IP Library Granted Patent US 8,349,297
Granted Patent B2
US 8,349,297 · App. 12/067,004 · Granted Jan 8, 2013

Topical formulations

Assignee: Medpharm Limited
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Quick Facts
Patent No.
US 8,349,297
App. No.
12/067,004
Granted
Jan 8, 2013
Kind
B2
Abstract

Saturated, monophasic solutions of drug in a solvent and propellant mixture, together with a film-forming agent, exhibit transdermal diffusion fluxes greater than those predicted by Fick's law when applied topically.

Claims (33)

1. A pharmaceutical formulation capable of forming a film on topical administration, said formulation comprising a preparation of a pharmaceutical, a solvent therefor, a film-forming agent, and a propellant, wherein the formulation is a monophasic solution and the pharmaceutical is present at at least 80% saturation under conditions of use, and wherein there is no undissolved pharmaceutical in the formulation.

2. The formulation of claim 1 , wherein the pharmaceutical is present at at least 90% saturation.

3. The formulation of claim 1 , wherein the pharmaceutical is present at at least 95% saturation.

4. The formulation of claim 1 , wherein the pharmaceutical is present at, or close to, 100% saturation.

5. The formulation of claim 1 , comprising an antinucleating agent.

6. The formulation of claim 5 , wherein said antinucleating agent is selected from the group consisting of: poly(vinyl alcohol)(PVA), methyl cellulose, ethyl cellulose, hydroxypropylmethylcellulose, hydroxypropylcellulose, glycol esters, polyacrylic acid, and derivatives thereof.

7. The formulation of claim 1 , wherein said pharmaceutical is selected from the group consisting of: local antipruritics; local anaesthetics; antihistamines; corticosteroids; topical preparations for psoriasis; topical preparations for acne; topical antibacterials for acne; dermatological drugs; topical retinoids and related preparations for acne; other topical preparations for acne; topical antibacterials; topical antifungals; antiviral preparations; preparations for minor cuts and abrasions; topical circulatory preparations; heparinoid antiperspirants; non-steroidal anti-inflammatories; actinic keratosis treatments; capsaicin; and combinations thereof.

8. The formulation of claim 1 , for application to a body surface selected from: skin, nail, wounds, oral mucosa, vagina, rectum, anus, nose, and teeth.

9. The formulation of claim 1 , wherein said film-forming agent is selected from the group consisting of polyvinyl pyrrolidone, polyvinyl alcohol, acrylic polymers, acrylic copolymers, methacrylate polymers, methacrylate copolymers, poly (vinyl acetate), cellulose based polymers and cellulose based co-polymers.

10. The formulation of claim 9 , wherein said film-forming component is PVP.

11. The formulation of claim 9 , wherein said film-forming component is PVA.

12. The formulation of claim 1 , wherein said film-forming agent is such that the formulation is capable of forming a hydrogel on skin.

13. The formulation of claim 1 , wherein said film-forming agent is present in an amount of between 0.1 and 40% w/w inclusive.

14. The formulation of claim 13 , wherein said film-forming agent is present in an amount of between 0.1 and 10% w/w inclusive.

15. The formulation of claim 13 , wherein said film-forming agent is present in an amount of between 0.1 and 4% w/w inclusive.

16. The formulation of claim 1 , comprising a plasticiser.

17. The formulation of claim 16 , wherein said plasticiser is selected from the group consisting of: water, glycerol, polyethylene glycol, oleic acid, citric acid, phosphate esters, fatty acid esters, glycol derivatives, hydrocarbons and hydrocarbon derivatives, adipic acid/butanediol polyesters, epoxidised soya oils, diethyl phthalate, dibutyl phthalate, citric acid esters, castor oil, triacetin, chlorinated paraffins, and mixtures thereof.

18. The formulation of claim 16 , wherein said plasticiser is present in an amount of between 0.1 and 40% w/w inclusive.

19. The formulation of claim 16 , wherein said plasticiser is present in an amount of between 0.1 and 10% w/w inclusive.

20. The formulation of claim 16 , wherein said plasticiser is present in an amount of between 0.1 and 4% w/w inclusive.

21. The formulation of claim 1 , wherein said propellant is one or more hydrofluoroalkanes.

22. The formulation of claim 1 , wherein said solvent is selected from the group consisting of: water, cyclomethicone, benzyl alcohol, propylene glycol, polyethylene glycol, propylene carbonate, ethanol, dimethyl sulphoxide, glycerin, isopropyl alcohol, isopropyl myristate, oleic acid, and mixtures thereof.

23. The formulation of claim 22 , wherein said solvent comprises benzyl alcohol in an amount of up to 2.5% w/w.

24. The formulation of claim 1 , wherein said solvent is present in an amount of up to 40%.

25. The formulation of claim 1 , wherein said solvent is selected from the group consisting of: ethanol and isopropyl alcohol.

26. The formulation of claim 25 , wherein said solvent is ethanol in an amount of no more than 15% w/w.

27. The formulation of claim 25 , wherein said solvent is ethanol and the amount of said ethanol is no more than 10% w/w.

28. The formulation of claim 1 , having a pH adjusted to enhance stability of the pharmaceutical.

29. The formulation of claim 1 , comprising a plasticiser selected from the group consisting of: polyethylene glycol, poly(meth)acrylate, polyvinyl pyrrolidone, and combinations thereof.

30. The formulation of claim 29 , comprising between 1 and 5% w/w, inclusive, polyethylene glycol.

31. The formulation of claim 1 , wherein the nature and concentration of the film-forming component are selected such that a film is formed after the evaporation of a portion of the solvent, wherein the film-forming component is selected from the group consisting of polyvinyl pyrrolidone, polyvinyl alcohol, acrylic polymers, acrylic copolymers, methacrylate polymers, methacrylate copolymers, poly (vinyl acetate), cellulose based polymers and cellulose based co-polymers.

32. An aerosol dispenser comprising a reservoir of the formulation of claim 1 .

33. A method for the treatment of a condition with a drug suitable for the treatment of said condition, comprising applying an effective amount of said drug to a patient in need thereof by administering the formulation of claim 1 to a topical surface of said patient.

Assignments (4)
SECURITY INTEREST Recorded Jul 1, 2024
From: MEDPHARM LIMITED
To: ORBIMED ROYALTY & CREDIT OPPORTUNITIES IV, LP
Reel/Frame 067881/0666 →
RELEASE OF SECURITY INTEREST Recorded Jan 17, 2024
From: WELLS FARGO BANK, NATIONAL ASSOCIATION
To: MEDPHARM LIMITED
Reel/Frame 066155/0458 →
PATENT SECURITY AGREEMENT Recorded Jan 4, 2021
From: MEDPHARM LIMITED
To: WELLS FARGO BANK, NATIONAL ASSOCIATION
Reel/Frame 054892/0506 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 24, 2008
From: BROWN, MARC BARRY; JONES, STUART ALLEN
To: MEDPHARM LIMITED
Reel/Frame 021141/0135 →
Priority Claims (1)
GB 0518769.5 · Sep 14, 2005 · national
Continuity (1)
Related Publication 20090191271A1 · Jul 30, 2009