Wetsteyn J C, De Vries P J, Oosterhuis B, Van Boxtel C J
Division of Infectious Diseases, Tropical Medicine and AIDS, Academic Medical Center, Amsterdam, The Netherlands.
Br J Clin Pharmacol. 1995 Jun;39(6):696-9. doi: 10.1111/j.1365-2125.1995.tb05731.x.
The pharmacokinetics of chloroquine were studied in healthy volunteers who received one of three different multiple-dose regimens for 3 weeks: once weekly 300 mg, twice weekly 200 mg and once daily 50 mg chloroquine. Plasma concentrations of chloroquine and metabolites were determined by h.p.l.c. with fluorescence detection. The concentration-time course was fitted to a multiple-dose pharmacokinetic model. Volume of distribution, elimination half-life and clearance were not different for the three regimens, ranging from 250-302 l kg-1, 374-479 h and 0.44-0.58 l h-1 kg-1 respectively. After the first week of all dosage regimens, peak and trough concentrations of chloroquine were above 16 micrograms l-1, sufficiently suppressive for chloroquine-sensitive P. falciparum strains. These data suggest that once daily chloroquine could be combined with proguanil in a single tablet and should improve compliance when given for malaria chemoprophylaxis.
在健康志愿者中研究了氯喹的药代动力学，这些志愿者接受了三种不同的多剂量给药方案之一，为期3周：每周一次300毫克、每周两次200毫克和每日一次50毫克氯喹。氯喹及其代谢物的血浆浓度通过带有荧光检测的高效液相色谱法测定。浓度-时间过程拟合到多剂量药代动力学模型。三种给药方案的分布容积、消除半衰期和清除率没有差异，分别为250 - 302升/千克、374 - 479小时和0.44 - 0.58升/小时·千克。在所有给药方案的第一周后，氯喹的峰浓度和谷浓度均高于16微克/升，对氯喹敏感的恶性疟原虫菌株具有足够的抑制作用。这些数据表明，每日一次的氯喹可以与氯胍制成单片制剂，在用于疟疾化学预防时应能提高依从性。
