Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai
Patent
1996-06-04
1998-10-27
Fay, Zohreh
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Cyclopentanohydrophenanthrene ring system doai
A61K 3156
Patent
active
058278435
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/EP94/62997 filed Sep. 8, 1994.
The present invention relates to a preparation for substitution therapy and for oral contraception. More particularly the present invention on the one hand relates to relieving the effects which occur because the ovaries decrease or stop production of female hormones, for instance during the menopause. The substitution therapy is mainly intended to induce amenorrhoea with negligible blood loss.
During and after the menopause these effects comprise hot flushes and nocturnal sweating, atrophy of the vagina which can result in sexual difficulties, bone decalcification, increase in heart and blood vessel disorders and psychic symptoms with a causal connection that is usually difficult to demonstrate.
Up to the present different types of substitution therapy have been applied comprising a hormone treatment with one or more estrogens and one or more progestogens.
According to a first therapy, low doses of estrogens and progestogens are administered, but such a treatment is ineffective in respect of the decalcification and heart and blood vessel disorders.
In another therapy the natural cycle of estrogens and progestogens is followed is closely as possible. This treatment inevitably results in menstruation and has the advantage of a reduced risk of cancer of the uterus.
According to yet another therapy only estrogens are administered in a dose which lies below the threshold for menstrual bleeding. This treatment has the drawback however of an increased risk of cancer of the uterus.
According to a most recently known therapy estrogens and progestogens are administered continuous! such that the endomotrium does not proliferate. This therapy has the drawback however of an unacceptably high incidence of slight, irregular blood loss.
The present invention has for its object to provide a substitution therapy wherein the above described drawbacks occur to a much lesser extent, with the objective of inducing amenorrhoea with negligible blood loss over a long period (many months to years).
On the other hand, the present invention relates to preparations designed for oral contraception with substantially continuous application.
In continuous application of oral contraceptive frequently intermediate bleedings occur. The preparations according to the present invention are designed to induce menstrual bleeding with a regular menstrual bleeding, with an extended cycle or eventually a constant amenorrhoea, but characterized by an optimal (cycle) control and/or by a substantially reduced ocurrence of intermediate bleeding.
EP-A-559 240 discloses preparations for substitution therapy and oral contraception in which the estrogen dose is constant and the progestagen dose is periodically alternated.
However, the improvement in inhibiting endometrium blooding is minor. Above that, since the use of higher progestogen doses provided better results than lower doses it appears illogical to use periodically varying estrogen doses.
The present invention is based on the finding that suprisingly when using periodically varying estrogen doses the occurence of blood loss and intermediate bleeding is substantially avoided. The estrogen dose is herein oscillated such that estrogen-dominant and progestogen-dominant periods occur alternatingly with a sufficiently short periodicity. This short periodicity in the estrogen dose is necessary to avoid blood loss.
Purely by administering a dose of progestogen or estrogen substantially constant in time and an estrogen or progestogen varying in time between at least two dose levels, it was possible to induce the desired amenorrhoea while no blood loss occurred over a longer period.
The invention therefore relates to a preparation for substitution therapy and for oral contraception comprising at least one progestogen and at least one estrogen in which the estrogen dose varies with a periodicity such that blood loss is substantially avoided.
It is noted that the preparation is formulated such that a substantially constant blood concentration is
Fay Zohreh
Saturnus A.G.
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