Sensation modifying topical composition foam

Abstract

This invention relates to foamable compositions that are capable of producing a sensation or sensation modifying effect upon application on a body surface. More particularly the invention relates to foamable pharmaceutical, therapeutic and cosmetic compositions, comprising an active agent, having a sensation or sensation modifying affect on a body surface, upon application. More particularly, the invention relates to foamable compositions comprising: (a) a foamable carrier; (b) at least one sensation or sensation modifying agent, selected from the group of a cooling agent; a warming agent; a relaxing or soothing agent; stimulating or refreshing agent; or mixtures thereof and (c) a propellant at a concentration of about 3% to about 45% by weight of the total composition. The foamable carrier can be an emollient emulsion foamable vehicle, a foamable gel vehicle and can also be a substantially non aqueous foamable vehicle.

1 . A composition for providing a subject with at least one sensation at a delivery site for a sustained period of time, the composition comprising:
 a. at least one sensation or sensation modifying agent, selected from the group consisting of
 i. a cooling agent; 
 ii. a warming agent; 
 iii. a relaxing or soothing agent; and 
 iv. a stimulating or refreshing agent; 
   or mixtures thereof;   b. a foamable carrier resistant to aging suitable for delivery of at least one sensation or sensation modifying agent; and   c. a propellant at a concentration of about 3% to about 45% by weight of the total composition,   wherein the composition is stored in an aerosol container and upon release expands to form a non-crackling short term stable foam; and   wherein upon contact with a surface at the delivery site the prolonged sensation is not primarily due to the propellant or an exothermic reaction.   
     
     
         2 . A composition according to  claim 1 , wherein the composition does not effect a substantial temperature change to the surface. 
     
     
         3 . A composition according to  claim 1 , wherein the cooling agent is selected from menthol; an isomer of menthol, a menthol derivative; 4-Methyl-3-(1-pyrrolidinyl)-2[5H]-furanone; WS-23, Icilin, Icilin Unilever Analog, 5-methyl-4-(1-pyrrolidinyl)-3-[2H]-furanone; 4,5-dimethyl-3-(1-pyrrolidinyl)-2[5H]-furanone; isopulegol, 3-(I-menthoxy)propane-1,2-diol, 3-(I-menthoxy)-2-methylpropane-1,2-diol, p-menthane-2,3-diol, p-menthane-3,8-diol, 6-isopropyl-9-methyl-1,4-dioxas-piro[4,5]decane-2-methanol, menthyl succinate and its alkaline earth metal salts, trimethylcyclohexanol, N-ethyl-2-isopropyl-5-methylcyclohexanecarb-oxamide, Japanese mint ( Mentha arvensis ) oil, peppermint oil, menthone, menthone glycerol ketal, menthyl lactate, 3-(I-menthoxy)ethan-1-ol, 3-(I-menthoxy)propan-1-ol, 3-(I-menthoxy)butan-1-ol, I-menthylacetic acid N-ethylamide, I-menthyl-4-hydroxypentanoate, I-menthyl-3-hydroxybutyrate, N,2,3-trimethyl-2-(1-methylethyl)-butanamide and spearmint oil. 
     
     
         4 . A composition according to  claim 1 , wherein the menthol derivative is selected from the group consisting of: menthol ethylene glycol carbonate, which is now known as Frescolat® type MGC, menthol Propylene Glycol Carbonate (Frescolat® type MPC), menthyl lactate (Frescolat ML®) and Menthone Glycerin Acetal (Frescolat MGA®) and 3-(I-Menthoxy)-1,2-propanediol. 
     
     
         5 . A composition according to  claim 1 , wherein the warming agent is selected from polyhydric alcohols, capsaicin,  capsicum  powder, a  capsicum tincture, capsicum  extract, capsaicin, hamamalis, homocapsaicin, homodihydrocapsaicin, nonanoyl vanillyl amide, nonanoic acid vanillyl ether, vanillyl alcohol alkyl ether derivatives, such as vanillyl ethyl ether, vanillyl butyl ether, vanillyl pentyl ether, and vanillyl hexyl ether, isovanillyl alcohol alkyl ethers, ethylvanillyl alcohol alkyl ethers, veratryl alcohol derivatives, substituted benzyl alcohol derivatives, substituted benzyl alcohol alkyl ethers, vanillin propylene glycol acetal, ethylvanillin propylene glycol acetal, ginger extract, ginger oil, gingeol and gingeron. 
     
