Medicaments based on progestins for dermal use

• US 20030109507A1
• Filed: 09/20/2002
• Published: 06/12/2003
• Est. Priority Date: 09/21/2001
• Status: Abandoned Application

• Current Assignee: DR. KADE Pharmazeutische Fabrik GmbH
• Original Assignee: Drkade Pharmazeutische Fabrik GmbH
• Inventors: Beckmann, Karsten, Franke, Christian
• Application Number:
  US10/247,629
• Publication Number:
  US 20030109507A1
• Time in Patent Office: Days
• US Class Current: 514/171
• CPC Class Codes: A61K 2800/522 Antioxidants; Radical scavengers
• CPC Class Codes: A61K 2800/59 Mixtures
• CPC Class Codes: A61K 31/375 Ascorbic acid, i.e. vitamin C; Salts thereof
• CPC Class Codes: A61K 31/56 Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 47/183 Amino acids, e.g. glycine, EDTA or aspartame
• CPC Class Codes: A61K 47/22 Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
• CPC Class Codes: A61K 47/26 Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
• CPC Class Codes: A61K 8/63 Steroids; Derivatives thereof
• CPC Class Codes: A61K 8/676 Ascorbic acid, i.e. vitamin C
• CPC Class Codes: A61K 9/0014 Skin, i.e. galenical aspects of topical compositions non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00
• CPC Class Codes: A61P 5/34 Gestagens
• CPC Class Codes: A61Q 19/00 Preparations for care of the skin

Abstract

The present invention relates to semisolid transcutaneous medicaments based on at least one oxidation-sensitive progestin or a pharmaceutically acceptable derivative thereof. The medicaments comprise ascorbic acid, an ascorbic acid derivative or a salt thereof and have excellent stability. Corresponding gels which comprise a combination of norethisterone acetate and estradiol are described in particular.

Claims

1. A semisolid transcutaneous medicament based on at least one oxidation-sensitive progestin or a pharmaceutically acceptable derivative thereof, which comprises ascorbic acid, a pharmaceutically acceptable derivative and/or salt thereof.

2. A medicament as claimed in claim 1, wherein the ascorbic acid content is from 0.01 to 1.5% by weight.

3. A medicament as claimed in claim 1 or 2, which comprises at least one chelating agent.

4. A medicament as claimed in claim 3, wherein the chelating agent is EDTA or a pharmaceutically acceptable salt thereof.

5. A medicament as claimed in claim 3, wherein the chelating agent content is from 0.01 to 1% by weight.

6. A medicament as claimed in claim 1, which comprises at least one solubilizer.

7. A medicament as claimed in claim 6, wherein the solubilizer is a diethylene glycol mono-C_1-4-alkyl ether or dimethylisosorbitol.

8. A medicament as claimed in claim 6 or 7, wherein the ethanol content of the medicament is less than 50% by weight.

9. A medicament as claimed in claim 1, wherein the progestin has a basic steroid structure which is monounsaturated in the 4,5 position.

10. A medicament as claimed in claim 9, wherein the progestin is allylestrenol, desogestrel, gestodene, hydroxyprogesterone, lynestrenol, norethisterone, norgestrel, levonorgestrel or a pharmaceutically acceptable derivative thereof.

11. A medicament as claimed in claim 10, based on norethisterone acetate.

12. A medicament as claimed in claim 11, wherein the norethisterone content is from 0.01 to 1.5% by weight.

13. A medicament as claimed in claim 1, which comprises an estrogen which can be administered transcutaneously.

14. A medicament as claimed in claim 13, wherein the estrogen which can be administered transcutaneously is estradiol or a pharmaceutically acceptable derivative thereof.

15. A medicament as claimed in claim 13, wherein the estrogen content is from 0.01 to 1.5% by weight.

16. A medicament as claimed in claim 1 in the form of a gel.