Meyer F P, Canzler E, Giers H, Walther H
Institut für Klinische Pharmakologie, Medizinischen Akademie Magdeburg.
Zentralbl Gynakol. 1988;110(22):1449-54.
The effect of the oral contraceptive, Non-Ovlon, on the pharmacokinetics of the model substance, caffeine, was studied in an intraindividual comparison in the course of seven months, i.e. four and two weeks before as well as 0.5, one, three and six months after the women had begun to take the contraceptive. The study commenced in twelve women of which, after seven months, only five were involved. The measuring compartment chosen was saliva so as to minimize strain on the volunteers by this noninvasive approach. Non-Ovlon delayed the caffeine elimination of 4.0 +/- 1.7 hr to 9.0 +/- 4.5 hr and 11.0 +/- 10.4 hr at the end of the first and third intake cycle, respectively. Markedly successive decreases in clearance and an increase in AUC levels were seen in addition to longer half-lives. Interindividual variations were considerable, a finding that might be relevant to the therapy by other, similarly interacting, drugs. There were no differences observed between the initial phase and the median phase of normal menstrual cycle. In one smoker, the caffeine elimination was highly accelerated compared to the average, throughout the period of investigation.
在一项个体内比较研究中,对口服避孕药Non - Ovlon在七个月期间对模型物质咖啡因药代动力学的影响进行了研究,即在女性开始服用避孕药前四周、两周以及服用后0.5个月、1个月、3个月和6个月。该研究始于12名女性,七个月后仅5人参与。选择唾液作为测量部位,以便通过这种非侵入性方法将对志愿者的负担降至最低。在第一个和第三个摄入周期结束时,Non - Ovlon分别将咖啡因的消除时间从4.0±1.7小时延迟至9.0±4.5小时和11.0±10.4小时。除了半衰期延长外,还观察到清除率明显连续下降以及AUC水平升高。个体间差异很大,这一发现可能与其他具有类似相互作用的药物治疗有关。在正常月经周期的初始阶段和中期之间未观察到差异。在一名吸烟者中,在整个研究期间,咖啡因的消除速度比平均水平快得多。