Surfactant-free, water-free formable composition and breakable foams and their uses

• US 10,029,013 B2
• Filed: 10/01/2010
• Issued: 07/24/2018
• Est. Priority Date: 10/02/2009
• Status: Active Grant

• Current Assignee: Journey Medical Corp. (Fortress Biotech, Inc.)
• Original Assignee: Foamix Pharmaceuticals, Ltd. (VYNE Therapeutics, Inc.)
• Inventors: Tamarkin, Dov, Gazal, Elana, Papiashvili, Irakliy, Hazot, Yohan, Schuz, David, Keynan, Rita
• Primary Examiner(s): Duffy, Patricia
• Assistant Examiner(s): Gotfredson, Garen
• Application Number:
  US13/499,709
• Publication Number:
  US 20130011342A1
• Time in Patent Office: 2,853 Days
• Field of Search: None
• CPC Class Codes: A61K 2800/31 Anhydrous
• CPC Class Codes: A61K 2800/33 Free of surfactant
• CPC Class Codes: A61K 31/137 Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
• 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 31/4164 1,3-Diazoles
• 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 31/593 9,10-Secocholestane derivatives, e.g. cholecalciferol, i.e. vitamin D3
• CPC Class Codes: A61K 31/65 Tetracyclines
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61K 47/02 Inorganic compounds
• CPC Class Codes: A61K 47/06 Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
• 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 47/24 containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
• CPC Class Codes: A61K 47/44 Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin synthetic glycerides, e.g. medium-chain triglycerides, A61K47/14
• CPC Class Codes: A61K 8/31 Hydrocarbons
• CPC Class Codes: A61K 8/342 Alcohols having more than seven atoms in an unbroken chain
• CPC Class Codes: A61K 8/361 Carboxylic acids having more than seven carbon atoms in an unbroken chain; Salts or anhydrides thereof
• 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 9/0048 : Eye, e.g. artificial tears
• 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: A61K 9/122 : Foams; Dry foams edible foams A61K9/0056
• CPC Class Codes: A61K 9/124 : characterised by the propellant
• CPC Class Codes: A61P 1/00 : Drugs for disorders of the alimentary tract or the digestive system
• CPC Class Codes: A61P 11/00 : Drugs for disorders of the respiratory system
• CPC Class Codes: A61P 15/00 : Drugs for genital or sexual disorders for disorders of sex hormones A61P5/24; Contraceptives
• CPC Class Codes: A61P 15/02 : for disorders of the vagina
• 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 17/04 : Antipruritics
• CPC Class Codes: A61P 17/06 : Antipsoriatics
• CPC Class Codes: A61P 17/08 : Antiseborrheics
• CPC Class Codes: A61P 17/10 : Anti-acne agents
• CPC Class Codes: A61P 17/12 : Keratolytics, e.g. wart or anti-corn preparations
• CPC Class Codes: A61P 17/14 : for baldness or alopecia
• CPC Class Codes: A61P 17/16 : Emollients or protectives, e.g. against radiation
• CPC Class Codes: A61P 19/02 : for joint disorders, e.g. arthritis, arthrosis
• CPC Class Codes: A61P 23/00 : Anaesthetics
• CPC Class Codes: A61P 25/00 : Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/20 : Hypnotics; Sedatives
• CPC Class Codes: A61P 25/24 : Antidepressants
• CPC Class Codes: A61P 27/02 : Ophthalmic agents
• CPC Class Codes: A61P 27/06 : Antiglaucoma agents or miotics
• 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 31/00 : Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
• CPC Class Codes: A61P 31/04 : Antibacterial agents
• CPC Class Codes: A61P 31/10 : Antimycotics
• CPC Class Codes: A61P 31/12 : Antivirals
• CPC Class Codes: A61P 31/14 : for RNA viruses
• CPC Class Codes: A61P 31/18 : for HIV
• CPC Class Codes: A61P 31/20 : for DNA viruses
• CPC Class Codes: A61P 31/22 : for herpes viruses
• CPC Class Codes: A61P 33/00 : Antiparasitic agents
• CPC Class Codes: A61P 33/10 : Anthelmintics
• CPC Class Codes: A61P 33/14 : Ectoparasiticides, e.g. scabicides
• CPC Class Codes: A61P 35/00 : Antineoplastic agents
• CPC Class Codes: A61P 37/00 : Drugs for immunological or allergic disorders
• CPC Class Codes: A61P 37/02 : Immunomodulators
• CPC Class Codes: A61P 37/04 : Immunostimulants
• CPC Class Codes: A61P 37/06 : Immunosuppressants, e.g. drugs for graft rejection
• CPC Class Codes: A61P 37/08 : Antiallergic agents antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14
• CPC Class Codes: A61P 39/06 : Free radical scavengers or antioxidants
• CPC Class Codes: A61P 5/00 : Drugs for disorders of the endocrine system
• CPC Class Codes: A61P 7/10 : Antioedematous agents; Diuretics
• CPC Class Codes: A61P 9/00 : Drugs for disorders of the cardiovascular system
• CPC Class Codes: A61P 9/08 : Vasodilators for multiple indications
• CPC Class Codes: A61Q 17/04 : Topical preparations for affording protection against sunlight or other radiation; Topical sun tanning preparations
• CPC Class Codes: A61Q 19/00 : Preparations for care of the skin
• CPC Class Codes: A61Q 19/10 : Washing or bathing preparations

