Dresse A, Rosen J M, Brems H, Masset H, Defrance R, Salvadori C
Laboratoire de Pharmacologie, Université de Liège, Belgium.
J Clin Pharmacol. 1988 Dec;28(12):1115-9. doi: 10.1002/j.1552-4604.1988.tb05726.x.
The influence of a test meal on the absorption and disposition of tianeptine (Stablon), a new antidepressant, was investigated in 12 healthy subjects in a two-way, randomized, open cross-over study. Single 12.5-mg oral doses of tianeptine were administered following a night of fasting or immediately after a standardized breakfast. When subjects received tianeptine under fasting conditions the lag time before absorption onset, and the time of the maximum plasma concentration were 0.55 +/- 0.26 hours and 1.29 +/- 0.29 hours, respectively. The maximum plasma concentration was 322 +/- 44 ng/mL, and the total area under the curve 994 +/- 248 ng/hr/mL. When tianeptine was given at the end of the meal, several significant changes were found for tianeptine kinetic parameters; the lag time increased by 0.3 hour and the maximum plasma concentration was lowered (decreased by 25%) and occurred later (tmax increased by 0.5 hour). However, no significant change was found in the area under the plasma concentration-time curve. The trend and extent of changes in the MC5 metabolite parameters were similar to those observed for the parent drug. Absorption of tianeptine is slightly delayed and slowed down without modification of its extent when tianeptine is given at the end of a meal. These slight changes are not clinically relevant for an antidepressant administered three times a day. Despite the changes observed, tianeptine may be given at meal times to improve compliance with treatment.
在一项双向、随机、开放交叉研究中，对12名健康受试者研究了试验餐对新型抗抑郁药噻奈普汀（Stablon）吸收和处置的影响。在禁食一夜后或在标准早餐后立即给予单次12.5mg口服噻奈普汀剂量。当受试者在禁食条件下接受噻奈普汀时，吸收开始前的滞后时间和血浆最大浓度时间分别为0.55±0.26小时和1.29±0.29小时。血浆最大浓度为322±44ng/mL，曲线下总面积为994±248ng/hr/mL。当在进餐结束时给予噻奈普汀时，发现噻奈普汀动力学参数有几个显著变化；滞后时间增加了0.3小时，血浆最大浓度降低（下降25%）且出现时间延迟（tmax增加0.5小时）。然而，血浆浓度-时间曲线下面积未发现显著变化。MC5代谢物参数的变化趋势和程度与母体药物观察到的相似。当在进餐结束时给予噻奈普汀时，其吸收略有延迟且减慢，但其吸收程度未改变。这些轻微变化对于每日给药三次的抗抑郁药而言在临床上不相关。尽管观察到有变化，但噻奈普汀可在进餐时给药以提高治疗依从性。