     
         6 . A composition according to  claim 1 , wherein the relaxing or soothing agent is selected from a herb extracts, selected from the group consisting of aloe vera, alpha bisabolol, D-panthenol, allantoin, hamamelis, chamomile, yarrow;  calendula , comfrey, witch hazel and other astringents, sea weed, and oat extracts; oils, selected from the group consisting of: almond oil, avocado oil, and comfrey; and essential oils, selected from the group consisting of: cardamone, eucalyptus,  mentha piperita  (peppermint), hyssop, and rosemary; waxy or unctuous substances selected from the group consisting of: lanolin or vaselline jelly, minerals, selected from the group consisting of: zinc oxide, calamine and selenium; vitamins, selected from the group consisting of: tocopheryl acetate (vitamin E), and pharmaceutical agents selected from the group consisting of: analgesics, anesthetics, anti-inflammatory agents, and anti-histamines, and muscle relaxants; menthol, camphor, eugenol, eucalyptol, safrol, methyl salicylate, menthyl lactate, menthyl ethoxyacetate, menthone glycerinacetal, 3-I-menthoxypropane-1,2-diol, ethyl 1-menthyl carbonate, (1S,3S,4R)-p-menth-8-en-3-ol, menthyl pyrrolidone carboxylate, N-substituted-p-menthane-3-carboxamides hamamelis extract and ginger oil. 
     
     
         7 . A composition according to  claim 1 , wherein the stimulating or refreshing agent is selected from an alcohol, L-menthol, camphor, menthe oil,  capsicum  extract, capsaicin, benzyl nicotinate, salicylate, glycol salicylate, acetyl choline, serotonin, histamine, a prostaglandin, a neurotransmitter; a CNS stimulant, caffeine and quinine. 
     
     
         8 . A composition according to  claim 1 , wherein the short term stable foam is stable at the delivery site for at least one minute. 
     
     
         9 . A composition according to  claim 8 , wherein the short term stable foam is stable at the delivery site for at least five minutes. 
     
     
         10 . A composition according to  claim 1 , wherein the sustained period of time is at least 15 minutes. 
     
     
         11 . A composition according to  claim 10 , wherein the sustained period of time is at least 30 minutes. 
     
     
         12 . A composition according to  claim 11 , wherein the sustained period of time is at least one hour. 
     
     
         13 . A composition according to  claim 1 , wherein said foamable carrier is at a concentration of about 40% to about 99% by weight of the total composition excluding propellant and is selected from the group consisting of an aqueous emulsion, and aqueous gel and a non aqueous carrier;
 wherein the carrier comprises:   i. at least one surface active agent at a concentration of about 0.1% to about 10% by weight of the carrier;   ii. at least one polymeric agent at a concentration of about 0.1% to about 5% by weight of the total composition; and   iii. at least one non aqueous solvent.   
     
     
         14 . A composition according to  claim 13 , wherein said non aqueous solvent is in the case of the aqueous emulsion, a hydrophobic emollient; in the case of the aqueous gel, a penetration enhancer; and in the case of the non aqueous carrier, a polyol. 
     
