孕激素药物动力学和药效学3剂量和2方案的冒泡的微缩黄体酮阴道插入。

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保尔森RJ,柯林斯毫克,Yankov VI

孕激素药物动力学和药效学3剂量和2方案的冒泡的微缩黄体酮阴道插入。

中国性金属底座。2014年11月,99 (11):4241 - 9。doi: 10.1210 / jc.2013 - 3937。Epub 2014年2月25日。

PubMed ID

24606090 (在PubMed

]

文摘

背景:黄体酮阴道插入(元太),一个冒泡的交付系统,迅速溶解,通过阴道上皮细胞吸收,达到更高的子宫内膜组织与孕酮浓度比实现石油(PIO)给我。目的:我们的目的是检查相比PIO元太的药代学和药效学。设计、设置和参与者:58健康的绝经前妇女被随机分配到50,100,或200毫克每日一次元太;100或200毫克每天两次元太;或者50到100毫克每日PIO通过im注射一次,10天。后血清样本获得第一剂量;后血清和子宫内膜组织得到最后的剂量。主要结果测量:最大观察血清浓度(Cmax),时间Cmax, serum-concentration时间曲线下的面积超过剂量间隔计算基线校正后孕激素浓度。方差分析和配对t检验比较结果和内部组织。结果:后观察Cmax PIO高于元太管理。 Endometrial tissue progesterone concentrations were higher for PVI regimens. Time to Cmax was 7.3 hours after PIO and 3.3 to 5.9 hours after PVI. Steady state was achieved within 24 and 48 hours for PVI and PIO regimens, respectively. The area under the curve increased with increasing PVI dosage; however, the increase was not proportional to the increase in dosage. Downregulation of estrogen and progesterone receptors was observed in secretory biopsy specimens. CONCLUSION: The PVI system consistently allowed for rapid progesterone absorption and achieved higher endometrial tissue concentrations and lower systemic exposures than observed after im PIO.

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药物

孕酮