TRANSDERMAL DELIVERY SYSTEM FOR HORMONES AND STEROIDS

• US 20100279988A1
• Filed: 10/31/2008
• Published: 11/04/2010
• Est. Priority Date: 11/02/2007
• Status: Abandoned Application

• Current Assignee: Acrux DDS Pty Ltd (Acrux Limited)
• Original Assignee: Acrux DDS Pty Ltd (Acrux Limited)
• Inventors: Setiawan, Kerrie, Watkinson, Adam
• Application Number:
  US12/740,666
• Publication Number:
  US 20100279988A1
• Time in Patent Office: Days
• US Class Current: 514/170
• 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 31/205 Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine
• CPC Class Codes: A61K 31/56 Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
• CPC Class Codes: A61K 31/565 not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
• 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 31/57 substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
• CPC Class Codes: A61K 31/573 substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
• 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 47/14 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 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 9/12 Aerosols; Foams A61K9/0043, A61K9/0056, A61K9/006, A61K9/0073 take precedence; spray-films A61K9/7015
• CPC Class Codes: A61M 35/003 Portable hand-held applicators having means for dispensing or spreading integral media hand-held massage devices with liquid delivery A61H7/003
• CPC Class Codes: A61P 15/00 Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: A61P 15/10 for impotence
• CPC Class Codes: A61P 15/16 Masculine contraceptives
• CPC Class Codes: A61P 15/18 Feminine contraceptives
• CPC Class Codes: A61P 25/24 Antidepressants
• 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 5/00 Drugs for disorders of the endocrine system
• CPC Class Codes: A61P 5/24 : of the sex hormones
• CPC Class Codes: A61P 5/26 : Androgens
• CPC Class Codes: A61P 5/30 : Oestrogens
• CPC Class Codes: A61P 5/44 : Glucocorticosteroids; Drugs increasing or potentiating the activity of glucocorticosteroids

Abstract

A transdermal delivery system comprising a composition comprising a pharmacological agent and a penetration enhancer wherein the penetration enhancer comprises polyethylene glycol (PEG) of average molecular weight no more than 300.

Claims

1-18. -18. (canceled)

19. A transdermal delivery system comprising a composition comprising at least one pharmacological agent selected from hormones and steroids and a penetration enhancer wherein the penetration enhancer comprises a polyethylene glycol (PEG) of average molecular weight no more than 300.

20. A transdermal delivery system according to claim 19 wherein the PEG of average molecular weight of no more than 300 is present in an amount in the range of from 0.1 to 40% by weight of the total composition.

21. A transdermal delivery system according to claim 19 wherein the composition comprises a solvent selected from C₂ to C₄alkanol and mixtures thereof.

22. A transdermal delivery system according to claim 19 wherein the volatile solvent is present in the composition in an amount in the range of from 70% to 95%, by weight of the total composition.

23. A transdermal delivery system according to claim 19 wherein the composition consists essentially of:

(i) at least one pharmacological agent selected from hormones and steroids;

(ii) a penetration enhancer component consisting of a polyethylene glycol of average molecular weight no more than 300;

(iii) a volatile solvent consisting of one or more of ethanol and isopropanol; and

(iv) optionally a propellant.

24. A transdermal delivery system according to claim 19 wherein the total water content of the composition is less than 10% by weight of the total composition.

25. A transdermal delivery system according to claim 19 which is non-occlusive.

26. A transdermal delivery system according to claim 19 wherein the weight ratio of penetration enhancer to pharmacological agent is in the range of from 500:

1 to 1;

10.

27. A transdermal delivery system according to claim 19 wherein at least one pharmacological agent comprises one or more selected from the group consisting of steroidal hormones.

28. A transdermal delivery system according to claim 19 wherein at least one pharmacological agent comprises one or more steroids which provide eutrogenic, androgenic, glucocorticoid, adrenocortoid, anabolic or birth control activity.

29. A transdermal delivery system according to claim 28 wherein the pharmacological agent comprises one or more steroids selected from the group consisting of dexamethasone, dexamethasone acetate, dexamethasone sodium phosphate, cortisone, cortisone acetate, hydrocortisone, hydrocortisone acetate, hydrocortisone cypionate, hydrocortisone sodium phosphate, hydrocortisone sodium succinate, prednisone, prednisolone, prednisolone acetate, prednisolone sodium phosphate, prednisolone tebutate, prednisolone pivalate, triamcinolone, triamcinolone acetonide, triamcinolone hexacetonide, triamcinolone diacetate, methylprednisolone, methylprednisolone acetate, methylprednisolone sodium succinate, flunsolide, beclomethasone dipropionate, betamethasone sodium phosphate, betamethasone, vetamethasone disodium phosphate, vetamethasone sodium phosphate, betamethasone acetate, betamethasone disodium phosphate, chloroprednisone acetate, corticosterone, desoxycorticosterone, desoxycorticosterone acetate, desoxycorticosterone pivalate, desoximethasone, estradiol, fludrocortisone, fludrocortisone acetate, dichlorisone acetate, fluorohydrocortisone, fluorometholone, fluprednisolone, paramethasone, paramethasone acetate, androsterone, fluoxymesterone, aldosterone, methandrostenolone, methylandrostenediol, methyl testosterone, norethandrolone, testosterone, testosterone enanthate, testosterone propionate, equilenin, equilin, estradiol benzoate, estradiol dipropionate, estriol, estrone, estrone benzoate, acetoxypregnenolone, anagestone acetate, chlormadinone acetate, fluorogestone acetate, hydroxymethylprogesterone, hydroxymethylprogesterone acetate, hydroxyprogesterone, hydroxyprogesterone acetate, hydroxyprogesterone caproate, melengestrol acetate, normethisterone, pregnenolone, progesterone, ethynyl estradiol, mestranol, dimethisterone, ethisterone, ethynodiol diacetate, norethindrone, norethindrone acetate, norethisterone, fluocinolone acetonide, flurandrenolone, hydrocortisone sodium succinate, methylprednisolone sodium succinate, prednisolone phosphate sodium, triamcinolone acetonide, hydroxydione sodium, spironolactone, oxandrolone, oxymetholone, prometholone, testosterone cypionate, testosterone phenylacetate, estradiol cypionate, and norethynodrel and the salts and prodrugs thereof.

30. A transdermal delivery system according to claim 19 for female contraception comprising a comprising one or more estrogens and one or more progestins.

31. A transdermal delivery system according to claim 19 wherein the drug delivery system comprises on a weight basis from about 0.1 to about 10% of the steroid or hormone, from about 0.1 to 12% of the penetration enhancer and from about 70 to 99.8% ethanol, isopropanol or mixture thereof.

32. A method of transdermal administration of an pharmacological agent to a subject comprising application to dermal surface of the animal a transdermal system according to claim 19.

33. A method of transdermal administration according to claim 32 wherein the subject is in need of male hormone replacement in testosterone deficient hypogonadal men, female hormone replacement therapy for postmenopausal women, or androgen replacement therapy for females lacking libido or suffering depression using an androgen, male contraception or female contraception.

34. A transdermal delivery system according to claim 19 further comprising a spray apparatus comprising a container containing the transdermal composition, a spray nozzle and an actuator for delivering a metered dose of spray from the container via the spray nozzle.