Pharmaceutical formulations of resveratrol and methods of use thereof

• US 6,414,037 B1
• Filed: 10/29/1999
• Issued: 07/02/2002
• Est. Priority Date: 01/09/1998
• Status: Expired due to Fees

• Current Assignee: Pharmascience Incorporated (Joddes Limitã©E)
• Original Assignee: Pharmascience Incorporated (Joddes Limitã©E)
• Inventors: Moon, Richard C., Lin, Shengzhao, Ouali, Aomar, Jang, Mei-Shiang, Barillas, Karla Slowing, Pezzuto, John M.
• Primary Examiner(s): Fay, Zohreh
• Assistant Examiner(s): KWON, YONG SOK
• Application Number:
  US09/430,337
• Time in Patent Office: 977 Days
• Field of Search: 514/733, 514/736, 514/734
• US Class Current: 514/733
• CPC Class Codes: A23L 33/105 Plant extracts, their artificial duplicates or their derivatives
• CPC Class Codes: A61K 31/05 Phenols cannabinoids A61K31/658
• CPC Class Codes: A61K 31/7034 attached to a carbocyclic compound, e.g. phloridzin
• 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 47/14 Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• CPC Class Codes: A61K 47/36 Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
• CPC Class Codes: A61K 47/549 Sugars, nucleosides, nucleotides or nucleic acids
• CPC Class Codes: A61K 8/347 Phenols
• CPC Class Codes: A61K 8/60 Sugars; 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: A61K 9/0019 Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner non-active ingredients are additionally classified in A61K47/00
• CPC Class Codes: A61K 9/1075 Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers A61K9/0026 takes precedence
• CPC Class Codes: A61P 17/00 Drugs for dermatological disorders
• CPC Class Codes: A61P 17/06 Antipsoriatics
• CPC Class Codes: A61P 17/12 Keratolytics, e.g. wart or anti-corn preparations
• CPC Class Codes: A61P 17/16 Emollients or protectives, e.g. against radiation
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: A61Q 19/08 Anti-ageing preparations
• CPC Class Codes: B82Y 5/00 Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery

Abstract

A method is provided for preventing or treating skin conditions, disorders or diseases, such as may be associated with or caused by inflammation, sun damage or natural aging. The method involves administration, preferably topical administration, of an active agent selected from the group consisting of resveratrol, pharmacologically acceptable salts, esters, amides, prodrugs and analogs thereof, and combinations of any of the foregoing. Pharmaceutical formulations for use in conjunction with the aforementioned method are provided as well.

Claims

1. A method for treating an individual susceptible to or afflicted with a skin condition, disorder or disease selected from the groups consisting of psoriasis, contact dermatitis, atopic dermatitis, actinic keratosis, a keratinization disorder, an epidermolysis bullosa disease, exfoliative dermatitis, seborrheic dermatitis, erythema multiforme, erythema nodosum, discoid lupus erythematosus, and dermatomyositis, comprising administering to the susceptible or affected area of the individual'"'"'s skin a therapeutically effective anti-inflammatory amount of a topical pharmaceutical formulation that comprises a topical carrier and an active agent selected from the group consisting of resveratrol, pharmacologically acceptable salts, esters, amides, prodrugs and analogs thereof, and combinations of any of the foregoing.

2. The method of claim 1, wherein the active agent is cis-resveratrol or a pharmacologically acceptable salt, ester, amide, prodrug or analog thereof.

3. The method of claim 2, wherein the active agent is cis-resveratrol.

4. The method of claim 2, wherein the active agent is a conjugate of cis-resveratrol and a mono- or di-saccharide.

5. The method of claim 4, wherein the active agent is cis-resveratrol glucoside.

6. The method of claim 1, wherein the active agent is trans-resveratrol or a pharmacologically acceptable salt, ester, amide, prodrug or analog thereof.

7. The method of claim 6, wherein the active agent is trans-resveratrol.

8. The method of claim 6, wherein the active agent is a conjugate of trans-resveratrol and a mono- or di-saccharide.

9. The method of claim 8, wherein the active agent is trans-resveratrol glucoside.

10. The method of claim 1, wherein the active agent comprises a mixture of cis-resveratrol and trans-resveratrol.

11. The method of claim 1, wherein the topical pharmaceutical formulation comprises an ointment, lotion, cream, emulsion, microemulsion, gel or solution.

12. The method of claim 1, wherein the topical pharmaceutical formulation contains approximately 0.25 wt. % to 75 wt. % active agent.

13. The method of claim 12, wherein the topical pharmaceutical formulation contains approximately 0.25 wt. % to 30 wt. % active agent.

14. The method of claim 13, wherein the topical pharmaceutical formulation contains approximately 0.5 wt. % to 15 wt. % active agent.

15. The method of claim 14, wherein the topical pharmaceutical formulation contains approximately 1.0 wt. % to 10 wt. % active agent.

16. The method of claim 1, wherein the topical pharmaceutical formulation is administered at least once daily.

17. The method of claim 16, wherein the topical pharmaceutical formulation is administered one to four times daily.

18. A method for preventing or treating an individual susceptible to or afflicted with a skin condition, disorder or disease selected from the group consisting of psoriasis, contact dermatitis, atopic dermatitis, actinic keratosis, a keratinization disorder, an epidermolysis bullosa disease, exfoliative dermatitis, seborrheic dermatitis, erythema multiforme, erythema nodosum, discoid lupus erythematosus, and dermatomyositis, comprising administering to a susceptible or affected individual a pharmaceutical formulation comprised of an isotropically clear dispersion containing a therapeutically effective anti-inflammatory amount of an active agent selected from the group consisting of resveratrol, pharmacologically acceptable salts, esters, amides, prodrugs and analogs thereof, and combinations of any of the foregoing.

19. The method of claim 18, wherein the active agent is cis-resveratrol or a pharmacologically acceptable salt, ester, amide, prodrug or analog thereof.

20. The method of claim 19, wherein the active agent is cis-resveratrol.

21. The method of claim 19, wherein the active agent is a conjugate of cis-resveratrol and a mono- or di-saccharide.

22. The method of claim 21, wherein the active agent is cis-resveratrol glucoside.

23. The method of claim 18, wherein the active agent is trans-resveratrol or a pharmacologically acceptable salt, ester, amide, prodrug or analog thereof.

24. The method of claim 23, wherein the active agent is trans-resveratrol.

25. The method of claim 23, wherein the active agent is a conjugate of trans-resveratrol and a mono- or di-saccharide.

26. The method of claim 25, wherein the active agent is trans-resveratrol glucoside.

27. The method of claim 18, wherein the active agent comprises a mixture of cis-resveratrol and trans-resveratrol.

28. The method of claim 18, wherein the formulation comprises approximately 0.25 wt. % to 75 wt. % active agent.

29. The method of claim 28, wherein the formulation comprises approximately 0.25 wt. % to 30 wt. % active agent.

30. The method of claim 29, wherein the formulation comprises approximately 0.5 wt. % to 15 wt. % active agent.

31. The method of claim 30, wherein formulation comprises approximately 1.0 wt. % to 10 wt. % active agent.

32. The method of claim 18, wherein the topical pharmaceutical formulation is administered at least once daily.

33. The method of claim 32, wherein the topical pharmaceutical formulation is administered one to four times daily.

34. The method of claim 18, wherein the formulation is administered orally.

35. The method of claim 18, wherein the formulation is administered parenterally.

36. The method of claim 18, wherein the formulation is administered at least once daily.

37. The method of claim 36, wherein the formulation is administered one to four times daily.