Transdermal therapeutic system based on polyacrylate-contact-bonding adhesives without functional groups

• US 20040241219A1
• Filed: 02/20/2004
• Published: 12/02/2004
• Est. Priority Date: 08/24/2001
• Status: Abandoned Application

• Current Assignee: LTS Lohmann Therapie-Systeme AG
• Original Assignee: LTS Lohmann Therapie-Systeme AG
• Inventors: Hille, Thomas, Theobald, Frank, Klein, Ursula Hildegard
• Application Number:
  US10/487,380
• Publication Number:
  US 20040241219A1
• Time in Patent Office: Days
• US Class Current: 424/449
• CPC Class Codes: A61K 9/7061 Polyacrylates
• CPC Class Codes: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: A61P 15/08 for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
• CPC Class Codes: A61P 15/12 for climacteric disorders
• CPC Class Codes: A61P 15/18 Feminine contraceptives
• CPC Class Codes: A61P 5/18 of the parathyroid hormones
• CPC Class Codes: A61P 5/24 of the sex hormones

Abstract

The invention relates to a transdermal therapeutic system (TTS) consisting of a rear layer, a protective layer and an active-substance-containing polymer layer. The polymer matrix comprises a polyacrylate which contains an extremely reduced number of functional groups. In one particular embodiment, the polyacrylate is free from hydroxyl groups and/or carboxyl groups.

Claims

1. A transdermal therapeutic system comprising back layer, protective layer and at least one active-compound-containing polymer matrix comprising a polyacrylate, the polyacrylate being a homopolymer, copolymer or block copolymer which can be prepared by polymerization of a monomer mixture consisting of:

a) a monomer or a mixture of monomers from the group consisting of the esters of acrylic or methacrylic acid, which carry linear, branched and/or cyclic aliphatic C₁-C₁₂ substituents without another functional group,

b) acrylic acid, methacrylic acid, 2-hydroxyethyl acrylate, 2-hydroxyethyl methacrylate, 3-hydroxypropyl acrylate and/or 3-hydroxypropyl methacrylate, the content of these monomers in the total being below 2% by weight,

c) vinyl acetate in a content of below 20% by weight,

d) crosslinkers in a content of below 0.5% by weight

e) auxiliaries from the group consisting of the antioxidants, stabilizers and/or alkylmercaptans in a content of below 0.1% by weight.

2. The transdermal therapeutic system as claimed in claim 1, characterized in that the polymerization of the monomer mixture is carried out by ionic, free-radical or light-induced means, in water which can contain emulsifiers or in organic solvents as a reaction medium.

3. The transdermal therapeutic system as claimed in claim 1 or 2, characterized in that the monomer mixture contains vinyl acetate in a content of below 5% by weight.

4. The transdermal therapeutic system as claimed in one or more of claims 1 to 3, characterized in that aluminum acetylacetonate, allyl glycidyl ether and/or glycidyl methacrylate is used in the monomer mixture as a crosslinker.

5. The transdermal therapeutic system as claimed in one or more of claims 1 to 4, characterized in that the group of esters of acrylic or methacrylic acid which contain linear, branched and/or cyclic aliphatic C₁-C₁₂ substituents without another functional group consists of n-butyl acrylate, n-butyl methacrylate, ethyl acrylate, 2-ethylhexyl acrylate, ethyl methacrylate, methyl acrylate, methyl methacrylate, tert-butyl acrylate, sec-butyl acrylate, tert-butyl methacrylate, cyclohexyl methacrylate, 2-ethylhexyl methacrylate, isobornyl methacrylate, isobutyl methacrylate, isopropyl acrylate, isopropyl methacrylate and mixtures of these monomers.

6. The transdermal therapeutic system as claimed in one or more of claims 1 to 5, characterized in that the monomer mixture is free of acrylic acid, methacrylic acid, 2-hydroxyethyl acrylate, 2-hydroxyethyl methacrylate, 3-hydroxypropyl acrylate and/or 3-hydroxypropyl methacrylate.

7. The transdermal therapeutic system as claimed in one or more of claims 1 to 6, characterized in that the active compound is a pharmaceutically active substance from the group consisting of the α

-adrenoreceptor agonists, the β

-adrenoreceptor agonists, the α

-adrenoreceptor blockers, the β

-adrenoreceptor blockers, the analgesics (narcotics), the analgesics (non-narcotics), the androgens, the anesthetics, the antiallergics, the antiandrogens, the antianginals, the antiarrhythmics, the penicillins, the antidiabetics, the antihistaminics, the antimigraine agents, the hydrogenated ergot alkaloids, the Ca antagonists, the serotonin antagonists, the platelet aggregation inhibitors, the anti-depressants, the bronchodilators, the estrogens, the gestagens, the vasodilators and nicotine.

8. The transdermal therapeutic system as claimed in one or more of claims 1 to 7, characterized in that the active compound is a hormone or a combination of hormones.

9. The transdermal therapeutic system as claimed in claim 8, characterized in that the hormone is 17β

-estradiol, ethinylestradiol, estradiol acetate, levonorgestrel, norethindrone, norethindrone acetate or testosterone.

10. The use of a transdermal therapeutic system as claimed in one of claims 1 to 9 for the treatment of hypogonadism, for hormone substitution therapy or for contraception.