     
         15 . A composition according to  claim 14 , wherein the at least one emollient is selected from the group consisting of: avocado oil, isopropyl myristate, mineral oil; capric triglyceride, caprylic triglyceride, isopropyl palmitate, isopropyl isostearate, diisopropyl adipate, diisopropyl dimerate, maleated soybean oil, octyl palmitate, cetyl lactate, cetyl ricinoleate, tocopheryl acetate, acetylated lanolin alcohol, cetyl acetate, phenyl trimethicone, glyceryl oleate, tocopheryl linoleate, wheat germ glycerides, arachidyl propionate, myristyl lactate, decyl oleate, ricinoleate, isopropyl lanolate, pentaerythrityl tetrastearate, neopentylglycol dicaprylate/dicaprate, isononyl isononanoate, isotridecyl isononanoate, myristyl myristate, triisocetyl citrate, octyl dodecanol, unsaturated or polyunsaturated oils, such as olive oil, corn oil, soybean oil, canola oil, cottonseed oil, coconut oil, sesame oil, sunflower oil, borage seed oil, syzigium aromaticum oil, hempseed oil, herring oil, cod-liver oil, salmon oil, flaxseed oil, wheat germ oil, evening primrose oils; essential oils; and silicone oils, such as dimethicone, cyclomethicone, polyalkyl siloxane, polyaryl siloxane, polyalkylaryl siloxane, a polyether siloxane copolymer and a poly(dimethylsiloxane)-(diphenyl-siloxane). 
     
     
         16 . A composition according to  claim 13 , wherein the at least one stabilizing surface active agent is selected from the group consisting of: stearlyl alcohol; steareth-2, steareth-21; polysorbate 80, PEG-40 stearate, glyceryl monostearate, cetostearyl alcohol, laureth 4, and Ceteareth-20, or is a combination of at least two surfactants selected from the group consisting of combinations of polyoxyethylene alkyl ethers, particularly Brij 59/Brij10; Brij 52/Brij 10; Steareth 2/Steareth 20; Steareth 2/Steareth 21 (Brij 72/BRIJ 721); Myrj 52/Myrj 59; combinations of sucrose esters, particularly Surphope 1816/Surphope 1807; combinations of sorbitan esters, particularly Span 20/Span 80; Span 20/Span 60; combinations of sucrose esters and sorbitan esters, particularly Surphope 1811 and Span 60; combinations of liquid polysorbate detergents and PEG compounds, particularly Twin 80/PEG-40 stearate/methyl glucaso sequistearate. 
     
     
         17 . A composition according to  claim 13 , wherein the at least one polymeric agent is selected from the group consisting of: locust bean gum, sodium alginate, sodium caseinate, egg albumin, gelatin agar, carrageenin gum, sodium alginate, xanthan gum, quince seed extract, tragacanth gum, guar gum, cationic guars, hydroxypropyl guar gum, starch, an amine-bearing polymer, chitosan, alginic acid, hyaluronic acid, a chemically modified starch, a carboxyvinyl polymer, polyvinylpyrrolidone, polyvinyl alcohol, a polyacrylic acid polymer, a polymethacrylic acid polymer, polyvinyl acetate, a polyvinyl chloride polymer, a polyvinylidene chloride polymer, methylcellulose, hypromellose, hydroxypropyl cellulose, hydroxypropyl methylcellulose, hydroxyethyl cellulose, hydroxy propylmethyl cellulose, methylhydroxyethylcellulose, methyl hydroxypropylcellulose, hydroxyethylcarboxymethylcellulose, carboxymethyl cellulose, carboxymethylcellulose carboxymethylhydroxyethylcellulose, a cationic cellulose, methocel K100M, PEG 1000, PEG 4000, PEG 6000 and PEG 8000 xanthan gum; sodium carboxymethyl-cellulose, hydroxypropyl-cellulose, microcrystalline-cellulose, Avicel RC581, aluminum starch octyl succinate and a polyacrylate. 
     
     
         18 . A composition according to  claim 13 , wherein said foamable carrier further comprises one or more of the following:
 i. a co-emulsifier or foam stabilizer at a concentration of about 0.1% to about 5% by weight of the total composition;   ii. a wax, viscosity, bulking or firming agent at a concentration of about 0.1% to about 15% by weight of the total composition;   iii. a co-solvent at a concentration of about 0.1% to about 20% by weight of the total composition;   iv. a penetration enhancer or potent solvent at a concentration of about 0.1% to about 25% by weight of the total composition;   v. a foam adjuvant agent, selected from the group consisting of a fatty alcohol having 15 or more carbons in their carbon chain; a fatty acid having 16 or more carbons in their carbon chain at a concentration of about 0.1% to about 25% by weight of the total composition;   vi. a stabilizer at a concentration of about 5% to about 30% by weight of the total composition; and   vii. an agent capable of having an occlusive effect at a concentration of about 5% to about 30% by weight of the total composition.   
     
