Walker O, Dawodu A H, Salako L A, Alván G, Johnson A O
Br J Clin Pharmacol. 1987 Apr;23(4):467-72. doi: 10.1111/j.1365-2125.1987.tb03077.x.
The single dose disposition of chloroquine was studied in five children with kwashiorkor and six normal control children after an oral dose of 10 mg kg-1 of chloroquine base. Plasma concentrations of chloroquine and its main metabolite were assayed by high performance liquid chromatography (h.p.l.c.). Chloroquine was detectable for up to 21 days in all the subjects. Chloroquine was detectable in all the subjects within 30 min after giving the drug except in one subject. Peak levels were reached between 0.5 and 8 h in all the subjects (with no significant difference in the tmax between the two groups of children). Peak plasma chloroquine concentrations in the children with kwashiorkor varied from 9 ng ml-1 to 95 ng ml-1 (mean 40 +/- 34 ng ml-1). Peak chloroquine concentrations in the controls varied between 69 ng ml-1 and 330 ng ml-1 (mean 134 +/- 99 ng ml-1). The mean AUC in the kwashiorkor children was significantly lower than the mean AUC in the control children (P less than 0.001). Peak plasma desethylchloroquine concentrations in the children with kwashiorkor varied between 3 and 13 ng ml-1 (mean 6 +/- 9 ng ml-1) while in the controls the concentrations varied between 14 and 170 ng ml-1 (mean 50 +/- 61 ng ml-1). There was no significant difference in the half-life of chloroquine between the kwashiorkor children and the normal control children. The possible influence of a different binding and distribution pattern of chloroquine in kwashiorkor could not be assessed in this study.(ABSTRACT TRUNCATED AT 250 WORDS)
对5名夸休可尔症患儿和6名正常对照儿童口服10 mg/kg氯喹碱基后,研究了氯喹的单剂量处置情况。采用高效液相色谱法(HPLC)测定血浆中氯喹及其主要代谢物的浓度。所有受试者中氯喹在长达21天内均可检测到。给药后30分钟内,除一名受试者外,所有受试者均可检测到氯喹。所有受试者在0.5至8小时内达到峰值水平(两组儿童的达峰时间无显著差异)。夸休可尔症患儿血浆氯喹峰值浓度在9 ng/ml至95 ng/ml之间(平均40±34 ng/ml)。对照组氯喹峰值浓度在69 ng/ml至330 ng/ml之间(平均134±99 ng/ml)。夸休可尔症患儿的平均曲线下面积显著低于对照儿童(P<0.001)。夸休可尔症患儿血浆去乙基氯喹峰值浓度在3 ng/ml至13 ng/ml之间(平均6±9 ng/ml),而对照组浓度在14 ng/ml至170 ng/ml之间(平均50±61 ng/ml)。夸休可尔症患儿和正常对照儿童氯喹的半衰期无显著差异。本研究无法评估氯喹在夸休可尔症中不同结合和分布模式的可能影响。(摘要截短至250字)