甲氟喹在人体中的分次给药动力学。
Divided-dose kinetics of mefloquine in man.
作者信息
Franssen G, Rouveix B, Lebras J, Bauchet J, Verdier F, Michon C, Bricaire F
机构信息
Departement de Pharmacologie Clinique, INSERM U13, Hôpital Claude Bernard, Paris, France.
出版信息
Br J Clin Pharmacol. 1989 Aug;28(2):179-84. doi: 10.1111/j.1365-2125.1989.tb05413.x.
Abstract
The kinetics of mefloquine was investigated following oral divided-doses in 10 healthy Caucasian volunteers. They received 500 or 750 mg followed by 500 mg 8 h later. Unchanged mefloquine (M) and its carboxylic acid metabolite (MM) were measured in whole blood and plasma for 50 days by h.p.l.c. Maximum blood and plasma M concentrations of 1872 +/- 362 ng ml-1 (mean +/- s.d.) and 1900 +/- 434 ng ml-1, respectively, were found within 6-10 h after the second dose. The terminal plasma elimination half-life was 20.1 +/- 3.7 days (mean +/- s.d.) and the oral clearance was 22.3 +/- 6.7 ml h-1 kg-1 (mean +/- s.d.). Plasma concentrations of MM exceeded those of M by 2-3 fold within 2 days. The whole blood concentration of MM was lower than that in plasma but also exceeded the whole blood concentration of M.
摘要
在10名健康的白种志愿者中，口服分次给药后研究了甲氟喹的动力学。他们先接受500或750毫克剂量，8小时后再接受500毫克剂量。通过高效液相色谱法在全血和血浆中测量未改变的甲氟喹（M）及其羧酸代谢物（MM）达50天。第二次给药后6 - 10小时内，全血和血浆中M的最大浓度分别为1872±362纳克/毫升（平均值±标准差）和1900±434纳克/毫升。血浆终末消除半衰期为20.1±3.7天（平均值±标准差），口服清除率为22.3±6.7毫升/小时/千克（平均值±标准差）。2天内血浆中MM的浓度超过M的浓度2 - 3倍。全血中MM的浓度低于血浆中的浓度，但也超过了全血中M的浓度。
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本文引用的文献
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Chemotherapy. 1982;28(1):70-84. doi: 10.1159/000238062.
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