     
         19 . The composition of  claim 1 , wherein the propellant is a cooling agent. 
     
     
         20 . The composition of  claim 1 , further comprising at least one additional active agent. 
     
     
         21 . The composition of  claim 20 , wherein the at least one additional active agent comprises a cosmetic active agent or a pharmaceutical active agent having a cosmetic or pharmaceutical effect other than a sensation or sensation modifying effect. 
     
     
         22 . The composition of  claim 21 , wherein the at least one additional active agent is selected from the group consisting of active herbal extracts, acaricides, age spot and keratose removing agents, allergen, analgesics, local anesthetics, antiacne agents, antiallergic agents, antiaging agents, antibacterials, antibiotics, antiburn agents, anticancer agents, antidandruff agents, antidepressants, antidermatitis agents, antiedemics, antihistamines, antihelminths, antihyperkeratolyte agents, antiinflammatory agents, antiirritants, antilipemics, antimicrobials, antimycotics, antiproliferative agents, antioxidants, anti-wrinkle agents, antipruritics, antipsoriatic agents, antirosacea agents antiseborrheic agents, antiseptic, antiswelling agents, antiviral agents, anti-yeast agents, astringents, topical cardiovascular agents, chemotherapeutic agents, cal tar, corticosteroids, dicarboxylic acids, disinfectants, fungicides, hair growth regulators, hormones, hydroxy acids, immunosuppressants, immunoregulating agents, insecticides, insect repellents, keratolytic agents, lactams, metals, metal oxides, mitocides, neuropeptides, non-steroidal anti-inflammatory agents, oxidizing agents, pediculicides, photodynamic therapy agents, retinoids, sanatives, scabicides, self tanning agents, skin whitening agents, vasoconstrictors, vasodilators, vitamins, vitamin derivatives, vitamin A and derivatives, vitamin D and derivatives, wound healing agents and wart removers. 
     
     
         23 . The composition of  claim 1 , wherein the foamable carrier comprises at least one carrier medium, selected from the group consisting of water, an oil, a silicone oil, an alcohol, a polyol, a polyethylene glycol (PEG), a propylene glycol, and a solvent or combinations thereof. 
     
     
         24 . The composition of  claim 1 , wherein the foamable carrier further comprises a polar solvent. 
     
     
         25 . The composition of  claim 1 , further comprising an additional component selected from the group consisting of an anti-perspirant, an anti-static agent, a buffering agent, a bulking agent, a chelating agent, a colorant, a conditioner, a deodorant, a diluent, a dye, an emollient, fragrance, a humectant, moisturizer, an occlusive agent, a penetration enhancer, a perfuming agent, a permeation enhancer, a pH-adjusting agent, a preservative, a skin penetration enhancer, a sunscreen, a sun blocking agent, a sunless tanning agent, and a vitamin. 
     
     
         26 . The composition of  claim 1 , wherein the sensation or sensation modifying is selected from the group consisting of:
 a. a combination of a cooling and a warming agent;   b. a combination of a cooling and a soothing or relaxing agent;   c. a combination of a cooling and a stimulating or refreshing agent;   d. a combination of a warming and a stimulating or refreshing agent;   e. a combination of a warming and a soothing or relaxing agent;   f. a combination of a cooling; a warming and a soothing or relaxing agent; and   g. a combination of a cooling; a warming and stimulating or refreshing agent.   
     
     
         27 . The composition of  claim 1 , wherein the propellant provides an initial cooling sensation combined with a sensation agent to provide a prolonged sensation. 
     
     
         28 . The composition of  claim 1 , wherein the foamable carrier further contains a foam adjuvant agent, selected from the group consisting of a fatty alcohol having 15 or more carbons in their carbon chain; a fatty acid having 16 or more carbons in their carbon chain. 
     
