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[经皮给药后17β-雌二醇的生物利用度——取决于贴片系统]

[Bioavailability of 17 beta-estradiol after transdermal administration--dependence on the patch system].

作者信息

Schmolling J, Kusche J, van der Ven H, Schander K

机构信息

Universitäts-Frauenklinik Bonn.

出版信息

Zentralbl Gynakol. 1998;120(3):121-5.

PMID:9556902
Abstract

The objective of this study was to compare the pharmacokinetics of serum estradiol concentrations after application of two different transdermal estradiol delivery systems. Ten postmenopausal women (E2 < or = 30 pg/ml; follicle-stimulating hormone > or = 30 mIE/ml) were prospectively randomized to a crossover treatment protocol separated by a 7-day wash out period. The absorption of estradiol was measured after application of a patch either containing 4.0 mg of E2 in a reservoir system or 1.8 mg of E2 in a specially designed matrix system. Although the increase of serum estradiol concentrations after application of the patches with the matrix system was slightly delayed, mean E2 levels over the whole observation period of 80 hours were significantly higher than those achieved with the reservoir system (difference of mean values: 5.1 pg/ml; p < 0.05). This observation was most striking at the end of the observation period and after removal of the patches. Yet, fluctuations of hormone concentrations were greater with the matrix system patches, and the areas under the E2 concentration-time curves were slightly but not significantly increased as compared to these of the patches with the reservoir system (3211 +/- 584 vs. 2556 +/- 249 pg/ml x h). In conclusion, both transdermal estradiol delivery systems are well suited for postmenopausal hormone substitution providing stable serum estradiol concentrations at about 50 pg/ml, with the matrix system possibly increasing the life span of the patch and thus the recommended application period.

摘要

本研究的目的是比较两种不同经皮雌二醇给药系统应用后血清雌二醇浓度的药代动力学。10名绝经后女性(雌二醇≤30 pg/ml;促卵泡激素≥30 mIE/ml)被前瞻性随机分为交叉治疗方案,间隔7天洗脱期。在应用含4.0 mg雌二醇的储库系统贴片或含1.8 mg雌二醇的特殊设计基质系统贴片后,测量雌二醇的吸收情况。虽然应用基质系统贴片后血清雌二醇浓度的升高略有延迟,但在80小时的整个观察期内,平均雌二醇水平显著高于储库系统贴片(平均值差异:5.1 pg/ml;p<0.05)。这一观察结果在观察期末和贴片去除后最为明显。然而,基质系统贴片的激素浓度波动更大,与储库系统贴片相比,雌二醇浓度-时间曲线下面积略有增加但无显著差异(3211±584 vs. 2556±249 pg/ml·h)。总之,两种经皮雌二醇给药系统都非常适合绝经后激素替代,能使血清雌二醇浓度稳定在约50 pg/ml,基质系统可能会延长贴片的使用寿命,从而延长推荐的应用期。

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