Na-Bangchang K, Limpaibul L, Thanavibul A, Tan-Ariya P, Karbwang J
Clinical Pharmacology Unit, Faculty of Tropical Medicine, Mahidol University, Bangkok, Thailand.
Br J Clin Pharmacol. 1994 Sep;38(3):278-81. doi: 10.1111/j.1365-2125.1994.tb04354.x.
The pharmacokinetics of chloroquine (CQ) and desethylchloroquine (DECQ) were studied in seven male Thai patients with P. vivax malaria and seven healthy male Thais, after the standard oral dosage regimen of CQ (a total dose of 1500 mg given over 3 days). All patients showed a rapid initial response to the treatment with median (range) values of fever and parasite clearance times of 13.7 (2-47) and 58 (33-38) h, respectively. In the patients, the median range Cmax value was significantly higher (1547 (996-2446) vs 838 (656-1587) ng ml-1), and AUC(0,28d) was greater (281 (250-515) vs 122 (103-182) micrograms ml-1 h). In addition, the median (AUC(0,28d) of DECQ was significantly greater (170 (72-265) vs 77 (49-140) micrograms ml-1 h). The AUC(0,28d) ratio of DECQ to CQ in patients was significantly higher than that in healthy subjects (0.67 (0.43-0.90) vs 0.51 (0.29-0.61)).
对7名患间日疟原虫疟疾的泰国男性患者和7名健康泰国男性给予氯喹（CQ）标准口服给药方案（3天内共给予1500mg）后，研究了氯喹（CQ）和去乙基氯喹（DECQ）的药代动力学。所有患者对治疗均表现出快速的初始反应，发热和寄生虫清除时间的中位数（范围）分别为13.7（2 - 47）小时和58（33 - 38）小时。患者的Cmax值中位数范围显著更高（1547（996 - 2446）对838（656 - 1587）ng/ml），且AUC(0,28d)更大（281（250 - 515）对122（103 - 182）μg/ml·h）。此外，DECQ的AUC(0,28d)中位数显著更大（170（72 - 265）对77（49 - 140）μg/ml·h）。患者中DECQ与CQ的AUC(0,28d)比值显著高于健康受试者（0.67（0.43 - 0.90）对0.51（0.29 - 0.61））。
