Compositions and methods

• US 7,198,800 B1
• Filed: 11/22/2000
• Issued: 04/03/2007
• Est. Priority Date: 11/23/1999
• Status: Expired due to Fees

• Current Assignee: Thomas Sai Ying Ko
• Original Assignee: Thomas Sai Ying Ko
• Inventors: Ko, Thomas Sai Ying
• Primary Examiner(s): Padmanabhan; Sreeni
• Assistant Examiner(s): JUSTICE, GINA CHIEUN YU
• Application Number:
  US09/717,088
• Time in Patent Office: 2,323 Days
• Field of Search: 424/443, 424/447, 424/448, 424/449, 424/78.35, 424/61, 525/363, 514/887, 514/494, 602/47, 602/43
• US Class Current: 424/443
• CPC Class Codes: A61K 9/12 Aerosols; Foams A61K9/0043, A61K9/0056, A61K9/006, A61K9/0073 take precedence; spray-films A61K9/7015
• CPC Class Codes: A61K 9/7015 Drug-containing film-forming compositions, e.g. spray-on
• CPC Class Codes: A61L 2300/202 with halogen atoms, e.g. triclosan, povidone-iodine
• CPC Class Codes: A61L 2300/208 Quaternary ammonium compounds
• CPC Class Codes: A61L 2300/404 Biocides, antimicrobial agents, antiseptic agents
• CPC Class Codes: A61L 2300/45 Mixtures of two or more drugs, e.g. synergistic mixtures
• CPC Class Codes: A61L 26/0066 Medicaments; Biocides
• CPC Class Codes: A61L 26/0071 Plasticisers
• CPC Class Codes: A61L 26/0076 Sprayable compositions
• CPC Class Codes: A61P 17/00 Drugs for dermatological disorders
• CPC Class Codes: A61P 17/02 for treating wounds, ulcers, burns, scars, keloids, or the like
• CPC Class Codes: A61P 17/04 Antipruritics
• CPC Class Codes: A61P 17/06 Antipsoriatics
• CPC Class Codes: A61P 31/02 Local antiseptics
• CPC Class Codes: A61P 31/04 Antibacterial agents
• CPC Class Codes: A61P 31/10 Antimycotics
• CPC Class Codes: A61P 37/08 Antiallergic agents antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14

Abstract

Non-aerosol spray-on skin patch compositions as described comprising at least one substantially water insoluble film forming agent, at least one film plasticizer agent, at least one water soluble compound, and at least one organic solvent, the composition forming a flexible, porous and physiologically compatible skin patch when sprayed on to skin and allowed to dry. Also described are methods of improving wound healing by administering a physiologically active ingredient to a patient in need of such treatment.

Claims

1. A non-aerosol sprayable skin patch composition consisting essentially of:

(a) 0.01% to 10% w/w of at least one water-soluble physiologically active ingredient;

(b) 1% to 50% w/w of at least one substantially water insoluble film forming agent selected from the group consisting of acrylic acid, polyacrylic acid, polybutylmethacrylate, polymethacrylic acid, ascorbyl palmitate, carbomer, cellulose acetate phthalate, hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose, ethyl cellulose, hydroxypropyl methlycellulose phthalate, hypomellose phthalate, crospovidone, cetyl alcohol, poloaxmer, polyethylene glycol, polyvinyl acetate, polyvinyl acetate phthalate, polyvinyl alcohol, and povidone;

(c) 0.1% to 20% w/w of at least one film plasticiser agent; and

(d) 30% to 90% w/w of at least one volatile organic solvent,

wherein said composition forms a flexible, porous and physiologically compatible skin patch when sprayed onto skin and is allowed to dry, wherein said patch disintegrates progressively over a 24–

48 hour time period.

2. The composition according to claim 1, wherein said at least one physiologically active ingredient is an antimicrobial agent and/or an antifungal agent.

3. The composition according to claim 2, wherein said antimicrobial agent is a quaternary ammonium compound.

4. The composition according to claim 3, wherein said quaternary ammonium compound is selected from the group consisting of cetrimide, alkylaryltrialkylammonium chloride, alkylaryltrimethylammonium chloride, amantanium bromide, benzalkonium chloride, benzethonium chloride, benzododecinium bromide, cetalkonium chloride, cethexonium bromide, centrimonium bromine, and cetyldimethylethylammonium bromide.

