Transmittal therapeutic systems containing steroid hormones and propylene glycol monocaprylate

• US 20050118244A1
• Filed: 11/16/2002
• Published: 06/02/2005
• Est. Priority Date: 12/01/2001
• Status: Abandoned Application

• Current Assignee: LTS Lohmann Therapie-Systeme AG
• Original Assignee: LTS Lohmann Therapie-Systeme AG
• Inventors: Rubenacher, Rene Eifler, Theobald, Frank
• Application Number:
  US10/497,057
• Publication Number:
  US 20050118244A1
• Time in Patent Office: Days
• US Class Current: 424/449
• CPC Class Codes: A61K 47/14 Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• CPC Class Codes: A61K 9/7061 Polyacrylates
• CPC Class Codes: A61P 15/18 Feminine contraceptives
• CPC Class Codes: A61P 5/24 of the sex hormones
• CPC Class Codes: A61P 5/30 Oestrogens
• CPC Class Codes: A61P 5/34 Gestagens

Abstract

The invention relates to transdermal therapeutic systems containing at least one steroid hormone and propylene glycol monocaprylate as permeation enhancers. The invention also relates to methods for the production of said systems and to the use of the same in hormone substitution therapy and contraception.

Claims

1. A transdermal therapeutic system comprising at least one steroid hormone and propylene glycol monocaprylate as penetration promoter.

2. The transdermal therapeutic system as claimed in claim 1, characterized in that estradiol, ethinylestradiol, progesterone, medroxy-progesterone, hydroxyprogesterone, levonorgestrel, (17α

)-17-hydroxy-11-methylene-19-norpregna-4,15-dien-20-yn-3-one (Org

     30659), norethisterone acetate, norgestrel, lynestrenol, allylestrenol, ethynodiol diacetate or testosterone is used as steroid hormone.

3. The transdermal therapeutic system as claimed in claim 1 or 2, characterized in that it comprises a combination of the active ingredients estradiol or ethinylestradiol with a progestogen.

4. The transdermal therapeutic system as claimed in claim 3, characterized in that it comprises the compound with the name Org 30659 as progestogen.

5. The transdermal therapeutic system as claimed in one or more of the preceding claims, characterized in that the active ingredient-containing matrix consists of a polymer of the group of polyacrylate, polydimethylsiloxane, polyisobutylene, polystyrene, styrene-isoprene-styrene block copolymer, styrene-butadiene-styrene block copolymer, resins, ethylvinyl acetate or of a combination of at least two of these polymers.

6. The transdermal therapeutic system as claimed in one or more of the preceding claims, characterized in that the content of propylene glycol monocaprylate is between 1 and 20% by weight, preferably between 2 and 10% by weight.

7. The transdermal therapeutic system as claimed in one or more of the preceding claims, characterized in that it is intended for hormone replacement therapy.

8. The transdermal therapeutic system as claimed in one or more of claims 1 to 6, characterized in that it is intended for contraception.

9. The use of propylene glycol monocaprylate for increasing the transdermal transport of a steroid hormone active ingredient.

10. The use as claimed in claim 9, characterized in that the relevant steroid hormone is selected from the group comprising estradiol, ethinylestradiol, progesterone, medroxyyprogesterone, hydroxy-progesterone, levonorgestrel, (17α

)-17-hydroxy-11-methylene-19-norpregna-4,15-dien-20-yn-3-one (Org

     30659), noresthisterone acetate, norgestrel, lynestrenol, allylestrenol, ethynodiol diacetate and testosterone.