Abstract

A substantially surface active agent-free and foam adjuvant-free composition which includes a hydrophobic solvent, a wax and a propellant. A substantially surface active agent-free and foam adjuvant-free composition, further comprising, a tetracycline antibiotic, or one or More other active agents. A method of treatment, using a substantially surface active agent-free and substantially foam adjuvant-free composition.

Claims

1. A waterless foamable composition free of surfactant and polymeric agent comprising:

a carrier comprising;

a) about 50% to about 90% by weight of the carrier of a liquid oil and about 10% to about 50% by weight of the carrier of a paraffin wax that has a melting point between about 47°

C. and about 64°

C., wherein the total weight of the liquid oil and paraffin wax together is between about 85% and about 100% by weight of the carrier;

or

b) about 40% by weight of the carrier of a liquid oil and about 60% by weight of the carrier of a paraffin wax that has a melting point between about 42°

C. and about 44°

C.; and

a liquefied or compressed gas propellant; and

a tetracycline antibiotic;

wherein the ratio of the carrier to the propellant is from about 100;

4 to about 100;

25;

wherein the composition comprises less than 5% foam adjuvant; and

wherein upon dispensing the foamable composition from a container, the composition forms a breakable foam that is stable, yet breaks easily upon application of shear force.

2. The composition of claim 1, further comprising at least one active agent.

3. The composition of claim 2, wherein the active agent is selected from the group consisting of an active herbal extract, an acaricide, an age spot and keratose removing agent, an allergen, an alpha hydroxyl acid, an analgesic agent, an antiacne agent, an antiallergic agent, an antiaging agent, an antibacterial agent, an antibiotic, an antiburn agent, an anticancer agent, an antidandruff agent, an antidepressant, an antidermatitis agent, an antiedemic agent, an antifungal agent, an antihistamine, an antihelminth agent, an antihyperkeratolyte agent, an anti-infective agent, an antiinflammatory agent, an antiirritant, an antilipemic agent, an antimicrobial agent, an antimycotic agent, an antioxidant, an antiparasitic agent, an antiproliferative agent, an antipruritic agent, an antipsoriatic agent, an antirosacea agent, an antiseborrheic agent, an antiseptic agent, an antiswelling agent, an antiviral agent, an anti-wart agent, an anti-wrinkle agent, an antiyeast agent, an astringent, a beta-hydroxy acid, benzoyl peroxide, a topical cardiovascular agent, a chemotherapeutic agent, a corticosteroid, an immunogenic substance, a dicarboxylic acid, a disinfectant, a fungicide, a hair growth regulator, a haptene, a hormone, a hydroxy acid, an immunosuppressant, an immunoregulating agent, an immunomodulator, an insecticide, an insect repellent, a keratolytic agent, a lactam, a local anesthetic agent, a lubricating agent, a masking agent, a metals, a metal oxide, a mitocide, a neuropeptide, a non-steroidal anti-inflammatory agent, an oxidizing agent, a pediculicide, a peptide, a protein, a photodynamic therapy agent, a radical scavenger, a refatting agent, a retinoid, a sanative, a scabicide, a self tanning agent, a skin protective agent, a skin whitening agent, a steroid, a steroid hormone, a vasoconstrictor, a vasodilator, a vitamin, a vitamin A, a vitamin A derivative, a vitamin B, a vitamin B derivative, a vitamin C, a vitamin C derivative, a vitamin D, a vitamin D derivative, a vitamin D analog, a vitamin F, a vitamin F derivative, a vitamin K, a vitamin K derivative, a wound healing agent and a wart remover, an androgen, an anti-hyperkeratosis agent, an estrogen, an immunestimulant, a pesticide, a progesterone, a sedative, a vaso active agent, and a mixture of any two or more thereof.