5. The composition according to claim 4, wherein said quaternary ammonium compound is cetrimide.

6. The composition according to claim 2, wherein said water-soluble compound is a mixture of a water-soluble antimicrobial agent and a water-soluble antifungal agent.

7. The compound according to claim 6, wherein said antimicrobial agent is a quaternary ammonium compound and said antifungal agent is selected from the group consisting of chlorbutanol, phenol, salicylic acids, arisoran, amoralfine, amphotericin, bifonazole, butoconazole nitrate, chlormidazole, clotrimazole, croconazole, econazole, enilconazole, fenticonazole, fluconazole, flutrimazole, isoconazole, itraconazole, ketoconazole, lanoconazole, miconazole, omoconazole, saperconazole, sertaconazole, sulconazole, terconazole, tioconazole, benzoyl disulphide, bromochlorosalicylanilide, buclosamide, butenafine, candicidicaprylic acid, chlorphenesin, ciclopirox olamine, cilofungin, fenticlor, flucytosine, criseofulvin, hachimycin, haloprogin, hamycin, hydroxystilbamidine, isethionate, loflucarban, mepartricin, natamycin, nifuroxime, p-nitrophenol, nystatin, pentamycin, propionic acid, protiofate, pyrrolnitrin, sulbentine, terbinafine, tolciclate, tolnaftate, triacetin, and undecenoic acid.

8. The compound according to claim 7, wherein said antifungal agent is chlorbutanol.

9. The composition according to claim 1, wherein said at least one physiologically active ingredient is selected from the group consisting of an antiseptic, an antiparasitic, a nicotine, a cortico steroid, a pain relieving agent, a cardiac dilater, a cardiac stimulant, an antihistamine, an anti-inflammatory, an anti blood clotting agent, a growth hormone, a sex hormone, a drug commonly used for diseases in the alimentary system, central nervous system, musculoskeletal system, genitourinary system allergy or immune system, and a biologically active peptide or protein.

10. The composition according to claim 9, wherein said at least one physiologically active ingredient is triclosan.

11. The composition according to claim 1, wherein the film forming agent is selected from the group consisting of polymethacrylic acid, polybutyl methacrylate and polyacrylic acid.

12. The composition according to claim 1, wherein said film plasticiser agent is polybutylphthalate.

13. The composition according to claim 1, wherein said organic solvent is selected from the group consisting of isopropanol, acetone and ethylacetate.

16. A method of improving wound healing or administering a physiologically active ingredient to a patient comprising spraying on to a wound or on to skin of a patient in need thereof, an effective amount of a composition according to claim 1.

17. A method for the treatment of skin wounds, fungal infections, eczema, bacterial infections in or on the skin and/or associated with skin wounds, athlete'"'"'s foot, skin ulceration, burns, scalds, insect bites, allergic skin diseases, psoriasis, itching and pain, which comprises spraying on to skin in need of such treatment a composition according to claim 1.

14. A non-aerosol sprayable skin patch composition consisting essentially of:

(a) 0.01% to 10% w/w of at least one water-soluble physiologically active ingredient;

(b) 1% to 50% w/w of polymethacrylic acid;

(c) 0.1% to 20% w/w of polybutylphthalate;

(d) 0% to 90% w/w of isopropanol;

(e) 0% to 90% w/w of acetone; and

(f) ethylacetate up to 100% w/w,

wherein said composition forms a flexible, porous and physiologically compatible skin patch when sprayed onto skin and is allowed to dry, and wherein said patch disintegrates progressively over a 24–

48 hour time period.

15. The composition according to claim 14, consisting essentially of:

(a) 0.05% w/w of cetrimide,

(b) 0.07% w/w of triclosan,

(c) 0.6% w/w of chlorbutanol,

(d) 10% w/w of polymethacrylic acid,

(e) 1.2% w/w of polybutylphthalate,

(f) 4% w/w of isopropanol,

(g) 24% w/w of acetone, and

(h) ethylacetate up to 100% w/w.