METHOD AND COMPOSITION FOR TRANSDERMAL DRUG DELIVERY

• US 20100322884A1
• Filed: 06/25/2010
• Published: 12/23/2010
• Est. Priority Date: 06/03/2005
• Status: Active Grant

• Current Assignee: Acrux DDS Pty Ltd (Acrux Limited)
• Original Assignee: Acrux DDS Pty Ltd (Acrux Limited)
• Inventors: Humberstone, Andrew, Wilkins, Nina, Stone, Carolyn, DiPietro, Tony, Gonda, Igor, Robinson, Monique, Setiawan, Kerrie, Watkinson, Adam
• Granted Patent: US 8,993,520 B2
• Time in Patent Office: Days
• US Class Current: 424/68
• CPC Class Codes: A61K 31/568 substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
• 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 47/12 Carboxylic acids; Salts or anhydrides thereof
• CPC Class Codes: A61K 47/14 Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• 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 8/37 Esters of carboxylic acids
• 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: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: A61P 17/00 Drugs for dermatological disorders
• CPC Class Codes: A61P 5/24 of the sex hormones
• CPC Class Codes: A61P 5/26 Androgens
• CPC Class Codes: A61Q 17/04 Topical preparations for affording protection against sunlight or other radiation; Topical sun tanning preparations

Abstract

The invention is directed to a transdermal drug delivery composition which includes at least one physiologically active agent; and at least one volatile solvent; and at least one viscosity modulating agent. The invention extends to methods of administering such a composition to a subject and treatment of subjects using the composition.

Claims

1-20. -20. (canceled)

21. A method of increasing the androgen blood level of a person in need thereof comprising applying to at least one axilla of the person, without occlusion by a patch device, a non-occlusive transdermal drug delivery composition comprising:

(a) a pharmaceutically effective amount of at least one androgen;

(b) a solvent selected from the group consisting of lower alkyl alcohols;

(c) a penetration enhancer selected from the group consisting of fatty acids, fatty acid esters, fatty alcohols, glycols and glycol esters, 1,3-dioxolanes and 1,3-dioxanes, macrocyclic ketones containing at least 12 carbon atoms, oxazolidinones and oxazolidinone derivates, alkyl-2-(N,N-disubstituted amino)-alkanoate esters, (N,N-disubstituted amino)-alkanol alkanoates, sunscreen esters and mixtures thereof; and

(d) a viscosity modulating agent for increasing the viscosity of the composition.

22. A method according to claim 21 wherein the penetration enhancer is one or more selected from the group consisting of octyl dimethyl-para-aminobenzoate, octyl para-methyoxycinnamate and octyl salicylate.

23. A method according to claim 21 wherein the penetration enhancer is octyl salicylate.

24. A method according to claim 21 wherein the androgen comprises at least one selected from the group consisting of testosterone;

pharmaceutically acceptable salts of testosterone;

alpha-reductase inhibitors;

methyltestosterone, clostebol acetate, drostanolone, furazabol, nandrolone oxandrolone, stanozolol, trenbolone acetate, dihydro-testosterone, 17-.alpha.-methyl-19-nortestosterone and fluoxymesterone.

25. A method according to claim 21 wherein the androgen is selected from testosterone and pharmaceutically acceptable salts thereof.

26. A method according to claim 25 wherein the androgen comprises at least one selected from the group consisting of testosterone and salts of testosterone selected from the group consisting of the acetate, enanthate, cypionate, isobutyrate, dehydro-epiandrosterone, propionate, undecanoate esters and cyproterone acetate salts.

27. A method according to claim 21 wherein the penetration enhancer is present in an amount of from 0.01% to 15% by volume based on the total volume of the composition and the solvent selected from lower alkyl alcohols is present in an amount of from 60% to 99% by volume based on the total volume of the composition.

28. A method according to claim 27 wherein the solvent is selected from the group consisting of ethanol, isopropanol, and mixtures thereof.

29. A method according to claim 28 wherein the solvent is present in an amount of at least 80% by volume based on the total volume of the composition.

30. A method according to claim 21 wherein the composition is applied to a male person in an amount effective to provide a testosterone level in the systemic circulation equivalent to from 300 to 1000 ng testosterone per dL serum.

31. A method according to claim 21 wherein the viscosity modulating agent increases the viscosity of the composition to within the range of from greater than the viscosity of water to 300 cps.

32. A method according to claim 21 wherein the viscosity modulating agent is polyvinyl pyrrolidone and is present in an amount of from 1% by weight to 3% by weight of the total composition.

33. A method according to claim 21 wherein the composition further comprises an antiperspirant and/or deodorant agent.

34. A method according to claim 31 wherein the composition comprises an antiperspirant selected from the group consisting of aluminium bromohydrate, aluminium chloride, aluminium citrate, aluminium sulfate, ammonium alum, cobalt acetylmethionate, potassium alum, sodium alum and sodium aluminium chlorohydroxy lactate.

35. A method according to claim 21 wherein the composition is applied as a gel or roll-on.

36. A method according to claim 21 wherein the composition is applied once a day.