Pharmacokinetics of a contraceptive patch (Evra™/Ortho Evra™) containing norelgestromin and ethinyloestradiol at four application sites
Pharmacokinetics of a contraceptive patch (Evra™/Ortho Evra™) containing norelgestromin and ethinyloestradiol at four application sites
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DOI：
10.1046/j.0306-5251.2001.01532.x
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发表时间：
2002-02-01
影响因子：
3.4
通讯作者：
Anderson, GD
中科院分区：
文献类型：
--
作者：
Abrams, LS;Skee, DM;Anderson, GD
目的确定诺孕曲明（NGMN）和炔雌醇（EE）的药代动力学曲线后，应用避孕贴片，埃夫拉（TM）/OrthoEvra（TM），在每个四个解剖部位（腹部，臀部，手臂，躯干）。受试者被随机分配至4个治疗序列（给药部位）之一。每个贴片佩戴7天，治疗之间有1个月的洗脱期。在每个贴剂贴敷前和贴敷后240 h内的不同时间采集血样。结果基于口服孕激素250 μ g和EE 35 μ g的平均C-ave研究，NGMN和EE的血清浓度参考范围分别为0.6-1.2 ng/ml和25-75 pg/ml。对于所有给药部位，在7天贴敷期间，NGMN和EE的平均浓度保持在这些范围内。尽管平均血清浓度仍在参考范围内，但在腹部贴剂贴敷期间NGMN和EE的吸收比在其他三个部位观察到的吸收低约20%。以前的研究表明，治疗等效的补丁上穿的腹部与其他sites.Conclusions NGMN和EE的避孕贴的血清浓度保持在参考范围内，在整个7天的磨损期间，无论网站的应用程序（腹部，臀部，手臂，或躯干）。
Aims To determine the pharmacokinetic profile of norelgestromin (NGMN) and ethinyloestradiol (EE) following application of the contraceptive patch, Evra(TM)/OrthoEvra(TM), at each of four anatomic sites (abdomen, buttock, arm, and torso).Methods Thirty-seven healthy, nonpregnant women aged 20-45 years participated in this open-label, four-period crossover study. Subjects were randomized to one of four treatment (site of application) sequences. Each patch was worn for 7 days, with a 1 month washout between treatments. Blood samples were collected before and at various times up to 240 h after application of each patch. Serum samples were assayed for NGMN and EE by validated methods.Results The serum concentration reference ranges for NGMN and EE are 0.6-1.2 ng ml(-1) and 25-75 pg ml-(1), respectively, based on studies of the mean C-ave of oral norgestiniate 250 mug and EE 35 mug. For all application sites, mean concentrations of NGMN and EE remained within these ranges during the 7 day wear period. Absorption of NGMN and EE during patch application on the buttock, arm, and torso was equivalent Absorption of NGMN and EE during patch application on the abdomen was approximately 20% less than observed for the other three sites, although mean serum concentrations were still within reference ranges. A previous study demonstrated therapeutic equivalence of patches worn on the abdomen vs other sites.Conclusions Serum concentrations of NGMN and EE from the contraceptive patch remain within the reference ranges throughout the 7 day wear period, regardless of the site of application (abdomen, buttock, arm, or torso).