Meyer F P, Canzler E, Giers H, Walther H
Institut für Klinische Pharmakologie, Medizinischen Akademie Magdeburg.
Zentralbl Gynakol. 1991;113(6):297-302.
In the course of six months, the influence of the oral depot contraceptive, Deposiston (3 mg ethinylestradiol sulphonate and 10 mg norethisterone acetate per menstrual cycle) on the pharmacokinetics of caffeine as a model substance was studied in seven women in intraindividual comparison. The first examination began prior to administration of Deposition. The women were subjected to little challenge as saliva was used as the measuring compartment. Deposiston was found markedly delay the elimination half-life life of caffeine (p less than 0.05): t1/2 prior to therapy 4.9 +/- 2.6 h and, after as little as 2 mg ethinylestradiol sulphonate 8.0 +/- 3.5 h. In contrast to the effect observed for preparations containing less estrogen, these longer half-lives persisted throughout the trial. As expected, the AUC values were slightly elevated during this period, whereas clearance values were reduced.
在六个月的时间里，以咖啡因作为模型物质，在七名女性中进行了个体内比较研究，考察了口服长效避孕药Deposiston（每个月经周期含3毫克炔雌醇磺酸盐和10毫克醋酸炔诺酮）对咖啡因药代动力学的影响。首次检查在服用Deposiston之前开始。由于使用唾液作为测量部位，女性受到的干扰较小。发现Deposiston显著延迟了咖啡因的消除半衰期（p<0.05）：治疗前t1/2为4.9±2.6小时，在仅服用2毫克炔雌醇磺酸盐后为8.0±3.5小时。与含雌激素较少的制剂所观察到的效果相反，这些较长的半衰期在整个试验过程中持续存在。正如预期的那样，在此期间AUC值略有升高，而清除率值降低。
