Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai
Reexamination Certificate
2000-04-10
2002-09-17
Dees, Jose′ G. (Department: 1616)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Cyclopentanohydrophenanthrene ring system doai
C424S422000, C424S426000, C424S430000, C424S435000, C424S436000, C424S448000, C424S449000
Reexamination Certificate
active
06451779
ABSTRACT:
The invention relates to a means for hormonal contraception with three components used especially for the treatment and/or prophylaxis of tumors of the mammary glands, as well as a process for the hormonal contraception and/or treatment and/or prophylaxis of tumors of the mammary glands.
Since the beginning of the availability of hormonal contraceptives in the 1960s, a large number of hormonal components were developed with regard to their suitability in very different administration schemes. Basically, a division into combination and sequence preparations is possible.
In known combination preparations, for example, in as far as the desired cycle period is 28 days, a combination of an estrogen and a gestagen preparation is administered for 21 days in a constant or changing, absolute or relative dosage, wherein the estrogen preparation can be, for example, natural estrogen or synthetic ethinylestradiol and a 7-day pause follows the ingestion of the above-mentioned 21 daily units during which time a withdrawal bleeding occurs simulating the natural monthly bleeding.
In the known sequence preparations, also in a desired cycle period of 28 days, a pure estrogen preparation is administer for 7 days and then for 15 days a combination of an estrogen preparation and a gestagen preparation, wherein also here an ingestion-free period of, for example, 6 days follows during which time a withdrawal bleeding occurs. Although it is known to bridge the period of ingestion pause of the combination and sequence preparations in the interest of a greater ingestion safety by administering placebos within those specific days, this was always based on the notion that during the approximately one-week long ingestion period no hormones of the here discussed type may be administered in order to guarantee a reliable withdrawal bleeding. Only in substitution preparations in the menopause of the older women were hormones administered during the total cycle, for example in the sequence of estrogen preparation for 10 days, combination of estrogen and gestagen preparation for 11 days, estrogen preparation for 7 days in especially low dosage; however, these substitution preparations are not suitable for the stopping of ovulation.
The sequence preparations used in substitution therapy are especially unsuitable for contraception because the natural estradiol in the given dosage does not prevent ovulation and the phase in which gestagen is administered is, at 11 days, too short. The below described sequential order guarantees in substitution preparations, however, a relatively good cycle control.
From DE-PS 43 08 406, a combination preparation for contraception is known consisting of one or more steps. In so doing, it is provided that at least one step contains the combination of three components, namely a biogenetic estrogen, a synthetic estrogen and a gestagen and the further steps consists of a pharmaceutically unobjectionable placebo or a biogenetic or synthetic gestagen, or a biogenetic or synthetic estrogen, or a combination of three components, namely a biogenetic estrogen, a synthetic estrogen and a gestagen or a combination of synthetic estrogens and a gestagen.
From the description of the above publication is can be seen that, with the step concept described therein, a change in condition occurs typically over time. Such a change in condition can also occur in such a way that the putting together of the phases that constitute the step can be changed in terms of the employed components, as well as by only changing the concentrations of the components employed in the phases that make up the step.
Even when only one single step without component change is provided as provided by a special embodiment of the combination preparation according to DE-PS 43 08 406, one proceed in any case in a way that a withdrawal bleeding occurs because, after the complete disclosure of DE-PS 43 08 406, such a withdrawal bleeding is considered indispensable for the achievement of the desired contraceptive safety.
It is the object of the invention to make available a means for hormonal contraception which offers a high contraceptive safety and eliminates intermediary bleedings. Furthermore, the side-effects otherwise observed in hormonal means of contraception should be further reduced.
In so doing, especially also an effective treatment and/or prophylaxis of tumors of the mammary glands should be make possible.
According to the invention, this problem is solved by a means for hormonal contraception with three components containing a first hormone component with at least one synthetic estrogen, a second hormone component with at least one biogenetic estrogen, and a third hormone component with at least one gestagen for continuous and combined administration.
Finally, the problem is solved through a process for hormonal contraception which provides that a means having at least one first hormone component with at least one synthetic estrogen, a second hormone component with at least one biogenetic estrogen, and a third hormone component with at least one gestagen be continuously administered.
In a further aspect, the invention relates to the use of the means of stopping ovulation according to the invention.
In still a further aspect, the invention relates to the use of the means according to the invention for the treatment and/or prophylaxis of tumors of the mammary glands.
In so doing, it can be provided that the synthetic estrogen is selected from a group consisting of ethinylestradiol, mestranol and others, as well as hormone combinations which quickly split off at least one synthetic estrogen upon ingestion.
In a preferred embodiment it is provided that the synthetic estrogen is ethinylestradiol.
In a completely preferred embodiment it is provided that the daily administered amount of ethinylestradiol is from 1 to 20 &mgr;g.
In so doing, it is even more preferred that the daily administered amount of ethinylestradiol is from 5 to 10 &mgr;g.
According to the invention, it can be further provided that the second hormone component is selected from a group consisting of estradiol, estriol, estrone, estran and others, as well as hormone combinations which quickly split off at least one of the mentioned estrogens upon ingestion.
In a preferred embodiment it is provided that the second hormone component consists of 17-&agr;-estradiol and/or 17-&bgr;-estradiol.
In a further embodiment of the means according to the invention, it can be provided that the daily administered amount of second hormone component is in the case of estradiol, especially &agr;- and &bgr;-estradiol from 0.1 to 2 mg and in the case of conjugated estrogen it is from 0.05 to 0.5 mg.
In a further embodiment of the means according to the invention, a third hormone component is selected from a group consisting of progesterone, chlormadinone acetate, norethisterone acetate, cyproterone acetate, desogestrel, levonorgestrel and other natural and/or synthetic gestagens as well as hormone combinations which quickly split off at least one of the mentioned gestagens upon ingestion.
In an embodiment, the means according to the invention can be provided for oral administration.
In an alternative embodiment, the means according to the invention can be provided for transdermal administration.
In a second alternative embodiment, the means according to the invention can be provided for intravaginal administration.
In a third alternative embodiment, the means according to the invention can be provided as depository injection.
In a fourth alternative embodiment, the means according to the invention can be provided as a hormone implant.
Finally, it can be provided that the daily units which each contain all three hormone components are arranged as spacially separated and individually dispensable in a packaging unit.
In an embodiment of the process according to the invention it can finally be provided that the means according to the invention are administered.
Providing the basis for the invention is a surprising notion that high contraceptive safety can be realized through continu
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