PHARMACEUTICAL PREPARATIONS FOR TREATMENTS OF DISEASES AND DISORDERS OF THE BREAST

• US 20110212934A1
• Filed: 08/30/2010
• Published: 09/01/2011
• Est. Priority Date: 01/02/2003
• Status: Active Grant

• Current Assignee: FemmePharma Global Healthcare, Inc. (Apollo Global Management, Inc.)
• Original Assignee: Femmepharma Holding Company Incorporated
• Inventors: Ziemniak, John, Mays, Peter Kevin, DiPiano, Gerianne Tringali
• Granted Patent: US 9,173,836 B2
• Time in Patent Office: Days
• US Class Current: 514/176
• CPC Class Codes: A61K 31/445 Non condensed piperidines, e.g. piperocaine
• 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 47/22 Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
• 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 9/0041 Mammary glands, e.g. breasts, udder; Intramammary administration
• CPC Class Codes: A61K 9/06 Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels composition of ointments, creams or gels A61K47/00
• CPC Class Codes: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: A61P 21/00 Drugs for disorders of the muscular or neuromuscular system

Abstract

Formulations for topical or local administration of drugs directly to the breast or chest to produce a regional or local effect with lower systemic drug levels than when an effective amount is administered systemically are disclosed herein. In a preferred embodiment, the drug is administered to the surface of the breast, areola, or directly to the nipple. The formulations provide increased patient comfort, increased bioavailability and relatively high blood levels in the region to be treated with a reduction of side effects compared to those administered systemically. The preferred formulations contain drugs in the form of micro or nanoparticles, which may be formed of drug alone or in combination with an excipient or carrier. The excipient or carrier may modify the release rates or enhance absorption into the affected area. The drug formulation may be in the form of a cream, lotion or foam.

Claims

1. A drug formulation comprising a drug selected from the group consisting of danazol, bromocriptine, and luteinizing hormone-releasing hormone (LHRH) analogues, in an amount effective to provide regional, not systemic, relief from benign diseases or disorders of the breast in a hydroalcoholic pharmaceutical carrier comprising a transdermal penetration enhancer to promote delivery of the drug across the stratum corneum.

2. The drug formulation of claim 1 wherein the carrier is selected from the group consisting of a gel, ointment, lotion, emulsion, cream, foam, mousse, liquid, spray, and aerosol.

3. The drug formulation of claim 1 wherein the drug is soluble in aqueous solutions.

4. The drug formulation of claim 2 comprising a solublizing agent that improves the solubility of the drug.

5. The drug formulation of claim 4 wherein the solublizing agent is also the penetration enhancer.

6. The drug formulation of claim 4 wherein the drug is in solution.

7. The drug formulation of claim 6, wherein the penetration enhancer is N-methyl-2-pyrrolidone or 2-pyrrolidone.

8. The drug formulation of claim 7 wherein the carrier is a hydroalcoholic gel.

9. The drug formulation of claim 1 wherein the drug is danazol.

10. The drug formulation of claim 1 in a dosage effective to treat benign diseases of the breast.

11. The drug formulation of claim 10 wherein the dosage is between about 40 mg and 80 mg of danazol.

12. A method for treating a disease or disorder of the breast, chest or underlying musculature comprising topically administering to a patient in need thereof a drug formulation comprising a drug selected from the group consisting of danazol, bromocriptine, and luteinizing hormone-releasing hormone (LHRH) analogues, in an amount effective to provide regional, not systemic, relief from benign diseases or disorders of the breast in a hydroalcoholic pharmaceutical carrier comprising a transdermal penetration enhancer to promote delivery of the drug across the stratum corneum.

13. The method of claim 12 wherein the carrier is selected from the group consisting of a gel, ointment, lotion, emulsion, cream, foam, mousse, liquid, spray, and aerosol.

14. The method of claim 13 comprising a solublizing agent that improves the solubility of the drug.

15. The method of claim 14 wherein the solublizing agent is also the penetration enhancer.

16. The method of claim 14 wherein the drug is in solution.

17. The method of claim 16, wherein the penetration enhancer is N-methyl-2-pyrrolidone or 2-pyrrolidone.

18. The method of claim 17, wherein the carrier is a hydroalcoholic gel.

19. The method of claim 18 wherein the drug is danazol.

20. The method of claim 12 in a dosage effective to treat benign diseases of the breast.

21. The method of claim 20 wherein the dosage is between about 40 mg and 80 mg of danazol.

22. The method of claim 12 wherein the benign disease of the breast is selected from the group consisting of mastalgia, mastodynia, Mondor'"'"'s disease, fibrocystic breast disease, costochondritis, mastitis, Paget'"'"'s disease of the areola, fibroadenoma, breast abscess, and breast infections.

23. The method of claim 22 wherein the drug formulation provides a dosage effective for regional treatment.

24. The method of claim 23 wherein the region is the breast, areola, and underlying musculature of the chest.

25. The method of claim 23 wherein the drug is danazol, the carrier is a hydroalcoholic gel, and the penetration enhancer is N-methyl-2-pyrrolidone or 2-pyrrolidone.

26. The method of claim 25 wherein the benign disease of the breast is treatable with danazol.