Modification of percutaneous absorption of topically active materials

• US 20080039405A1
• Filed: 04/20/2007
• Published: 02/14/2008
• Est. Priority Date: 04/25/2006
• Status: Abandoned Application

• Current Assignee: Croda, Inc. (Croda International Plc (Technology Investment Group))
• Original Assignee: Croda, Inc. (Croda International Plc (Technology Investment Group))
• Inventors: Joseph, Laurie, Pereira, Abel, Langley, Nigel
• Application Number:
  US11/788,759
• Publication Number:
  US 20080039405A1
• Time in Patent Office: Days
• US Class Current: 514/29
• 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 9/0014 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: A61K 9/107 Emulsions ; Emulsion preconcentrates; Micelles composition of emulsions A61K47/00

Abstract

The present invention relates to methods of influencing the flux or surface retention time of a topically active pharmaceutical ingredient through skin and formulations relating thereto.

Claims

1. A topical pharmaceutical preparation exhibiting decreased flux or increased skin retention comprising:

a topical active pharmaceutically ingredient in an amount of at least about 0.1% by weight of the final preparation, about 0.1 to about 20% by weight of mixed fatty alcohol phosphate esters comprising at least one alkoxylated fatty alcohol phosphate ester and at least one non-alkoxylated fatty alcohol phosphate ester present in a ration of 80;

20 to 20;

80 and a vehicle, said preparation having an improved flux or increased skin retention time of at least about 10% in 24 hours when compared to the same preparation without said mixed fatty alcohol phosphate esters.

2. The topical pharmaceutical preparation of claim 1 wherein said vehicle is an oil-in-water, water-in-oil or oil-in-oil emulsion.

3. The topical pharmaceutical preparation of claim 1 wherein said topical active pharmaceutically ingredients are vitamins, insect repellents, bioflavonoids, squalenes, salicylic acids, resouncinols, miconazoles, (N,N, diethyl-m-toluamide), tocopherols, tocopherol acetateS, retinoic acids, retinols, retinoids, zinc, benzoyl peroxide, perhydrocyclopentanophenanthrene derivatives including steroids, androgens, progestational hormones, corticosteroids, and estrogen based compounds.

4. The topical pharmaceutical preparation of claim 1 wherein said topical active pharmaceutically ingredient are hydrocortisone, salicylic acid, resouncinol, miconazole, DEET (N,N, diethyl-m-toluamide), tocopherol, tocopherol acetate, retinoic acid, retinol, hydrocortisone, retinoids, sulfur, erythromycin, zinc, and benzoyl peroxide.

5. The topical pharmaceutical preparation of claim 1 further comprising ³H cortisol.

6. The topical pharmaceutical preparation of claim 1 wherein said topical active pharmaceutically ingredient is present in an amount of between about 0.1 and about 50% by weight.

7. The topical pharmaceutical preparation of claim 1 further comprising at least one of an emollient, an emulsifier, a thickener, water, a preservative, a stabilizer, a pH adjusting substance, a color, a solvent, a cosolvent, a dispersion aid, a solid particulate.

8. The topical pharmaceutical preparation of claim 1 whose form is that of a cream, milk, lotion, gel, salve, ointment, spray, mousse, liquid, stick.

9. The topical pharmaceutical preparation of claim 1 further comprising:

a gauze, pad, swab, cotton ball, batting, bandage, patch or occlusive barrier.

19. A method of treating a topical condition in a patient in need thereof comprising:

applying to an afflicted area of a patient the composition of claim 1, maintaining said composition in contact with said afflicted area of said patient, and optionally reapplying said formulation, for a time sufficient to treat said topical condition.

10. A pharmaceutical preparation exhibiting decreased flux or increased skin retention comprising:

a active pharmaceutically ingredient in an amount of at least about 0.1% by weight of the final preparation, about 0.1 to about 20% by weight of mixed fatty alcohol phosphate esters comprising at least one alkoxylated fatty alcohol phosphate ester and at least one non-alkoxylated fatty alcohol phosphate ester present in a ration of 80;

20 to 20;

80 and a vehicle, said preparation having an improved flux or increased skin retention time of at least about 10% in 24 hours when compared to the same preparation without said mixed fatty alcohol phosphate esters.

11. The pharmaceutical preparation of claim 10 wherein said vehicle is an oil-in-water, water-in-oil or oil-in-oil emulsion.

12. The pharmaceutical preparation of claim 10 wherein said active pharmaceutically ingredients are vitamins, insect repellents, bioflavonoids, squalenes, salicylic acids, resouncinols, miconazoles, (N,N, diethyl-m-toluamide), tocopherols, tocopherol acetate, retinoic acids, retinols, retinoids, zinc, benzoyl peroxide, perhydrocyclopentanophenanthrene derivatives including steroids, androgens, progestational hormones, corticosteroids, and estrogen based compounds.

13. The pharmaceutical preparation of claim 10 wherein said active pharmaceutically ingredient are hydrocortisone, salicylic acid, resouncinol, miconazole, DEET (N,N, diethyl-m-toluamide), tocopherol, tocopherol acetates, retinoic acid, retinol, hydrocortisone, retinoids, sulfur, erythromycin, zinc, and benzoyl peroxide.

14. The pharmaceutical preparation of claim 10 further comprising ³H cortisol.

15. The pharmaceutical preparation of claim 10 wherein said active pharmaceutically ingredient is present in an amount of between about 0.1 and about 50% by weight.

16. The pharmaceutical preparation of claim 10 further comprising at least one of an emollient, an emulsifier, a thickener, water, a preservative, a stabilizer, a pH adjusting substance, a color, a solvent, a cosolvent, a dispersion aid, a solid particulate.

17. The pharmaceutical preparation of claim 10 whose form is that of a cream, milk, lotion, gel, salve, ointment, spray, mousse, liquid, stick.

18. The pharmaceutical preparation of claim 10 further comprising:

a gauze, pad, swab, cotton ball, batting, bandage, patch or occlusive barrier.