LOW-DOSAGE PERORAL MEDICATION FOR CONTRACEPTION CONTAINING CRYSTALLINE DIENOGEST AND ETHINYL ESTRADIOL

• US 20080038350A1
• Filed: 06/13/2007
• Published: 02/14/2008
• Est. Priority Date: 08/10/2006
• Status: Abandoned Application

• Current Assignee: Bayer Schering Pharma AG (Bayer AG)
• Original Assignee: Bayer Schering Pharma AG (Bayer AG)
• Inventors: Wiesinger, Herbert, Buske, Alexander, Gerecke, Hagen, Fricke, Sabine, Ladwig, Ralf
• Application Number:
  US11/762,207
• Publication Number:
  US 20080038350A1
• Time in Patent Office: Days
• US Class Current: 424/474
• CPC Class Codes: A61K 31/56 Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
• CPC Class Codes: A61K 31/567 substituted in position 17 alpha, e.g. mestranol, norethandrolone
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61K 9/14 Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles microspheres A61K9/16; microcapsules A61K9/50; nanocapsules, nanoparticles of the matrix type A61K9/51
• CPC Class Codes: A61K 9/2018 Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
• CPC Class Codes: A61K 9/2059 Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
• CPC Class Codes: A61K 9/2813 Inorganic compounds
• CPC Class Codes: A61K 9/282 Organic compounds, e.g. fats
• CPC Class Codes: A61K 9/284 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
• CPC Class Codes: A61K 9/2853 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers, poly(lactide-co-glycolide)
• CPC Class Codes: A61K 9/2866 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61P 15/18 Feminine contraceptives

Abstract

The peroral medication for prevention of conception contains as one active ingredient crystalline 17α-cyanomethyl-17β-hydroxyestra-4,9-dien-3-one (dienogest) at a daily dosage equal to or less than 2.0 mg and as another active ingredient 17α-ethinyl estradiol at a daily dosage of less than 0.030 mg, together with one or more pharmaceutically acceptable carriers. The active ingredient dienogest is contained in the medication in crystalline form with an average particle size of preferably 25 to 70 μm. The other active ingredient ethinyl estradiol is incorporated during granulation in micronized form or by spraying an ethanolic solution containing it.

Claims

1. A peroral medication for contraception containing 2.0 mg or less of crystalline 17α

-cyanomethyl-17β

-hydroxyestra-4,9-dien-3-one and less than 0.030 mg of 17α

-ethinyl estradiol as effective active ingredients for preventing conception, wherein said crystalline 17α

-cyanomethyl-17β

-hydroxy-estra-4,9-dien-3-one has an average particle size from 25 to 270 μ

m.

2. The peroral medication as defined in claim 1, wherein said average particle size is from 30 to 70 μ

m.

3. The peroral medication as defined in claim 1, wherein said average particle size is from 40 to 65 μ

m.

4. The peroral medication as defined in claim 1, containing from 0.75 to 2.0 mg of said crystalline 17α

-cyanomethyl-17β

-hydroxyestra-4,9-dien-3-one and from 0.015 to 0.020 mg of said ethinyl estradiol.

5. The peroral medication as defined in claim 1, containing from 1.5 to 2.0 mg of said crystalline 17α

-cyanomethyl-17β

-hydroxyestra-4,9-dien-3-one dienogest and from 0.015 to 0.020 mg of said ethinyl estradiol.

6. The peroral medication as defined in claim 1, comprising 21, 22, 23, 24, 25, or 26 daily dosage units containing said crystalline 17α

-cyanomethyl-17β

-hydroxyestra-4,9-dien-3-one and said ethinyl estradiol and 7, 6, 5, 4, 3, or 2 daily dosage units respectively not containing said crystalline 17α

-cyanomethyl-17β

-hydroxyestra-4,9-dien-3-one and not containing said ethinyl estradiol for a 28-day menstrual cycle.

7. A peroral medication for contraception comprising a tablet or a coated tablet for daily oral administration, wherein said tablet or said coated tablet contains an active ingredient combination effective for preventing conception, together with pharmaceutically acceptable carriers;

wherein said active ingredient combination consists of from 0.75 to 2.0 mg of crystalline 17α

-cyanomethyl-17β

-hydroxyestra-4,9-dien-3-one and from 0.015 to 0.020 mg of ethinyl estradiol; and

wherein said crystalline 17α

-cyanomethyl-17β

-hydroxy-estra-4,9-dien-3-one consists of crystals of said 17α

-cyanomethyl-17β

-hydroxy-estra-4,9-dien-3-one with an average particle size of from 25 to 270 μ

m.

8. A contraceptive preparation for oral administration consisting of 21 daily dosage units each consisting of an effective ingredient combination for contraception and 7 daily dosage units each not containing active ingredients for preventing conception, or consisting of 22 daily dosage units each consisting of said effective ingredient combination

for contraception and 6 daily dosage units each not containing said active ingredients for preventing conception, or

consisting of 23 daily dosage units each consisting of said effective ingredient combination for contraception and 5 daily dosage units each not containing said active ingredients for preventing conception, or

consisting of 24 daily dosage units each consisting of said effective ingredient combination for contraception and 4 daily dosage units each not containing said active ingredients for preventing conception, or

consisting of 25 daily dosage units each consisting of said effective ingredient combination for contraception and 3 daily dosage units each not containing said active ingredients for preventing conception, or

consisting of 26 daily dosage units each consisting of said effective ingredient combination for contraception and 2 daily dosage units each not containing said active ingredients for preventing conception;

wherein said effective ingredient combination for contraception consists of from 0.75 to 2.0 mg of said crystalline 17α

-cyanomethyl-17β

-hydroxyestra-4,9-dien-3-one and from 0.015 to 0.020 mg of said ethinyl estradiol; and

wherein said crystalline 17α

-cyanomethyl-17β

-hydroxy-estra-4,9-dien-3-one consists of crystals of said 17α

-cyanomethyl-17β

-hydroxy-estra-4,9-dien-3-one with an average particle size of from 25 to 270 μ

m.