Axelson J E, Chan G L, Kirsten E B, Mason W D, Lanman R C, Kerr C R
Br J Clin Pharmacol. 1987 Jun;23(6):735-41. doi: 10.1111/j.1365-2125.1987.tb03109.x.
The effect of food intake on the bioavailability of propafenone, a new antiarrhythmic agent, was evaluated by comparing its kinetics in 24 healthy volunteers in a fasted state and after a standard breakfast. With food, the maximum plasma drug concentration was reached earlier and was significantly increased. When data from 'slow' metabolizers were excluded, there was an average increase of 147% in the area under the concentration-time curve (AUCo) following the standard breakfast. There was a significant correlation (r = 0.946) between [(AUCo fed - AUCo fasted)/AUCo fasted] and propafenone intrinsic clearance in the fasted state. Food intake, however, does not appear to affect the bioavailability of propafenone in 'slow' metabolizers. Patients should be advised to take propafenone in a constant relationship to food to assure consistent bioavailability.
通过比较24名健康志愿者在禁食状态和标准早餐后丙吡胺（一种新型抗心律失常药物）的动力学，评估了食物摄入对其生物利用度的影响。进食后，血浆药物浓度峰值出现得更早，且显著升高。排除“慢”代谢者的数据后，标准早餐后浓度-时间曲线下面积（AUCo）平均增加了147%。在禁食状态下，[(AUCo进食 - AUCo禁食)/AUCo禁食]与丙吡胺固有清除率之间存在显著相关性（r = 0.946）。然而，食物摄入似乎并不影响“慢”代谢者中丙吡胺的生物利用度。应建议患者在与食物的固定关系下服用丙吡胺，以确保生物利用度一致。
