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Drug delivery system comprising a tetrahydroxylated estrogen for use in hormonal contraception

机译:用于激素避孕的包含四羟基化雌激素的药物递送系统

摘要

A method of contraception in mammalian females, which method comprises the parenteral or rectal administration of an estrogenic component and a progestogenic component to a female of childbearing capability in an amount effective to inhibit ovulation, wherein the estrogenic component is selected from the group consisting of substances represented by the following formula (1); embedded image in which R1, R2, R3, R4 independently are a hydrogen atom, a hydroxyl group or an alkoxy group with 1-5 carbon atoms; each of R5, R6, R7 is a hydroxyl group; and no more than 3 of R1, R2, R3, R4 are hydrogen atoms; precursors capable of liberating a substance according to the aforementioned formula when used in the present method; and mixtures of one or more of the aforementioned substances and/or precursors. Another aspect of the invention concerns a drug delivery system for parenteral or rectal administration that contains the aforementioned estrogenic component and a progestogenic component, said drug delivery system being selected from the group consisting of suppositories, systems for intravaginal delivery, inhalers, nasal sprays and transdermal delivery systems.
机译:一种在哺乳动物雌性中避孕的方法,该方法包括以有效抑制排卵的量将雌激素成分和孕激素成分经肠胃外或直肠给药给具有生育能力的雌性,其中雌激素成分选自由以下物质组成的组:由下式(1)表示; “嵌入式图像” 其中R 1 ,R 2 ,R 3 ,R 4 独立地是氢原子,羟基或具有1-5个碳原子的烷氧基;或R 5 ,R 6 ,R 7 分别为羟基。 R 1 ,R 2 ,R 3 ,R 4 中不超过3个为氢原子;当在本方法中使用时,能够释放根据上述通式的物质的前体;以及一种或多种上述物质和/或前体的混合物。本发明的另一方面涉及用于肠胃外或直肠给药的药物输送系统,其包含上述雌激素成分和孕激素成分,所述药物输送系统选自栓剂,阴道内输送系统,吸入器,鼻喷雾剂和透皮药物。投放系统。

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