Pharmaceutical composition for the treatment of psoriasis and other skin diseases

• US 20040225140A1
• Filed: 06/11/2004
• Published: 11/11/2004
• Est. Priority Date: 12/12/2001
• Status: Abandoned Application

• Current Assignee: Larranaga Lazcano, Pidal Fernandez, Tomasi Sciano
• Original Assignee: Larranaga Lazcano, Pidal Fernandez, Tomasi Sciano
• Inventors: Fernandez, Pidal, Sciano, Tomasi, Lazcano, Larranaga
• Application Number:
  US10/865,991
• Publication Number:
  US 20040225140A1
• Time in Patent Office: Days
• US Class Current: 552/500
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/57 substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
• CPC Class Codes: A61K 31/573 substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
• 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 8/63 Steroids; Derivatives thereof
• CPC Class Codes: A61K 9/0014 Skin, i.e. galenical aspects of topical compositions non-active ingredients are additionally classified in A61K47/00; A61K9/0009, A61K9/0021, A61K9/7015, A61K9/7023 take precedence; cosmetic preparations A61K8/00, A61Q; preparations for wound dressings or bandages A61L26/00
• CPC Class Codes: A61P 17/00 Drugs for dermatological disorders
• CPC Class Codes: A61P 17/06 Antipsoriatics
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 37/00 Drugs for immunological or allergic disorders
• CPC Class Codes: A61P 37/08 Antiallergic agents antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14
• CPC Class Codes: A61Q 19/00 Preparations for care of the skin
• CPC Class Codes: C07J 7/00 Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms C07J5/00 takes precedence

Abstract

The invention relates to a pharmaceutical composition for the treatment of psoriasis and other skin diseases. The inventive composition comprises 17-clobetasol propionate and a hydroxyl derivative of progesterone having formula (I) wherein: R6 denotes H or methyl; R11 denotes H or hydroxyl; and R17 denotes H or hydroxyl, but R11 and R17 cannot be H simultaneously. Preferably, said composition is administered as a lotion with: 0.05-2% 17-clobetasol propionate; 0.3-1% of (I); a solvent selected from among ethanol, isopropanol and mixtures thereof; 40% cosolvent selected from among propylene glycol, glycerine, sorbitol and mixtures thereof; and 20% water. In the ideal lotion, the solvent is ethanol and the cosolvents are approximately: 35% propylene glycol, 5% glycerine and 20% water. The invention affords the following advantages: longer interval between recurrences and fewer local secondary effects. Moreover, the inventive composition can be used for the treatment of psoriasis.

Claims

1. A composition for topical administration that comprises a therapeutically effective amount of 17-clobetasol propionate, and a therapeutically effective amount of a hydroxy derivative of progesterone having formula (I), or of one of its pharmaceutically acceptable esters,

2. The composition according to claim 1, wherein the respective therapeutically effective amounts of 17-clobetasol propionate, and of a hydroxy derivative of progesterone having formula (I), or of one of its pharmaceutically acceptable esters, are therapeutically effective amounts for pharmaceutical or cosmetic formulations.

3. The composition according to claim 1, wherein R6 is hydrogen, R11 is hydroxyl and R17 is hydrogen.

4. The composition according to claim 3, wherein the hydroxy derivative of progesterone having formula (I) is 11-α

-hydroxyprogesterone.

5. The composition according to claim 3, wherein the hydroxy derivative of progesterone having formula (I) is 11 -α

-hydroxyprogesterone, and its pharmaceutically acceptable ester is acetate.

6. The composition according to claim 1, wherein R6 is hydrogen, R11 is hydrogen and R17 is hydroxyl.

7. The composition according to claim 6, wherein the hydroxy derivative of progesterone having formula (I) is 17-α

-hydroxyprogesterone.

8. The composition according to claim 6, wherein the hydroxy derivative of progesterone having formula (I) is 17-α

-hydroxyprogesterone, and its pharmaceutically acceptable ester is acetate or hexanoate.

9. The composition according to claim 1, wherein R6 is methyl, R11 is hydrogen and R17 is hydroxyl.

10. The composition according to claim 9, wherein the hydroxy derivative of progesterone having formula (I) is medroxyprogesterone.

11. The composition according to claim 9, wherein the hydroxy derivative of progesterone having formula (I) is medroxyprogesterone, and its pharmaceutically acceptable ester is acetate.

12. The composition according to claim 1, wherein the topical formulation is a galenic topical form selected from a cream, a pomade, a gel, a solution, an emollient, a direct lotion or a spray lotion, any of which having one or more pharmaceutically acceptable monoalcohols as a dissolvent, and one or more pharmaceutically acceptable polyols as co-dissolvents at a proportion between 20% and 50%, in addition to water at a proportion between 10% and 30%.

13. The composition according to claim 12, wherein the monoalcohol dissolvent is selected from ethanol, isopropanol and its combinations, and the polyol co-dissolvent is selected from propylene glycol, glycerin, sorbitol and its combinations.

14. The composition according to claim 1, wherein the amount of 17-clobetasol propionate is between 0.05% and 0.4% in weight, and the amount of hydroxy derivative of progesterone having formula (I) or its pharmaceutically acceptable ester is between 0.1% and 1.5%.

15. The composition according to claim 1, wherein the amount of 17-clobetasol propionate is between 0.1% and 0.2% in weight, and the amount of hydroxy derivative of progesterone having formula (I) or its pharmaceutically acceptable ester is between 0.3% and 1%.

16. The composition according to claim 1, further comprising adequate amounts of one or any combination of excipients, stabilizers, preservatives, perfumes acceptable for pharmaceutical or cosmetic formulations for topical administration.

17. The composition according to claim 1, wherein the 17-clobetasol propionate, the hydroxy derivative of progesterone having formula (I), or one of its pharmaceutically acceptable esters is one of a stereoisomer, solvate or hydrate.

18. A method for the preparation of a composition for topical administration for the treatment of inflammatory or allergic skin diseases comprising:

combining a 17-clobetasol propionate with a hydroxy derivative of progesterone having formula (I), or with any of its pharmaceutically acceptable esters,

19. A method of use of a composition in topical administration to skin, the method comprising:

obtaining a combination of a 17-clobetasol propionate with a hydroxy derivative of progesterone having formula (I), or with any of its pharmaceutically acceptable esters,

and,

applying the combination of a 17-clobetasol propionate, hydroxy derivative of progesterone having formula (I), or its pharmaceutically acceptable ester, to skin.

20. A method of use according to claim 19 wherein the use is a treatment of a human suffering from a skin inflammatory or allergic disease, wherein the skin disease is psoriasis.