Karbwang J, Bunnag D, Breckenridge A M, Back D J
Eur J Clin Pharmacol. 1987;32(2):173-7. doi: 10.1007/BF00542191.
The kinetics of mefloquine were studied in 12 healthy Thai male and 12 healthy Thai female volunteers. Mefloquine (MQ) was administered either alone (750 mg orally) or in combination (MSP) with sulphadoxine (1.5 g) and pyrimethamine (75 mg) to each of 6 male and 6 female subjects. Plasma concentrations of MQ were measured by HPLC at intervals for 42 days. There was considerable interindividual variability in the pharmacokinetic parameters; for example in the male subjects receiving MQ alone peak concentrations ranged between 638 and 2494 ng X ml-1 with a mean concentration of 1442 ng X ml-1. Compared to previously published data on MQ concentrations in Caucasian male subjects, the present study indicates that higher concentrations are achieved in Thai subjects. The only significant difference in kinetic parameters between male and female subjects receiving MQ alone was in the mean residence time (MRT) which was greater in females. However, an analysis of pharmacokinetic parameters following administration of the combination preparation showed that the time to peak (tmax) was significantly reduced in females receiving MSP compared to the corresponding females given MQ alone and males given MSP. When data obtained from all subjects (male and female) receiving either MQ alone or MSP were combined, both MRT and half-life were significantly greater in subjects given MSP. There is therefore some evidence that therapeutic concentrations of MQ are maintained for a longer period of time following MSP administration.
在12名健康泰国男性和12名健康泰国女性志愿者中研究了甲氟喹的动力学。给6名男性和6名女性受试者分别单独服用甲氟喹（MQ，口服750 mg）或与磺胺多辛（1.5 g）和乙胺嘧啶（75 mg）联合服用（MSP）。每隔一段时间用高效液相色谱法（HPLC）测量血浆中甲氟喹的浓度，持续42天。药代动力学参数存在相当大的个体间差异；例如，单独接受甲氟喹的男性受试者的峰值浓度在638至2494 ng·ml⁻¹之间，平均浓度为1442 ng·ml⁻¹。与先前发表的关于高加索男性受试者中甲氟喹浓度的数据相比，本研究表明泰国受试者体内达到的浓度更高。单独接受甲氟喹的男性和女性受试者在动力学参数上唯一的显著差异在于平均驻留时间（MRT），女性的平均驻留时间更长。然而，对联合制剂给药后的药代动力学参数分析表明，与单独接受甲氟喹的相应女性和接受MSP的男性相比，接受MSP的女性的达峰时间（tmax）显著缩短。当将单独接受甲氟喹或MSP的所有受试者（男性和女性）的数据合并时，接受MSP的受试者的MRT和半衰期均显著延长。因此，有证据表明服用MSP后甲氟喹的治疗浓度能维持更长时间。
