University of Texas Southwestern Medical Center, Department of Obstetrics and Gynecology, Dallas, TX 75235-9032, USA.
Am J Obstet Gynecol. 2011 Jun;204(6 Suppl 1):S89-93. doi: 10.1016/j.ajog.2011.03.005. Epub 2011 Mar 9.
The purpose of this study was to determine pharmacokinetic parameters for oseltamivir in all trimesters of pregnancy. Thirty pregnant women, 10 per trimester, who were receiving oseltamivir phosphate (75 mg) were recruited to study first-dose pharmacokinetics. Plasma samples were obtained at 0, 0.5, 1, 2, 4, 8, and 12 hours after the first dose. Samples were analyzed for oseltamivir and oseltamivir carboxylate levels. With the use of a noncompartmental model, we estimated the area-under-the-curve, maximum concentration, time-to-maximum concentration, and half-life. There were no significant differences in the pharmacokinetics of oseltamivir by trimester, except for an increased half-life in the first trimester for oseltamivir phosphate and an increased maximum concentration in the third trimester for oseltamivir carboxylate. The levels of oseltamivir carboxylate that were observed were within the range that was needed to achieve inhibitory concentrations at 50% for pandemic H1N1. The pharmacokinetics of oseltamivir does not change significantly according to trimester of pregnancy.
本研究旨在确定妊娠各期磷酸奥司他韦的药代动力学参数。招募了 30 名接受磷酸奥司他韦（75mg）治疗的孕妇，每个孕期 10 名，以研究首剂药代动力学。在首剂后 0、0.5、1、2、4、8 和 12 小时采集血样，分析奥司他韦和奥司他韦羧酸的水平。使用非房室模型，我们估算了曲线下面积、最大浓度、达峰时间和半衰期。除了奥司他韦磷酸盐在孕早期半衰期延长，奥司他韦羧酸在孕晚期最大浓度增加外，孕期各期奥司他韦的药代动力学无显著差异。观察到的奥司他韦羧酸水平在达到大流行 H1N1 的 50%抑制浓度所需范围内。奥司他韦的药代动力学不因孕期不同而有显著变化。
