Foamable composition combining a polar solvent and a hydrophobic carrier

Patent metadata

Field	Value
Publication number	US-10117812-B2
Application number	US-48898906-A
Country	US
Kind code	B2
Filing date	Jul 19, 2006
Priority date	Oct 25, 2002
Publication date	Nov 6, 2018
Grant date	Nov 6, 2018

Abstract

The present invention relates to a foamable vehicle or cosmetic or pharmaceutical composition, comprising: (1) an organic carrier, at a concentration of 10% to 70% by weight, wherein said organic carrier concurrently comprises: (i) at least one hydrophobic organic carrier, and (ii) at least one polar solvent; (2) at least one surface-active agent; (3) water; and (4) at least one liquefied or compressed gas propellant at a concentration of 3% to 25% by weight of the total composition.
The present invention further provides a method of treating, alleviating or preventing a disorder of mammalian subject, comprising administering the above-mentioned compositions to an afflicted target site.

First claim

What is claimed is:

1. A foamable pharmaceutical vehicle or composition, comprising:
(1) a liquid organic carrier, at a concentration of 10% to 70% by weight of the composition, wherein said organic carrier concurrently comprises:
(i) at least one hydrophobic organic carrier comprising a triglyceride, and
(ii) at least one polar solvent comprising dimethyl isosorbide,

(2) a surface-active agent selected from the group consisting of at least one non-ionic surface-active agent, and a mixture of a non-ionic surface-active agent and an ionic surface-active agent, wherein the ratio of non-ionic surface-active agent to ionic surface-active agent is greater than 14:1;
(3) water;
(4) at least one liquefied or compressed gas propellant at a concentration of 3% to 25% by weight of the total composition; and
(5) a polymeric agent selected from the group consisting of a locust bean gum, sodium caseinate, an egg albumin, a gelatin agar, a carrageenin gum, sodium alginate, a xanthan gum, a quince seed extract, a tragacanth gum, a guar gum, a starch, a chemically modified starch, a cellulose ether, an alkyl cellulose, a hydroxyalkyl cellulose, a hydroxyethyl cellulose, a hydroxypropyl cellulose, a methyl cellulose, a carboxymethyl cellulose, a methylhydroxyethylcellulose, a methylhydroxypropylcellulose, a hydroxypropylmethyl cellulose, a hydroxyethylcarboxymethylcellulose, a carboxymethylhydroxyethylcellulose, a hydroxypropyl guar gum, a soluble starch, a carboxyvinyl polymer, a polyvinylpyrrolidone, a polyvinyl alcohol, a polyacrylic acid polymer, a polymethacrylic acid polymer, a polyvinyl acetate polymer, a polyvinyl chloride polymer, a polyvinylidene chloride polymer, an acrylic acid/ethyl acrylate copolymer, a carboxyvinyl polymer, a silicone dioxide, a poly(acrylic)acid, a poly(methylvinyl ether/maleic anhydride) copolymer, a chitosan, an alginic acid, a hyaluronic acid, a pectin, a karaya gum, a cyclodextrin, a chemically modified cyclodextrin, hydroxypropyl-β-cyclodextrin, a poly(N-isopropylamide), a poloxamer, and mixtures of any two or more thereof; and
wherein the composition is provided in an aerosol container and upon release expands to form a breakable foam that collapses upon application of shear force.

2. The composition of claim 1 , wherein the surface active agent is 0.1% to 5% by weight of the composition.

3. The composition of claim 1 or 2 , wherein the ratio of the hydrophobic organic carrier and the polar solvent are selected to provide a selected pharmacological or safety property.

4. The composition of claim 1 , wherein the polymeric agent is 0.01% to 5% by weight of the composition.

5. The composition of claim 1 , wherein the polymeric agent is 0.01% to 1% by weight of the composition.

6. The composition of claim 1 , further comprising 0.1% to 5% by weight of the composition of a therapeutically active foam adjuvant 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; fatty alcohols derived from beeswax and including a mixture of alcohols, a majority of which has at least 20 carbon atoms in their carbon chain; a fatty alcohol having an double bond; a fatty acid having an double bond; a branched fatty alcohol; a branched fatty acid; a fatty acid substituted with a hydroxyl group; cetyl alcohol; stearyl alcohol; arachidyl alcohol; behenyl alcohol; 1-triacontanol; hexadecanoic acid; stearic acid; arachidic acid; behenic acid; octacosanoic acid; 12-hydroxy stearic acid; and a mixture of any two or more thereof.

