Polymeric topical compositions

• US 8,481,591 B2
• Filed: 11/01/2010
• Issued: 07/09/2013
• Est. Priority Date: 11/01/2010
• Status: Active Grant

• Current Assignee: Stiefel Research Australia Pty Limited (GSK plc)
• Original Assignee: Stiefel Research Australia Pty Limited (GSK plc)
• Inventors: Sawant, Prashant
• Primary Examiner(s): BLAND, LAYLA D
• Application Number:
  US12/916,692
• Publication Number:
  US 20120108527A1
• Time in Patent Office: 981 Days
• Field of Search: None
• US Class Current: 514/460
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/192 having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid cannabinoids A61K31/658
• CPC Class Codes: A61K 31/203 Retinoic acids ; Salts thereof
• CPC Class Codes: A61K 31/351 not condensed with another ring
• CPC Class Codes: A61K 31/4164 1,3-Diazoles
• CPC Class Codes: A61K 31/4174 Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole
• CPC Class Codes: A61K 31/573 substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
• CPC Class Codes: A61K 31/7056 containing five-membered rings with nitrogen as a ring hetero atom
• CPC Class Codes: A61K 31/728 Hyaluronic acid
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• 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 47/32 Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers , poly(meth)acrylates, or polyvinyl pyrrolidone
• CPC Class Codes: A61K 47/34 Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers A61K47/10 takes precedence
• 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 9/08 Solutions composition of solutions A61K47/00
• 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 17/10 Anti-acne agents
• CPC Class Codes: A61P 31/00 Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
• CPC Class Codes: A61P 31/04 Antibacterial agents

Abstract

The present invention relates to topical antibacterial compositions. The compositions comprise an antibacterial agent such as mupirocin, water, a polymer and a volatile solvent present in an amount of less than about 40%. The invention also relates to methods of treatment by administering the compositions to a patient in need thereof, and to the use of such compositions in the treatment of bacterial conditions.

Claims

1. A topical pharmaceutical composition comprising:

(a) calcium mupirocin,

(b) a polyvinvylpyrrolidone-vinyl acetate (PVP/VA) co-polymer in an amount from about 30% to about 60% by weight,

(c) water in an amount from about 20% to about 40% by weight, and

(d) a volatile solvent in an amount from about 10% to about 25% by weight; and

optionally a gelling agent, and other dermatologically acceptable excipients thereof.

2. The composition according to claim 1 wherein the volatile solvent is a mixture of at least two volatile solvents, and wherein the first volatile solvent is ethanol.

3. The composition according to claim 1 wherein the ratio of PVP monomer to VA monomer in the PVP/VA copolymer is from about 30:

70 to about 70;

30.

4. The composition according to claim 1 wherein the PVP/VA copolymer is solublized in the composition.

5. The composition according to claim 1 wherein the volatile solvent is selected from ethanol, propanol, iso-propanol, n-butyl alcohol, t-butyl alcohol, butoxy ethanol, acetone, ethyl acetate or butyl acetate.

6. The composition according to claim 1 wherein the dermatologically acceptable excipients are selected from the group consisting of a co-solvent, a pH adjusting agent, a humectant, a film extender, a chelating agent, an antioxidant, a preservative, a fragrance, a colorant, a penetration enhancer, and a combination or mixture thereof.

7. The composition according to claim 1 wherein the gelling agent is xanthan gum.

8. The composition according to claim 1 wherein the topical pharmaceutical composition further comprises a second pharmaceutically acceptable active agent.

9. The composition according to claim 1 wherein the volatile solvent is ethanol.

10. The composition according to claim 1 wherein the calcium mupirocin is present in an amount from about 0.1% to about 10% by weight.

11. The composition according to claim 2 wherein the volatile solvent is a mixture of ethanol and iso-propanol.

12. The composition according to claim 2 wherein the volatile solvent is a mixture of ethanol and ethyl acetate.

13. The composition according to claim 3 wherein ratio of PVP monomer to VA monomer in the PVP/VA copolymer is about 30:

70 and wherein the composition is free of hexylene glycol.

14. The composition according to claim 3 wherein the ratio of PVP monomer to VA monomer in the PVP/VA is about 60:

40.

15. The composition according to claim 5 wherein the volatile solvent is ethanol.

16. The composition according to claim 5 wherein the dermatologically acceptable excipients are selected from the group consisting of a co-solvent, a pH adjusting agent, a humectant, a film extender, a chelating agent, an antioxidant, a preservative, a fragrance, a colorant, a penetration enhancer, and a combination or mixture thereof.

17. The composition according to claim 6 which composition is substantially devoid or devoid of a co-solvent.

18. The composition according to claim 6 wherein the co-solvent is selected from an alcohol, a carboxylic acid, a diol, a polyol or a combination or mixture thereof, present in an amount from about 1% to about 30% by weight.

19. The composition according to claim 6 wherein the co-solvent is a mixture of polyethylene glycol and propylene glycol.

20. The composition according to claim 8 wherein the second pharmaceutically acceptable active agent is selected from the group consisting of a second antibacterial agent, a retinoid, a corticosteroid, an antifungal agent, a skin conditioning agent, a nutritional agent, or an antiseptic agent.

21. The composition according to claim 8 wherein the second pharmaceutically acceptable active agent is mupirocin, clotrimazole, clobetasol propionate or hyaluronic acid.

22. The composition according to claim 10 wherein the calcium mupirocin is present in an amount from about 1% to about 3% by weight.

23. The composition according to claim 16 wherein the gelling agent is xanthan gum.

24. The composition according to claim 16 wherein the at least one co-solvent is selected from an alcohol, a carboxylic acid, a diol, a polyol or a combination or mixture thereof, present in an amount from about 1% to about 30% by weight.

25. The composition according to claim 18 wherein the alcohol is selected from amyl alcohol, benzyl alcohol, cyclohexanedimethanol, diacetone alcohol, hexyl alcohol, or tetrahydrofurfuryl alcohol;

and the diol is selected from 1,2-hexanediol, butylene glycol, diethylene glycol, dipropylene glycol, ethyl hexanediol, ethylene glycol, hexylene glycol, pentylene glycol, propylene glycol, tetraethylene glycol, triethylene glycol, or tripropylene glycol; and

the polyol is selected from polyethylene glycol, butanetriol, glycerol or 1,2,6-hexanetriol.

26. The composition according to claim 18 wherein the co solvent is propylene glycol.

27. The composition according to claim 22 wherein the calcium mupirocin is present in an amount of about 2% by weight.

28. The composition according to claim 24 wherein the alcohol is selected from amyl alcohol, benzyl alcohol, cyclohexanedimethanol, diacetone alcohol, hexyl alcohol, or tetrahydrofurfuryl alcohol;

and the diol is selected from 1,2-hexanediol, butylene glycol, diethylene glycol, dipropylene glycol, ethyl hexanediol, ethylene glycol, hexylene glycol, pentylene glycol, propylene glycol, tetraethylene glycol, triethylene glycol, or tripropylene glycol; and

the polyol is selected from polyethylene glycol, butanetriol, glycerol or 1,2,6-hexanetriol.

29. The composition according to claim 25 wherein the gelling agent is xanthan gum.