4. The composition of claim 1, wherein the tetracycline antibiotic is a minocycline or a doxycycline.

5. The composition of claim 3, wherein the active agent is a retinoid.

6. The composition of claim 1, wherein the carrier comprises about 1% or less than 1% by weight of a foam adjuvant.

7. The composition of claim 1, wherein the composition is foam adjuvant free.

8. The composition of claim 1, wherein the carrier comprises about 5% or less than 5% by weight of the carrier of polyols.

9. The composition of claim 1, wherein the paraffin wax is selected from the group consisting of a paraffin wax 58-62°

C., a paraffin wax 51-53°

C., and a paraffin wax 42-44°

C., and a mixture thereof.

10. The composition of claim 1, wherein the composition is free of short chain alcohols.

11. The composition of claim 1, wherein the composition is a single phase.

12. The composition of claim 1, further comprising a solid or semi-solid oil.

13. The composition of claim 1, wherein the composition is short chain alcohol free and polyol free.

14. The composition of claim 1, wherein the propellant is a hydrocarbon propellant or a hydrofluorocarbon or another environmentally acceptable propellant.

15. The composition of claim 1, wherein the composition further comprises a wax selected from a hydrogenated castor oil, beeswax, and a mixture thereof.

16. The composition of claim 2, wherein the active agent is suitable for treating a disorder selected form the group consisting of abscess, acne, acne conglobata, acne fulminans, acne vulgaris, acne scars, acute febrile neutrophilic dermatosis, acute lymphangitis, allergic contact dermatitis, alopecia, athlete'"'"'s foot, atopic dermatitis, bacterial skin infections, baldness, basal cell carcinoma, blisters, bromhidrosis, bullous pemphigoid, burn, calluses candidiasis, carbuncles, cellulitis, chemical burns, chicken pox, cholesteatoma, cholinergic urticaria, chronic effects of sunlight, cold sores, cold urticaria, comedones, corns, creeping eruption, cutaneous abscess, cutaneous larva migrans, cutaneous myiasis, dark spots, delusional parasitosis, Dercum disease, dermatitis, dermatitis herpetiformis, dermatological pain, dermatological inflammation, dermographism, dermatophytoses, drug eruptions and reactions, dyshidrotic eczema, ectodermal dysplasia, eczema, ecthyma, epidermoid cyst, epidermal necrolysis, erysipelas, erysipelas, erythrasma, exfoliative dermatitis, erythema multiforme, erythema nodosum, folliculitis, fungal nail infections, fungal skin infections, furuncles, gangrene, genital herpes, granuloma annulare, head lice, hidradenitis suppurativa, hives, folliculitis, hirsutism, hyperhidrosis, hypohidrosis, ichthyosis, impetigo, inflammatory acne, ingrown nails, intertrigo, irritant contact dermatitis, ischemic necrosis, itching, jock itch, Kaposi'"'"'s sarcoma, keratosis pilaris, lichen simplex chronicus, lichen planus, lichen sclerosus, lymphadenitis, lymphadenitis, lymphangitis, malignant melanoma, mastocytosis, measles, melanoma, miliaria, moles, molluscum contagiosum, MRSA, necrotizing subcutaneous infection, necrotizing fasciitis, necrotizing myositis, nodular papulopustular acne, non-inflammatory acne, nummular dermatitis, oral herpes, panniculitis, parapsoriasis paronychia, parasitic skin infections, pemphigus, photo-allergy, photo-damage, photo-irritation, photosensitivity, papules, pediculosis, perioral dermatitis, pimples, pityriasis rosea, pityriasis Lichenoides, pityriasis rosea, pityriasis rubra pilaris, poison ivy, poison oak post-operative or post-surgical skin conditions, pressure ulcers, pressure urticaria, pruritis, pseudofolliculitis barbae, psoriasis, PUPPP, purpura, pustules, pyogenic granuloma, rash, ringworm, rosacea, roseola, rubella, scabies, scalded skin syndrome, scarring, scleroderma, sebaceous cyst, seborrheic dermatitis, seborrheic keratosis, shingles, skin aging, skin cancer, skin neoplasia, skin neoplasms, skin rash, skin ulcers, squamous cell carcinoma, staphylococcal scalded skin syndrome, stasis dermatitis, Stevens-Johnson syndrome, sunburn, sun spots, thermal burns, tinea corporis, tinea cruris, tinea pedis, tinea versicolor, toxic epidermal necrolysis, trauma or injury to the skin, varicella zoster virus, vitamin D deficiency, viral skin infections, vitiligo, warts, water hives, wrinkles, xerosis, yeast skin infections, and zoster.

