Pharmaceuticals for contraception/hormone substitution containing a biogenous estrogen component

• US 5,633,242 A
• Filed: 08/03/1995
• Issued: 05/27/1997
• Est. Priority Date: 08/12/1994
• Status: Expired due to Term

• Current Assignee: Schering Ag (Merck & Co., Inc.)
• Original Assignee: Jenapharm GmbH & Co. KG (Bayer AG)
• Inventors: Moore, Claudia, Osterwald, Hermann, Gr aser, Thomas, Oettel, Michael
• Primary Examiner(s): JORDAN, KIMBERLY R
• Application Number:
  US08/511,026
• Time in Patent Office: 663 Days
• Field of Search: 514/170, 514/841, 514/843
• US Class Current: 514/170
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/565 not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
• CPC Class Codes: A61K 31/57 substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
• CPC Class Codes: A61P 15/18 Feminine contraceptives

Abstract

This invention relates to a compound preparation for contraception and hormone replacement that consists of three steps totalling 28 daily doses. The pharmaceutical is characterized in that

step 1 consists of 3 or 4 daily doses, each containing a preparation in which the active ingredient is at least one biogenous estrogen component,

step 2 consists of 20 to 22 daily doses, each containing a preparation in which the active ingredients are at least one biogenous estrogen and one gestagen component from the group of C₂₁ -gestagens including progesterone, as well as dienogest, desogestrel, 3-keto desogestrel, gestodene, levonorgestrel, norgestimate, norethisterone, norethisterone acetate and dydrogesterone, and

step 3 consists of 3 or 4 daily doses, each containing a preparation in which the active ingredient is at least one biogenous estrogen component.

Claims

1. A method of contraception or hormone replacement beginning on the first day of menses consisting of the steps of:

(1) administering 3 or 4 daily doses of a preparation in which the active ingredient comprises at least one biogenous estrogen component;

(2) administering 20 to 22 daily doses of a preparation in which the active ingredients comprise at least one biogenous estrogen and one gestagen component; and

(3) administering 3 or 4 daily doses of a preparation in which the active ingredient comprises at lease one biogenous estrogen component,

wherein the total daily doses of steps (1), (2) and (3) is 28.

2. The method of claim 1, wherein the second step consists of two groups of daily doses, the first group (a) comprising 7 to 9 daily doses and the second group (b) comprising 12 to 14 daily doses, with daily doses in both groups containing equal quantities of at least one gestagen component and the daily doses of the second group containing a greater quantity of the biogenous estrogen component than the first group.

3. The method of claim 1, wherein the biogenous estrogen component is selected from the group consisting of 17β

-estradiol, an ester of 17β

-estradiol with a physiologically acceptable acid, a 17β

-estradiol derivative that releases 17β

-estradiol in physiological conditions, and a mixture thereof.

4. The method of claim 1, wherein the gestagen component is selected from the group consisting of a C₂₁ -gestagen, progesterone, and a mixture of a C₂₁ -gestagen and progesterone.

5. The method of claim 1, wherein the gestagen component is selected from the group consisting of chlormadinon acetate, dienogest, and a mixture of chlormadinon acetate and dienogest.

6. The method of claim 1 wherein the gestagen component is selected from the group consisting of desogestrel, 3-keto desogestrel, gestodene, levonorgestrel, norgestimate, norethisterone, norethisterone acetate, dydrogesterone and combinations thereof.