究国产注射用盐酸米诺环素人体内的药动学特征,为临床提供合理给药方案。方法 12 名健康志愿者随机分成 3组, 采用 3×3 的交叉设计, 每人单剂量分别静脉给予 100 、 200 和 300mg 注射用盐酸米诺环素, 2h 衡速滴完, 分别在给药前和给药后 0、 025 、 05、 075 、1、 15、2、 4、6、8、 12、 24、 48、 72h 取血。每次间隔一周。采用高效液相色谱法测定血清中米诺环素浓度。结果用 3P97 程序计算其药动学参数。单次静脉注射盐酸米诺环素 100 、 200 和 300mg , 药动学参数 cmax 分别为(311 ± 067) μ g/ml 、(709 ± 189) μ g/ml 及(1180 ± 285) μ g/ml ; AUC 分别为(5098 ± 1365) μ gh/ml 、(9385 ± 1782) μ gh/ml 及(16360 ± 3169) μ gh/ml ; t1/2 α分别为(113 ± 062)h 、(075 ± 044)h 及(071 ± 041)h ; t1/2 β分别为(1784 ± 597)h 、(1405 ± 260)h 及(1416 ± 172)h ; CLs 分别为(211 ± 063)L/h 、(220 ± 040)L/h 及 2 (190 ± 034)L/h ; Vc 分别为(2544 ± 617)L 、(1948 ± 940)L 及(1803 ± 724)L 。结论注射用盐酸米诺环素在人体内的药动学符合二室模型特征。关键词: 注射用盐酸米诺环素; 药动学; 反相高效液相色谱法 ics of minocycline hydrochloride for injection in healthy human ABSTRACT Objective To study the ics of minocycline hydrochloride for injection in healthy human. Methods Twelve healthy volunteers were selected to recEive a single dose of minocycline 100, 200 and 300mg within 2h infusion in an open randomized threefold crossover study. The re was a week washout in every project. Blood samples were taken for detecting serum concentration before administration and at 0, 025, 05, 075, 1, 15, 2, 4, 6, 8, 12, 24, 48, 72h pletion of the intravenous infusion. The concentrations of minocycline in serum were determined bya highpressure liquid chromatography (HPLC) method. Results ic profiles were conformed to an open partment model 3 analyzed by using 3P97 and the result of HPLC method were as follows: the Cmax of 100, 200, 300mg minocycline at the end of infusion were (311 ± 067) μ g/ml, (709 ± 189) μ g/ml and (1180 ± 285) μ g/ml; the AUCs were (5098 ± 1365) μ gh/ml, (9385 ± 1782) μ gh/ml and (16360 ± 3169) μ gh/ml; the t1/2 α were (113 ± 062) h, (075 ± 044)h and (071 ± 041)h; the t1/2 β were (1784 ± 597)h, (1405 ± 260)h and (1416 ± 172)h; the CLs were (211 ± 063)L/h, (220 ± 040)L/h and (190 ± 034)L/h; the Vc were (2544 ±