Schwartz D E, Eckert G, Ekue J M
Biological Pharmaceutical Research Department, F. Hoffmann-La Roche & Co. Ltd., Basel, Switzerland.
Chemotherapy. 1987;33(5):305-8. doi: 10.1159/000238513.
Because of the extremely long terminal elimination half-life of mefloquine it is practically impossible to measure quantitatively its urinary excretion after a single dose. Indeed, a correct estimation would require collection of urine over a period of several months. This difficulty was overcome by measuring excretion in the course of a multiple-dose study when steady-state conditions had been reached. Six male African volunteers were given at an interval of 1 week 250 mg mefloquine base in the form of its hydrochloride. Urine was quantitatively collected from each subject during the 11th week and analyzed for unchanged drug and its alcohol and acid metabolites. Excretion of the unchanged drug and of its acid metabolite amounted respectively to 9% (5.2-13.1%) and 4.2% (2.9-6.2%) of the weekly dose. Concentrations of the alcohol metabolite were too low to be measured.
由于甲氟喹的终末消除半衰期极长，单次给药后几乎不可能对其尿排泄进行定量测定。实际上，要进行准确估算需要收集数月的尿液。在多剂量研究达到稳态条件时通过测量排泄克服了这一困难。6名非洲男性志愿者每隔1周服用250mg盐酸甲氟喹碱。在第11周从每个受试者定量收集尿液，并分析其中未变化的药物及其醇和酸代谢产物。未变化药物及其酸代谢产物的排泄量分别相当于每周剂量的9%（5.2 - 13.1%）和4.2%（2.9 - 6.2%）。醇代谢产物的浓度过低无法测量。
