Topical pharmaceutical composition based on semifluorinated alkanes

Patent metadata

Field	Value
Publication number	US-10130707-B2
Application number	US-201214122044-A
Country	US
Kind code	B2
Filing date	May 24, 2012
Priority date	May 25, 2011
Publication date	Nov 20, 2018
Grant date	Nov 20, 2018

Abstract

The invention provides liquid or semi-solid pharmaceutical compositions for topical administration comprising a semifluorinated alkane. The compositions are useful for the delivery of active ingredients into the deep layers of the skin or skin appendages. Various active ingredients may be incorporated, such as immunosuppressants, antiinfectives, antifungal agents, antiinflammatory agents, and retinoids.

First claim

The invention claimed is:

1. A method for the prevention or treatment of a disease or condition affecting the skin, wherein the disease or condition affecting the skin is psoriasis, comprising administering to the skin a topical pharmaceutical composition comprising an effective amount of an active ingredient which is an immunosuppressant selected from tacrolimus, sirolimus, and ciclosporin A, and a semifluorinated alkane according to formula
RFRH
wherein RF is a linear perfluorinated hydrocarbon segment with 4 to 12 carbon atoms, and RH is a linear alkyl group with 4 to 8 carbon atoms; wherein the semifluorinated alkane is selected from F4H5 and F6H8, wherein F means a perfluorinated hydrocarbon segment, H means a non-fluorinated segment, and the number is the number of carbon atoms of the respective segment;
and wherein the composition is in the form of a liquid solution; and
wherein the composition comprises a physiologically acceptable cosolvent selected from ethanol, isopropyl alcohol, glycerol, and propylene glycol.

2. The method of claim 1 , wherein the semifluorinated alkane is F6H8.

3. The method of claim 1 , wherein the composition is in the form of a single-phase liquid solution.

4. The method of claim 1 , wherein the semifluorinated alkane is F4H5.

5. The method of claim 1 , wherein the disease or condition affects the vital epidermis, dermis, and/or hypodermis of the skin.

6. The method of claim 1 , wherein the active ingredient is delivered to the vital layers below the stratum corneum of the epidermis.

7. The method of claim 1 , wherein the method is for the prevention or treatment of skin affected by psoriasis, and wherein the topical pharmaceutical composition is administered to the skin.

8. The method of claim 1 , wherein the immunosuppressant is tacrolimus.

9. The method of claim 4 , wherein the physiologically acceptable cosolvent is selected from ethanol and isopropyl alcohol.

10. The method of claim 2 , wherein the immunosuppressant is tacrolimus.

11. The method of claim 1 , wherein the physiologically acceptable co-solvent is selected from ethanol and isopropyl alcohol.

12. The method of claim 2 , wherein the physiologically acceptable co-solvent is selected from ethanol and isopropyl alcohol.

13. The method of claim 10 , wherein the physiologically acceptable co-solvent is selected from ethanol and isopropyl alcohol.

14. The method of claim 1 , wherein the physiologically acceptable co-solvent is ethanol.

15. The method of claim 2 , wherein the physiologically acceptable co-solvent is ethanol.

16. The method of claim 10 , wherein the physiologically acceptable co-solvent is ethanol.

17. The method of claim 14 , wherein the ethanol is present at a concentration of up to 5 wt %.

18. The method of claim 15 , wherein the ethanol is present at a concentration of up to 5 wt %.

19. The method of claim 16 , wherein the ethanol is present at a concentration of up to 5 wt %.

Assignees

• Gunther Bernhard
• Theisinger Bastian
• Theisinger Sonja
• Scherer Dieter
• Novaliq Gmbh

Inventors

• Gunther Bernhard
• Theisinger Bastian
• Theisinger Sonja
• Scherer Dieter

Classifications

• A61P37/08

  Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14) · CPC title

• A61P37/06

  Immunosuppressants, e.g. drugs for graft rejection · CPC title

• A61P31/12

  Antivirals · CPC title

• A61P31/04

  Antibacterial agents · CPC title

• A61P29/00

  Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] · CPC title