17. The composition of claim 1, wherein the composition comprises less than 1% foam adjuvant.

18. The composition of claim 1, wherein the composition is free of foam adjuvants having a gel building role.

25. The composition of claim 2, wherein the active agent is a cosmetic agent.

26. The composition of claim 1, wherein the liquid oil is selected from a mineral oil, capric/caprylic triglyceride, PPG-15 stearyl ether, isopropyl palmitate, isopropyl myristate, octyldodecanol, and a mixture of two or more thereof.

27. The composition of claim 26, wherein the liquid oil comprises a mineral oil.

28. The composition of claim 27, wherein the mineral oil is a heavy mineral oil, a light mineral oil, or a mixture thereof.

33. The composition of claim 1, wherein the ratio of the carrier to the propellant is from about 100:

8 to about 100;

12.

43. The composition of claim 1, wherein the liquid oil comprises a mineral oil, a soybean oil, a coconut oil, a silicone oil or a mixture of any two or more thereof.

19. A waterless foamable composition free of surfactant and polymeric agent comprising:

a carrier comprising;

a) about 50% to about 90% by weight of the carrier of a liquid oil and about 10% to about 50% by weight of the carrier of a paraffin wax selected from the group consisting of a paraffin wax 58-62°

C., a paraffin wax 51-53°

C., and a mixture thereof, wherein the total weight of the liquid oil and wax together is between about 85% and about 100% by weight of the carrier;

or

b) about 40% by weight of the carrier of a liquid oil and about 60% by weight of the carrier of a paraffin wax 42-44°

C.; and

a liquefied or compressed gas propellant, wherein the gas propellant has a vapor pressure of about 40 to about 90 psi;

wherein the ratio of the carrier to the propellant is from about 100;

4 to about 100;

25;

wherein the composition comprises less than 5% foam adjuvant;

wherein the foamable composition is flowable; and

wherein upon dispensing the foamable composition from a container, the composition forms a breakable foam that is stable, yet breaks easily upon application of shear force.

20. The composition of claim 19, wherein the composition further comprises a tetracycline antibiotic.

21. The composition of claim 19, wherein the foamable composition comprises about 5% to about 16% by weight of the gas propellant.

22. The composition of claim 19, wherein the foamable composition comprises about 7% to about 17% of the gas propellant.

23. The composition of claim 19, wherein the foamable composition comprises less than about 0.1% by weight polymeric agent.