     
         29 . The composition of  claim 21 , wherein:
 a. the at least one sensation or sensation modifying agent comprises menthol in a concentration of 0.5 to about 3% by weight;   b. the at least one active agent comprises:
 i. coal tar extract in a concentration of around 2% up to around 20% by weight; and 
 ii. at least one other active agent selected from salicylic acid and hydrocortisone in a concentration of around 0.5% up to around 10% by weight; and 
   c. the menthol is adapted to provide an improved sensation by ameliorating a negative sensation effect of said coal tar extract.   
     
     
         30 . The composition of  claim 21 , wherein the carrier is an emulsion and:
 a. the at least one sensation or sensation modifying agent comprises menthol crystals in a concentration of 0.5 to about 3% by weight;   b. the at least one active agent comprises:
 i. coal tar in a concentration of around 2% up to around 20% by weight; and 
 ii. hydrocortisone butyrate in a concentration of around 0.5% up to around 10% by weight; and 
   c. the menthol crystals are adapted to provide an improved sensation by ameliorating a negative sensation effect of said coal tar; and   wherein the composition does not effect a substantial temperature change to the surface.   
     
     
         31 . A method for providing a subject with at least one sensation at a delivery site, the method comprising administering to the delivery site of the subject a composition comprising:
 a. at least one sensation or sensation modifying agent, selected from the group of
 i. a cooling agent; 
 ii. a warming agent; 
 iii. a relaxing or soothing agent; and 
 iv. a stimulating or refreshing agent; 
   or mixtures thereof;   b. a foamable carrier resistant to aging suitable for delivery of at least one sensation or sensation modifying agent; and   c. a propellant at a concentration of about 3% to about 45% by weight of the total composition,   wherein the composition is stored in an aerosol container and upon release expands to form a non-crackling short term stable foam; and   wherein upon contact with a surface at the delivery site the prolonged sensation is not primarily due to the propellant or an exothermic reaction, so as to provide the subject with the at least one sensation for the sustained period of time.   
     
     
         32 . A method according to  claim 31 , wherein foam is stable at the delivery site for at least one minute. 
     
     
         33 . A method according to  claim 32 , wherein foam is stable at the delivery site for at least five minutes. 
     
     
         34 . A method according to  claim 33 , wherein the subject senses the at least one sensation at the delivery site for at least at least 15 minutes. 
     
     
         35 . A method according to  claim 34 , wherein the subject senses the at least one sensation at the delivery site for at least 30 minutes. 
     
     
         36 . A method according to  claim 35 , wherein the subject senses the at least one sensation at the delivery site for at least one hour. 
     
     
         37 . A method according to  claim 31 , wherein the subject senses the at least one sensation as increasing, peaking and decreasing over said sustained period of time. 
     
     
         38 . A method according to  claim 31 , wherein the subject senses at least one sensation at the delivery site selected from a cooling sensation, a warming sensation, a heating sensation, a soothing sensation, a relaxing sensation, a stimulating sensation and a refreshing sensation. 
     
     
         39 . A method according to  claim 31 , wherein said administration step further comprises spreading said foam over a surface at the delivery site. 
     
     
         40 . The method of  claim 31 , wherein the delivery site is selected from the group consisting of the skin, a body cavity, a mucosal surface, the nose, the mouth, the eye, the ear canal, the respiratory system, the vagina and the rectum. 
     
     
         41 . The method of  claim 31 , wherein the composition further comprises at least one additional active agent. 
     
     
         42 . The method of  claim 41 , wherein the at least one additional active agent comprises a cosmetic active agent or a pharmaceutical active agent having a cosmetic or pharmaceutical effect other than a sensation or sensation modifying effect. 
     
