Pharmaceutical preparations for treatments of diseases and disorders of the breast

• US 7,812,010 B2
• Filed: 01/02/2004
• Issued: 10/12/2010
• Est. Priority Date: 01/02/2003
• Status: Active Grant

• Current Assignee: FemmePharma Global Healthcare, Inc. (Apollo Global Management, Inc.)
• Original Assignee: FemmePharma, Inc.
• Inventors: DiPiano, Gerianne T., Mays, Peter Kevin, Ziemniak, John
• Primary Examiner(s): Kim; Jennifer M
• Application Number:
  US10/751,056
• Publication Number:
  US 20040229813A1
• Time in Patent Office: 2,475 Days
• Field of Search: 514/899, 514/169, 514/171, 424/430, 424/484, 424/400, 424/401
• US Class Current: 514/171
• 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 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: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: A61P 15/14 for lactation disorders, e.g. galactorrhoea
• CPC Class Codes: A61P 21/00 Drugs for disorders of the muscular or neuromuscular system
• CPC Class Codes: A61P 25/02 for peripheral neuropathies
• 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 31/00 Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
• CPC Class Codes: A61P 31/04 Antibacterial agents
• CPC Class Codes: A61P 35/00 Antineoplastic agents
• CPC Class Codes: A61P 5/32 Antioestrogens
• CPC Class Codes: A61P 7/02 Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors

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

danazol in an amount providing regionally effective, not systemically effective, levels of danazol when administered transdermally to the breast, to provide relief from benign diseases or disorders of the breast,

wherein the danazol is formulated in a hydroalcoholic gel comprising N-methyl-2-pyrrolidone or 2-pyrrolidone in an effective amount to solubilize danazol and to deliver danazol across the stratum corneum to the underlying breast tissue.

2. A method for treating a disease or disorder of the breast treatable with danazol comprising

topically administering to the breast of a patient,

a drug formulation comprising an effective amount of danazol in an amount providing regionally effective, not systemically effective, levels of danazol when administered transdermally to the breast tissue, to provide relief from benign diseases or disorders of the breast,

wherein the danazol is formulated in a hydroalcoholic gel comprising N-methyl-2-pyrrolidone or 2-pyrrolidone in an effective amount to solubilize danazol and to deliver danazol across the stratum corneum to the underlying breast tissue.

3. The method of claim 2 wherein the benign disease of the breast is selected from the group consisting of mastalgia, mastodynia, and fibrocystic breast disease.

4. The method of claim 2 wherein the region is the breast, areola, and underlying musculature of the chest.