Aderounmu A F, Salako L A, Lindström B, Walker O, Ekman L
Br J Clin Pharmacol. 1986 Nov;22(5):559-64. doi: 10.1111/j.1365-2125.1986.tb02935.x.
The pharmacokinetics of chloroquine were studied after intramuscular and intravenous administration of the drug to healthy African adults. Chloroquine was analysed in plasma using an h.p.l.c. method and pharmacokinetic parameters were derived from the concentration-time data using a non-linear computer programme. A two-compartment open model was assumed. Chloroquine was rapidly absorbed from an intramuscular site, producing a plasma concentration-time profile similar to that obtained after a 15 min i.v. infusion of a comparable dose. The pharmacokinetics of chloroquine after i.m. and i.v. administration were characterised by a long half-life and a very large volume of distribution. There was no significant difference between the values of each parameter obtained from the different routes. It is suggested that the high Cmax obtained after i.m. and i.v. administration of chloroquine might contribute to its toxicity when these routes are used in treatment.
在健康非洲成年人中，对氯喹进行肌肉注射和静脉注射后，研究了其药代动力学。采用高效液相色谱法分析血浆中的氯喹，并使用非线性计算机程序从浓度 - 时间数据中得出药代动力学参数。假定为二室开放模型。氯喹从肌肉注射部位迅速吸收，产生的血浆浓度 - 时间曲线与静脉注射相当剂量15分钟后的曲线相似。肌肉注射和静脉注射后氯喹的药代动力学特征为半衰期长和分布容积非常大。从不同给药途径获得的各参数值之间无显著差异。有人提出，当采用这些给药途径进行治疗时，肌肉注射和静脉注射氯喹后获得的高血药峰浓度可能会导致其毒性。
