USE OF SEMI-FLUORINATED ALKANES IN TRANSDERMAL THERAPEUTIC SYSTEMS

• US 20170182060A1
• Filed: 05/07/2015
• Published: 06/29/2017
• Est. Priority Date: 05/13/2014
• Status: Active Application

• Current Assignee: Novaliq GmbH
• Original Assignee: LTS Lohmann Therapie-Systeme AG
• Inventors: SCHERER, Dieter, WIEDERSBERG, Sandra, GNTHER, Bernhard
• Application Number:
  US15/309,595
• Publication Number:
  US 20170182060A1
• Time in Patent Office: Days
• CPC Class Codes: A61K 31/381 having five-membered rings
• CPC Class Codes: A61K 31/485 Morphinan derivatives, e.g. morphine, codeine
• CPC Class Codes: A61K 31/565 not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
• CPC Class Codes: A61K 31/568 substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
• CPC Class Codes: A61K 47/06 Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
• 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 47/24 containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
• CPC Class Codes: A61K 9/7084 Transdermal patches having a drug layer or reservoir, and one or more separate drug-free skin-adhesive layers, e.g. between drug reservoir and skin, or surrounding the drug reservoir; Liquid-filled reservoir patches

Abstract

The invention relates to the use of semi-fluorinated alkanes, in particular mixed with ethanol, as solubilising agents, permeation promoters and/or enhancers for lipophilic and/or poorly skin-permeable pharmaceutical agents that are administered via a transdermal therapeutic system (TTS), and to corresponding TTSs containing such substances.

Claims

1. A transdermal therapeutic system (TTS) for applying active pharmaceutical ingredients across the human skin, characterized in that the active pharmaceutical ingredient(s) is/are present in combination with one or more semifluorinated alkanes (SFAs).

2. The TTS as claimed in claim 1, characterized in that the active pharmaceutical ingredient(s) is/are in dissolved, suspended, or emulsified form in an SFA or in a mixture of multiple SFAs.

3. The TTS as claimed in claim 1 or 2, characterized in that the SFAs are linear alkanes of the general formula FnHm, where F is a perfluorinated segment of the molecule, H is a nonfluorinated segment, of the molecule and n and m are independently the number of carbon atoms in the particular segment.

4. The TTS as claimed in claim 3, characterized in that, n=4-12 and m=4-10.

5. The TTS as claimed in claim 3 or 4, characterized in that FnHm is F4H5, F4H6, F4H8, F6H4, F6H6, F6H8 or F6H_10.

6. The TTS as claimed in any of claims 1 to 5, characterized in that the SFA or the SFAs is/are present in combination with a monohydric or polyhydric alcohol.

7. The TTS as claimed in claim 6, characterized in that the alcohol is a monohydric alcohol.

8. The TTS as claimed in claim 6 or 7, characterized in that the alcohol is ethanol.

9. The TTS as claimed in any of claims 6 to 8, characterized in that the volume ratio of SFA or SFAs to alcohol is from 5:

1 to 1;

5.

10. The TTS as claimed in any of claims 1 to 9, characterized in chat the active ingredient is a lipophilic and/or sparingly skin-permeable active ingredient.

11. The TTS as claimed in any of claims 1 to 10, characterized in that the active ingredient is one or more active ingredients selected from the group:

testosterone, estradiol, buprenorphine, rotigotine and other hormones.

12. The TTS as claimed in any of claims 1 to 11, characterized in that the fraction of active ingredient in the active-ingredient-containing preparation is 0.1-50% by weight.

13. The TTS as claimed in any of claims 1 to 12, characterized in that the TTS is a reservoir or liquid reservoir system.

14. The use of SFA or SFAs alone or in a mixture with monohydric or polyhydric alcohols as solubilizer, permeation promoter and/or enhancer for active pharmaceutical ingredients in a TTS as claimed in any of claims 1 to 13.

15. The use as claimed in claim 14, characterized in that a mixture of one or more SFAs with ethanol is used.