Cardot J M, Lecaillon J B, Czendlik C, Godbillon J
Laboratoires Ciba-Geigy, Bioanalytics and Pharmacokinetics (BPK), Rueil-Malmaison, France.
Biopharm Drug Dispos. 1998 May;19(4):259-62. doi: 10.1002/(sici)1099-081x(199805)19:4<259::aid-bdd98>3.0.co;2-v.
The effect of food on the pharmacokinetics of the antiepileptic rufinamide was investigated in healthy volunteers. Twelve subjects were treated with single pre-oral doses of 600 mg of rufinamide after overnight fasting or a fat and protein rich breakfast. Mean (+/- S.D.) areas under the plasma concentration-time curves (AUCs) of the unchanged compound were 57.2 (16) micrograms mL-1 h when given to the fasted volunteers and 81.7 (22.2) micrograms mL-1 h (p = 0.0001) when given after the breakfast. The average AUC was increased by 44% when rufinamide was given with food and the maximum concentration (Cmax) by about 100%. The time at which Cmax was reached (tmax) was shorter (8 h in fasted conditions and 6 h in fed after breakfast); the terminal half-life was not influenced by concomitant intake of food.
在健康志愿者中研究了食物对抗癫痫药物卢非酰胺药代动力学的影响。12名受试者在空腹过夜或食用富含脂肪和蛋白质的早餐后，接受单次口服600mg卢非酰胺的治疗。给予空腹志愿者时，未变化化合物的血浆浓度-时间曲线（AUC）下的平均（±标准差）面积为57.2（16）μg·mL-1·h，早餐后给予时为81.7（22.2）μg·mL-1·h（p = 0.0001）。当卢非酰胺与食物一起服用时，平均AUC增加44%，最大浓度（Cmax）增加约100%。达到Cmax的时间（tmax）较短（空腹条件下为8小时，早餐后进食时为6小时）；终末半衰期不受同时摄入食物的影响。