7. The composition of claim 1 , wherein the polar solvent is soluble in both water and oil.

8. The composition of claim 1 , wherein the hydrophobic organic carrier is a liquid at ambient temperature, and has a solubility in distilled water at ambient temperature selected from:
(i) less than 1 gm per 100 mL;
(ii) less than 0.5 gm per 100 mL; and
(iii) less than 0.1 gm per 100 mL.

9. The composition of claim 1 , wherein the foamable composition is an emulsion or a micro emulsion selected from the group consisting of an oil-in-water emulsion and a water-in-oil emulsion.

10. The composition of claim 1 , wherein upon release from the container, a foam having a density range selected from (1) between 0.02 gr/mL and 0.1 gr/mL; and (2) between 0.04 gr/mL and 0.23 gr/mL is produced.

11. The composition of claim 1 , wherein the triglyceride is capric-caprylic triglyceride.

12. The composition of claim 1 , further comprising an active agent.

13. The composition of claim 12 , wherein the active agent is selected from the group consisting of an anti-infective agent, an antibiotic agent, an antibacterial agent, an antifungal agent, an antiviral agent, an antiparasitic agent, a steroidal anti-inflamatory agent, a nonsteroidal anti-inflammatory agent, an immunosuppressive agent, an immunomodulator, an immunoregulating agent, a hormonal agent, a steroid, a vasoactive agent, a vasoconstructor, a vasodilator, vitamin A, a vitamin A derivative, a retinoid, vitamin B, a vitamin B derivative, vitamin C, a vitamin C derivative, vitamin D, a vitamin D derivative, vitamin E, a vitamin E derivative, vitamin F, a vitamin F derivative, vitamin K, a vitamin K derivative, a wound healing agent, a burn healing agent, an antiallergic agent, a dicarboxylic acid, azelaic acid, sebacic acid, adipic acid, fumaric acid, a retinoid, and a mixture of any two or more thereof at any proportion.

14. The composition of claim 1 , further comprising an active agent, selected from the group consisting of a nonsteroidal anti-inflammatory drug, an immunosuppressive agent, an immunomodulator, an immunoregulating agent, a hormonal agent, a steroid, a steroidal anti-inflammatory agent, vitamin A, a vitamin A derivative, vitamin D, a vitamin D derivative, and a mixture of any two or more thereof.

15. The composition of claim 12 , wherein the active agent comprises an extract or tincture comprising one or more beneficial agents selected from the group consisting of a hyularonic acid, a herbal extract, coal tar, and a mixture of any two or more thereof.

16. The composition of claim 12 , wherein the active agent comprises one or more herbal extracts.

17. The composition of claim 16 , wherein the herbal extract is selected from the group consisting of angelica, calendula, celery, coltsfoot, comfrey, dandelion, jamaica dogwood, kava, marshmallow, prickly ash, northern prickly ash, southern senna, valerian, agrimony, aloe vera, alfalfa, artichoke, avens, bayberry, bloodroot, blue flag, bogbean, boldo, boneset, broom, buchu, burdock, burnet, calamus, calendula, cascara, centaury, cereus, chamomile, german chamomile, roman chamomile, cinnamon, divers, cohosh, black, cohosh, blue, cola, corn silk, couchgrass, cowslip, damiana, devil's claw, drosera, echinacea, elder, elecampane, euphorbia, eyebright, figwort, frangula, fucus, fumitory, garlic, golden seal, gravel root, ground ivy, guaiacum, hawthorn, holy thistle, hops, horehound black, horehound white, horse chestnut hydrangea, ispaghula, juniper, lady's lipper, liferoot, lime flower, liquorice, lobelia, mate, meadowsweet, mistletoe, motherwort, myrrh, nettle, parsley, parsley piert, passionflower, pennyroyal, pilewort, plantain, pleurisy root, pokeroot, poplar, pulsatilla, queen's delight, raspberry, red clover, rosemary, sage, sarsaparilla, sassafras, scullcap, senega, shepherd's purse, skunk cabbage, slippery elm, squill, St. john's wort, stone root, tansy, thyme, uva-ursi, vervain, wild carrot, wild lettuce, willow, witch hazel, yarrow, yellow dock, and a mixtu

Assignees

• Tamarkin Dov
• Friedman Doron
• Eini Meir
• Besonov Alex
• Foamix Pharmaceuticals Ltd

Inventors

• Tamarkin Dov
• Friedman Doron
• Eini Meir
• Besonov Alex

Classifications

• A61K47/22

  Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones · CPC title

• A61K47/38

  Cellulose; Derivatives thereof · CPC title

• A61K9/0014

  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 title

• A61K8/4973

  with oxygen as the only hetero atom · CPC title

• A61K9/122

  Foams; Dry foams (edible foams A61K9/0056) · CPC title