Transdermal delivery system for hormones and steroids

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.

1 - 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 C 2  to C 4 alkanol 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.