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来自新型基质和传统储库型经皮治疗系统的雌二醇生物利用度。

Bioavailability of estradiol from a new matrix and a conventional reservoir-type transdermal therapeutic system.

作者信息

Müller P, Botta L, Ezzet F

机构信息

Human Pharmacology, Ciba-Geigy Limited, Basel, Switzerland.

出版信息

Eur J Clin Pharmacol. 1996;51(3-4):327-30. doi: 10.1007/s002280050206.

Abstract

OBJECTIVE

Bioavailability of estradiol delivered from a newly developed matrix-type transdermal therapeutic system (MTTS) was compared with that of the conventional reservoir-type system (RTTS). Both formulations have a nominal delivery rate of 50 micrograms per day of 17 beta-estradiol (E2). Plasma concentrations of E2 and estrone (E1) were determined at steady state during a 96-h application of each formulation to 34 postmenopausal volunteers, using a two-stage randomized two-period crossover design.

RESULTS

The MTTS proved to be equivalent to the RTTS with respect to the extent of E2 absorption. Due to differences in patch design and composition, the rate of absorption was different between the two systems, with less fluctuating E2 plasma levels during application of the matrix system. Local tolerability and adhesion of MTTS appeared to be better than those of the reservoir system.

摘要

目的

将一种新开发的基质型透皮治疗系统(MTTS)释放的雌二醇生物利用度与传统储库型系统(RTTS)的进行比较。两种制剂的17β-雌二醇(E2)标称释放速率均为每日50微克。采用两阶段随机双周期交叉设计,在34名绝经后志愿者身上分别应用每种制剂96小时期间,测定稳态下E2和雌酮(E1)的血浆浓度。

结果

就E2吸收程度而言,MTTS被证明与RTTS相当。由于贴片设计和成分的差异,两种系统的吸收速率不同,在应用基质系统期间,E2血浆水平波动较小。MTTS的局部耐受性和黏附性似乎优于储库系统。

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