     
         43 . The method of  claim 41 , wherein the at least one additional active agent is selected from the group consisting of active herbal extracts, acaricides, age spot and keratose removing agents, allergen, analgesics, local anesthetics, antiacne agents, antiallergic agents, antiaging agents, antibacterials, antibiotics, antiburn agents, anticancer agents, antidandruff agents, antidepressants, antidermatitis agents, antiedemics, antihistamines, antihelminths, antihyperkeratolyte agents, antiinflammatory agents, antiirritants, antilipemics, antimicrobials, antimycotics, antiproliferative agents, antioxidants, anti-wrinkle agents, antipruritics, antipsoriatic agents, antirosacea agents antiseborrheic agents, antiseptic, antiswelling agents, antiviral agents, anti-yeast agents, astringents, topical cardiovascular agents, chemotherapeutic agents, cal tar, corticosteroids, dicarboxylic acids, disinfectants, fungicides, hair growth regulators, hormones, hydroxy acids, immunosuppressants, immunoregulating agents, insecticides, insect repellents, keratolytic agents, lactams, metals, metal oxides, mitocides, neuropeptides, non-steroidal anti-inflammatory agents, oxidizing agents, pediculicides, photodynamic therapy agents, retinoids, sanatives, scabicides, self tanning agents, skin whitening agents, vasoconstrictors, vasodilators, vitamins, vitamin derivatives, vitamin A and derivatives, vitamin D and derivatives, wound healing agents and wart removers. 
     
     
         44 . The method of  claim 43 , further comprising treating a disorder selected from the group consisting of dermatological pain, dermatological inflammation, acne, acne vulgaris, inflammatory acne, non-inflammatory acne, acne fulminans, nodular papulopustular acne, acne conglobata, dermatitis, bacterial skin infections, fungal skin infections, viral skin infections, parasitic skin infections, skin neoplasia, skin neoplasms, pruritis, cellulitis, acute lymphangitis, lymphadenitis, erysipelas, cutaneous abscesses, necrotizing subcutaneous infections, scalded skin syndrome, folliculitis, furuncles, hidradenitis suppurativa, carbuncles, paronychial infections, rashes, erythrasma, impetigo, eethyma, yeast skin infections, warts, molluscum contagiosum, trauma or injury to the skin, post-operative or post-surgical skin conditions, scabies, pediculosis, creeping eruption, eczemas, psoriasis, pityriasis rosea, lichen planus, pityriasis rubra pilaris, edematous, erythema multiforme, erythema nodosum, grannuloma annulare, epidermal necrolysis, sunburn, photosensitivity, pemphigus, bullous pemphigoid, dermatitis herpetiformis, keratosis pilaris, callouses, corns, ichthyosis, skin ulcers, ischemic necrosis, miliaria, hyperhidrosis, moles, Kaposi's sarcoma, melanoma, malignant melanoma, basal cell carcinoma, squamous cell carcinoma, poison ivy, poison oak, contact dermatitis, atopic dermatitis, rosacea, purpura, moniliasis, candidiasis, baldness, alopecia, Behcet's syndrome, cholesteatoma, Dercum disease, ectodermal dysplasia, gustatory sweating, nail patella syndrome, lupus, hives, hair loss, Hailey-Hailey disease, chemical or thermal skin burns, scleroderma, aging skin, wrinkles, sun spots, necrotizing fasciitis, necrotizing myositis, gangrene, scarring, and vitiligo, chlamydia infection, gonorrhea infection, hepatitis B, herpes, HIV/AIDS, human papillomavirus (HPV), genital warts, bacterial vaginosis, candidiasis, chancroid, granuloma Inguinale, lymphogranloma venereum, mucopurulent cervicitis (MPC), molluscum contagiosum, nongonococcal urethritis (NGU), trichomoniasis, vulvar disorders, vulvodynia, vulvar pain, yeast infection, vulvar dystrophy, vulvar intraepithelial neoplasia (VIN), contact dermatitis, pelvic inflammation, endometritis, salpingitis, oophoritis, genital cancer, cancer of the cervix, cancer of the vulva, cancer of the vagina, vaginal dryness, dyspareunia, anal and rectal disease, anal abscess/fistula, anal cancer, anal fissure, anal warts, Crohn's disease, hemorrhoids, anal itch, pruritus ani, fecal incontinence, constipation, polyps of the colon and rectum; and wherein the at least one active agent is suitable for treating said disorder.