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目的研究单次口服莫达芬尼片的药代动力学。方法选择9名健康成年男性受试者分别单次口服100,200,300mg 3个剂量的莫达芬尼片后,用HPLC法测定血中原形药莫达芬尼及代谢产物莫达芬尼酸浓度,用3P97软件进行数据处理,计算药代动力学参数。结果原形药莫达芬尼的药-时曲线符合二房室模型,其主要药代动力学参数的Cmax、AUC0-∞、AUC0-t随剂量加大而增加;t1/2b、tmax、b、CL与给药剂量无关。莫达芬尼片原形药经肾排泄较少,48h经肾累积排泄率分别为(4.44±4.28)%,(3.35±2.20)%和(2.86±1.39)%。主要代谢产物莫达芬尼酸药-时曲线符合二房室模型,48h莫达芬尼酸经肾累积排泄率分别为(33.51±18.90)%,(32.36±19.92)%和(22.88±6.89)%。结论莫达芬尼在100～300mg内,呈线性动力学特征而无饱和性,其消除过程是经肝脏代谢,代谢产物为莫达芬尼酸,代谢产物主要经肾排泄。
Objective To study the pharmacokinetics of a single oral modafinil tablet. Methods Nine healthy adult male subjects were given a single oral dose of 100, 200, and 300 mg, respectively, of the modalfenib tablets. The concentrations of modafinil and its metabolite modafinil in the blood were measured by HPLC. 3P97 software for data processing, calculation of pharmacokinetic parameters. Results The drug-time curve of the prototype form of modafinil conformed to the two-compartment model and the main pharmacokinetic parameters of Cmax, AUC0-∞ and AUC0-t increased with dose increase; t1 / 2b, tmax, b, CL Has nothing to do with the dose. Modal pill tablets were less excreted by the kidneys, and the accumulated excretion rate of renal viablens at 48h were (4.44 ± 4.28)%, (3.35 ± 2.20)% and (2.86 ± 1.39)%, respectively. The main metabolite modafinil-time curve accorded with two-compartment model. The cumulative excretion rate of modafinil by renal in 48h was (33.51 ± 18.90)%, (32.36 ± 19.92)% and (22.88 ± 6.89)%, respectively . Conclusions Modafinil has a linear kinetic characteristic with no saturation in the range of 100-300 mg. The elimination process is via the liver, the metabolite is modafinil and the metabolites are mainly excreted through the kidneys.