PROCESS FOR PRODUCING A PHARMACEUTICAL PREPARATION FOR THERAPEUTIC TREATMENT OF ENDOMETRIOSIS CONTAINING A COMBINATION OF A GESTAGEN AND (6S)-5-METHYLTETRAHYDROFOLATE

• US 20090060997A1
• Filed: 08/04/2008
• Published: 03/05/2009
• Est. Priority Date: 08/27/2007
• Status: Abandoned Application

• Current Assignee: Bayer Schering Pharma AG (Bayer AG)
• Original Assignee: Bayer Schering Pharma AG (Bayer AG)
• Inventors: King, Kristina, Zimmermann, Holger, Wasserfall, Annemarie, Seitz, Christian, Diefenbach, Konstanze
• Application Number:
  US12/185,456
• Publication Number:
  US 20090060997A1
• Time in Patent Office: Days
• US Class Current: 424/479
• 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 31/519 ortho- or peri-condensed with heterocyclic rings
• CPC Class Codes: A61K 31/56 Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives

Abstract

A combination of an anti-androgenic gestagen at a daily dose of from an ovulation-inhibiting dose up to at most twice the ovulation-inhibiting dose and from 0.1 to 10 mg of (6S)-5-methyltetrahydrofolate are used to produce a pharmaceutical preparation for therapeutically treating endometriosis while simultaneously reducing therapy side effects including the negative effect on bone density and/or bone metabolism, reducing the risk of osteoporosis and, in the event of pregnancy, reducing the risk of congenital malformations, such as medullary tube defects, cleft lip, cleft jaw, or cleft palate, and the risk of pregnancy complications, such as detachment of the placenta and premature birth. The preparation is suitable for long-term administration, which continues daily for at least 169 days to at least two years.

Claims

1. A process of producing a pharmaceutical preparation for therapeutic treatment of endometriosis with simultaneous reduction of therapy side effects including a negative effect on bone density and/or bone metabolism, of the risk of osteoporosis, and of the risk of congenital malformations and pregnancy complications in the event of pregnancy, said process comprising using a combination of a gestagen and (6S)-5-methyltetrahydrofolate and wherein a daily dose of said gestagen is from an ovulation-inhibiting dose to twice said ovulation-inhibiting dose.

2. The process as defined in claim 1, wherein the congenital malformations and the pregnancy complications are medullary tube defects, cleft lip, cleft jaw, cleft palate, detachment of the placenta and premature birth.

3. The process as defined in claim 1, wherein said gestagen is dienogest, cyproterone acetate, or chlormadinone acetate.

4. The process as defined in claim 1, wherein said daily dose comprises from 1 to 2 mg of dienogest, an equivalent amount of cyproterone acetate, or an equivalent amount of chlormadinone acetate.

5. The process as defined in claim 1, wherein a daily dose of said (6S)-5-methyltetrahydrofolate in the preparation is from 0.1 to 10 mg.

6. The process as defined in claim 5, wherein said daily dose of said (6S)-5-methyltetrahydrofolate is from 0.4 to 1 mg.

7. The process as defined in claim 1, wherein a daily dose of said (6S)-5-methyltetrahydrofolate in the preparation consists of 451 μ

g of a calcium salt of said (6S)-5-methyltetrahydrofolic acid.

8. The process as defined in claim 1, wherein said preparing comprises preparing a number of daily dose units containing said gestagen and said (6S)-5-methyltetrahydrofolic acid for continuous administration of said combination over a period of from at least 169 days or from 25 weeks up to at least two years.

9. The process as defined in claim 1, wherein the pharmaceutical preparation is in the form of tablets, capsules, sugar-coated tablets, wafers, transdermal therapy systems, ampoules, suppositories, gels, ointments, implants, vaginal rings, or nasal sprays.