Pharmaceutical application of 15- or 16- substituted...

A - Human Necessities – 61 – K

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A61K 31/56 (2006.01) A61K 31/565 (2006.01) A61K 31/568 (2006.01)

Patent

CA 2497838

The present invention relates to pharmaceutical dosage units for oral, transmucosal or transdermal administration containing 15- or 16-substituted testosterone analogues, as well as to therapeutic methods that employ these testosterone analogues. More particularly, the present invention is concerned with such pharmaceutical dosage units containing at least 10 ~g of an androgenic steroid selected from the group consisting of 15- hydroxytestosterones, 16-hydroxytestosterones, precursors thereof and mixtures of these hydroxytestosterones and/or their precursors; and a pharmaceutically acceptable excipient. The term "15-hydroxytestosterones" encompasses both 15.alpha.-hydroxytestosterone (15.alpha., 17.beta.-dihydroxy-4-androsten-3- one) and 15.beta.-hydroxytestosterone (15.beta., 17.beta.-dihydroxy- 4~androsten-3-one). Similarly, the term "16-hydroxytestosterones" encompasses both 16.alpha.-hydroxytestosterone hydroxytestosterone (16.alpha., 17.beta.- dihydroxy-4-androsten-3-one) and 16.beta.~hydroxytestosterone (16.beta., 17.beta.-dihydroxy-4-androsten-3-one). The androgenic steroids according to the invention are advantageously employed in e.g. a method of treating or preventing androgen deficiency or a method of hormonal contraception.

La présente invention concerne des unités posologiques pharmaceutiques destinées à l'administration par voie orale, par voie transmucosale ou par voie transdermique qui renferment des analogues de testostérone à substitution 15 ou 16, ainsi que des méthodes thérapeutiques dans lesquelles on utilise ces analogues de testostérone. La présente invention se rapporte plus particulièrement aux unités posologiques pharmaceutiques qui contiennent au moins 10 µg d'un stéroïde androgénique sélectionné dans le groupe formé par les 15-hydroxytestostérones, les 16-hydroxytestostérones, les précurseurs de ces dernières et les mélanges de ces hydroxytestostérones et/ou de leurs précurseurs; ainsi qu'un excipient pharmaceutiquement acceptable. Le terme "15-hydroxytestostérones" englobe à la fois la 15.alpha.-hydroxytestostérone (15.alpha., 17.beta.-dihydroxy-4-androsten-3-one) et la 15.beta.-hydroxytestostérone (15.beta., 17.beta.-dihydroxy-4-androsten-3-one). De même, le terme "16-hydroxytestostérones" englobe à la fois la 16.alpha.-hydroxytestostérone hydroxytestostérone (16.alpha., 17.beta.-dihydroxy-4-androsten-3-one) et la 16.beta.-hydroxytestostérone (16.beta., 17.beta.-dihydroxy-4-androsten-3-one). Les stéroïdes androgéniques selon la présente invention sont avantageusement employés par exemple, dans une méthode de traitement ou de prévention de la carence androgénique ou dans une méthode de contraception hormonale.

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