Transdermal system that contains a new highly potent gestagen

• US 20030003139A1
• Filed: 12/20/2001
• Published: 01/02/2003
• Est. Priority Date: 12/21/2000
• Status: Abandoned Application

• Current Assignee: Schering Ag (Merck & Co., Inc.)
• Original Assignee: Schering Ag (Merck & Co., Inc.)
• Inventors: Lipp, Ralph, Gunther, Clemens
• Application Number:
  US10/022,834
• Publication Number:
  US 20030003139A1
• Time in Patent Office: Days
• US Class Current: 424/449
• 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 47/32 Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers , poly(meth)acrylates, or polyvinyl pyrrolidone
• CPC Class Codes: A61K 9/7053 obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene
• CPC Class Codes: A61K 9/7061 Polyacrylates
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 5/34 Gestagens

Abstract

Matrix-transdermal system that contains (21S)-21-hydroxy-21-methyl-14,17-ethano-19-norpregna-4,9,15-triene-3,20-dione that comprises a polyacrylate adhesive.

Claims

1. Matrix-transdermal system that contains (21S)-21-hydroxy-21-methyl-14,17-ethano-19-norpregna-4,9,15-triene-3,20-dione, characterized in that the matrix comprises polyacrylate adhesive.

2. Transdermal system according to claim 1, wherein the polyacrylate adhesive is a copolymer of at least two of the following monomers:

2-ethylhexylhexylacrylate, hydroxyethylhexylacrylate, vinyl acetate, vinyl pyrrolidone.

3. Transdermal system according to claim 2, wherein the polyacrylate adhesive is a copolymer that consists of 2-ethylhexylacrylate and hydroxyethylacrylate (Gelva^(R)) or a copolymer of these monomers with vinyl acetate and 2-ethylhexylacrylate-N-vinyl-2-pyrrolidone (TSR^(R)-adhesive of the Sekisui Company).

4. Transdermal system according to one of claims 1 to 3, characterized by a content of 0.1 to 20% by weight, preferably 1 to 15% of (21S)-21-hydroxy-21-methyl-14,17-ethano-19-norpregna-4,9,15-triene-3,20-dione in the matrix.

5. Transdermal system according to one of claims 1 to 4, wherein the matrix comprises at least one crystallization inhibitor.

6. Transdermal system according to claim 5, wherein the matrix comprises at least one N-vinyllactam polymer such as N-vinyl -1-aza-cycloheptan-2-one homopolymer, N-vinyl-piperidin-2-one homopolymer, polymers of vinylpyrrolidone such as polyvidone (Kollidon^(R)) or co-polymers of vinylpyrrolidone with vinyl acetate (copovidones).

7. Transdermal system according to one of claims 1 to 6, characterized by an additional content of at least one of the following penetration intensifiers:

Monovalent or multivalent alcohols such as ethanol, 1,2-propanediol or benzyl alcohol;

saturated or unsaturated fatty alcohols with 8 to 18 carbon atoms, such as lauryl alcohol or cetyl alcohol;

hydrocarbons such as mineral oil;

saturated and unsaturated fatty acids with 8 to 18 carbon atoms such as stearic acid or oleic acid;

fatty acid esters with up to 24 carbon atoms or dicarboxylic acid diesters with up to 24 carbon atoms, such as methyl ester, ethyl ester, isopropyl ester, butyl ester, sec-butyl ester, isobutyl ester, tert-butyl ester or monoglyceric acid ester of acetic acid, caproic acid, lauric acid, myristic acid, stearic acid and palmitic acid, phosphatide derivatives, such as lecithin, terpenes, urea and its derivatives or ethers, such as dimethyl isosorbide and diethylene glycol monoethyl ether.

8. Transdermal system according to claim 7, characterized by a content of at least one of the following penetration intensifiers:

lauryl alcohol, 1,2-propanediol, methyl ester and especially the isopropyl ester of myristic acid or oleic acid, diisopropyl adipate and diisopropyl sebacate, lauric acid and oleic acid, as well as mixtures thereof.

9. Transdermal system according to one of the preceding claims, characterized by an additional content of at least one estrogen such as estradiol, estriol, ethinylestradiol, derivatives thereof such as, for example, mono-esters and diesters such as estradiol-3,17β

-diproprionate.

10. Transdermal system according to one of the preceding claims, characterized by an additional content of at least one stabilizer, such as, for example, β

-cyclodextrin.