29. The composition of claim 19, wherein the liquid oil is selected from a mineral oil, capric/caprylic triglyceride, PPG-15 stearyl ether, isopropyl palmitate, isopropyl myristate, octyldodecanol, and a mixture of two or more thereof.

30. The composition of claim 29, wherein the liquid oil comprises a mineral oil.

34. The composition of claim 19, wherein the ratio of the carrier to the propellant is from about 100:

8 to about 100;

12.

44. The composition of claim 19, wherein the liquid oil comprises a mineral oil, a soybean oil, a coconut oil, a silicone oil or a mixture of any two or more thereof.

24. A waterless foamable composition free of surfactant and polymeric agent comprising:

a carrier comprising;

a) about 60% to about 85% by weight of the carrier of a liquid oil and about 15% to about 40% by weight of the carrier of a paraffin wax 58-62°

C., a paraffin wax 51-53°

C., and a mixture thereof, wherein the total weight of the liquid oil and wax together is between about 85% and about 100% by weight of the carrier;

or

b) about 40% by weight of the carrier of a liquid oil and about 60% by weight of the carrier of a paraffin wax 42-44°

C.; and

a liquefied or compressed gas propellant;

wherein the ratio of the carrier to the propellant is from about 100;

4 to about 100;

25;

wherein the composition comprises less than 5% foam adjuvant; and

wherein upon dispensing the foamable composition from a container, the composition forms a breakable foam that is stable, yet breaks easily upon application of shear force.

31. The composition of claim 24, wherein the liquid oil is selected from a mineral oil, capric/caprylic triglyceride, PPG-15 stearyl ether, isopropyl palmitate, isopropyl myristate, octyldodecanol, and a mixture of two or more thereof.

32. The composition of claim 31, wherein the liquid oil comprises a mineral oil.

35. The composition of claim 24, wherein the ratio of the carrier to the propellant is from about 100:

8 to about 100;

12.

45. The composition of claim 24, wherein the liquid oil comprises a mineral oil, a soybean oil, a coconut oil, a silicone oil or a mixture of any two or more thereof.

36. A waterless foamable composition free of surfactant and polymeric agent comprising:

a carrier comprising;

a) about 50% to about 90% by weight of the carrier of a liquid oil and about 10% to about 50% by weight of the carrier of a paraffin wax that has a melting point between about 47°

C. and about 64°

C., wherein the total weight of the liquid oil and paraffin wax together is between about 85% and about 100% by weight of the carrier;

or

b) about 40% by weight of the carrier of a liquid oil and about 60% by weight of the carrier of a paraffin wax that has a melting point between about 42°

C. and about 44°

C.; and

c) an active agent;

wherein the composition comprises less than 5% foam adjuvant; and

wherein, when a liquefied propellant is added to the foamable composition in an aerosol in an amount effective to achieve an acceptable foam, the composition forms a breakable foam upon dispensing that is stable, yet breaks easily upon application of shear force.

37. The composition of claim 36, wherein the ratio of the carrier to the propellant is from about 100:

4 to about 100;

25.

38. The composition of claim 36, wherein the ratio of the carrier to the propellant is from about 100:

8 to about 100;

12.

39. The composition of claim 36, wherein the liquid oil is selected from a mineral oil, capric/caprylic triglyceride, PPG-15 stearyl ether, isopropyl palmitate, isopropyl myristate, octyldodecanol, and a mixture of two or more thereof.

40. The composition of claim 39, wherein the liquid oil comprises a mineral oil.

41. The composition of claim 40, wherein the mineral oil is a heavy mineral oil, a light mineral oil, or a mixture thereof.

42. The composition of claim 36, wherein the paraffin wax is selected from a paraffin wax 58-62°

C., a paraffin wax 51-53°

C., and a mixture thereof.

46. The composition of claim 36, wherein the liquid oil comprises a mineral oil, a soybean oil, a coconut oil, a silicone oil or a mixture of any two or more thereof.

47. The composition of claim 36, wherein the active agent comprises a doxycycline, a minocycline, or both.

48. The composition of claim 36, wherein the active agent comprises a tetracycline.