Pharmaceutical and cosmetic carrier and composition for topical application
View Patent ↗A pharmaceutical or cosmetic carrier or composition for topical application characterized by rheological properties which render the carrier or composition semi-solid at rest and a liquid upon application of shear forces thereto. The composition or carrier are prepared by mixing 1–25 percent of a solidifying agent and 75–99 percent of a hydrophobic solvent, by weight, wherein at least one of them has therapeutic or cosmetic benefits, in the presence or absence of a biologically active substance.
1. A method of treating a disease or disorder of a skin or a mucosal membrane comprising:
topically administering to the skin or the mucosal membrane a pharmaceutical composition containing, by weight, 1–25 percent of a solidifying agent, wherein the solidifying agent consists essentially of at least one long chain fatty alcohol having at least 15 carbons atoms in its carbon backbone and at least one fatty acid, having at least 18 carbon atoms in its carbon backbone, and 75–99 percent of a hydrophobic solvent, wherein at least one of the solidifying agent and the hydrophobic agent has a therapeutic or cosmetic beneficial effect, and wherein the solidifying agent and the hydrophobic solvent are selected such that under ambient conditions, the composition is semi-solid a rest and liquefies upon application of shear forces thereto,
wherein the disease or disorder is selected from the group consisting of psoriasis, acne, seborrhea, seborrheic dermatitis, alopecia and excessive hair growth, ichthyosis, wounds, burns, cuts, ulcers, psoriasis, seborrheic dermatitis of the face and trunk, seborrheic blepharitis, contact dermatitis, stasis dermatitis and exfoliative dermatitis.
2. The method of claim 1 , wherein the statis dermatitis is selected from the group consisting of gravitational eczema, varicose eczema and further wherein the exfoliative dermatitis is erythroderma.
3. The method of claim 1 , wherein the mucosal membrane is selected from the group consisting of a mucosa of a nose, a mucosa of a mouth, a mucosa of an eye, a mucosa of an ear, a mucosa of a vagina and a mucosa of a rectum.
4. The method of claim 1 , wherein the disease or disorder is an inflammation caused by an inflammatory agent selected from the group consisting of a bacterial inflammatory agent, a fungal inflammatory agent, a viral inflammatory agent, a parasitic inflammatory agent, an autoimmune inflammatory agent, an allergic inflammatory agent, a hormonal inflammatory agent and a malignant inflammatory agent.
5. The method of claim 1 , wherein the hydrophobic solvent is selected from the group consisting of marine animal derived oils, terrestrial animal derived oils, mineral oils, silicone oils and plant-derived oils.
6. The method of claim 1 , wherein the hydrophobic solvent includes an oil selected from the group consisting of olive oil, soybean oil, canola oil, rapeseed oil, cottonseed oil, coconut oil, palm oil, sesame oil, sunflower oil, safflower oil, rice bran oil, borage seed oil, syzigium aromaticum oil, hempseed oil, herring oil, cod-liver oil, salmon oil, corn oil, flaxseed oil, wheat germ oil, rape seed oil, evening primrose oil, rosehip oil, tea tree oil, melaleuca oil and jojova oil.
7. The method of claim 1 , wherein the hydrophobic solvent includes an oil selected from the group consisting of omega-3 oil and omega-6 oil.
8. The method of claim 1 , wherein at least one of the fatty alcohol and the fatty acid has at least one alkyl group side chain in its carbon backbone.
9. The method of claim 1 , wherein the carbon backbone of at least one of the fatty acid and fatty alcohol has at least one hydroxyl group.
10. The method of claim 9 , wherein the carbon backbone of at least one of the fatty acid and the fatty alcohol has at least one hydroxyl group at positions 8–14.
11. The method of claim 1 , wherein the solidifying agent includes a 12-hydroxy fatty acid.
12. A method of treating a disease or disorder of a skin or a mucosal membrane comprising the step of topically administrating thereto a pharmaceutical composition containing:
(a) a pharmaceutical or cosmetic carrier containing, by weight, 1–25 percent of a solidifying agent, wherein the solidifying agent consists essentially of at least one long chain fatty alcohol having at least 15 carbon atoms in its carbon backbone and at least one fatty acid having at least 18 carbon atoms in its carbon backbone, and 75–99 percent of a hydrophobic solvent; and
(b) a therapeutically or cosmetically effective amount of a biologically active substance,
wherein the solidifying agent and the hydrophobic solvent are selected such that under ambient conditions, the carrier is semi-solid at rest and liquefies upon application of shear forces thereto, and
wherein the biologically active substance is effective in the treatment of a disease or disorder selected from the group consisting of psoriasis, acne, seborrhea, seborrheic dermatitis, alopecia and excessive hair growth, ichthyosis, wounds, burns, cuts, ulcers, psoriasis, seborrheic dermatitis of the face and trunk, seborrheic blepharitis, contact dermatitis, stasis dermatitis and exfoliative dermatitis.
13. The method of claim 12 , wherein the mucosal membrane is selected from the group consisting of a mucosa of a nose, a mucosa of a mouth, a mucosa of an eye, a mucosa of an ear, a mucosa of a vagina and mucosa of a rectum.
14. The method of claim 12 , wherein the hydrophobic solvent is selected from the group consisting of marine animal derived oils, terrestrial animal derived oils, mineral oils, silicone oils and plant-derived oils.
15. The method of claim 12 , wherein the hydrophobic solvent includes an oil selected from the group consisting of olive oil, soybean oil, canola oil, rapeseed oil, cottonseed oil, coconut oil, palm oil, sesame oil, sunflower oil, safflower oil, rice bran oil, borage seed oil, syzigium aromaticum oil, hempseed oil, herring oil, cod-liver oil, salmon oil, corn oil, flaxseed oil, wheat germ oil, rape seed oil, evening primrose oil, rosehip oil, tea tree oil, melaleuca oil and jojova oil.
16. The method of claim 12 , wherein the hydrophobic solvent includes an oil selected from the group consisting of omega-3 oil and omega-6 oil.
17. The method of claim 12 , wherein at least one of the fatty acid and the fatty alcohol has at least one alkyl group side chain in its carbon backbone.
18. The method of claim 12 , wherein the carbon backbone of at least one of the fatty acid and the fatty alcohol has at least one hydroxyl group.
19. The method of claim 12 , wherein the carbon backbone of at least one of the fatty acid and the fatty alcohol has at least one hydroxyl group at positions 8–14.
20. The method of claim 12 , wherein the solidifying agent comprises a 12-hydroxy fatty acid.
21. The method of claim 12 , wherein the disease or disorder is inflammation caused by an inflammatory agent selected from the group consisting of a bacterial inflammatory agent, a fungal inflammatory agent, a viral inflammatory agent, a parasitic inflammatory agent, an autoimmune inflammatory agent, an allergic inflammatory agent, a hormonal inflammatory agent and a malignant inflammatory agent.
22. The method of claim 12 , wherein the statis dermatitis is selected from the group consisting of gravitational eczema, varicose eczema and further wherein the exfoliative dermatitis is erythroderma.
23. The method of claim 12 , wherein the biologically active substance is effective in the treatment of a disease or disorder selected from the group consisting of psoriasis, acne, seborrhea, seborrheic dermatitis, alopecia and excessive hair growth, ichthyosis, wounds, burns, cuts, ulcers, psoriasis, seborrheic dermatitis of the face and trunk, seborrheic blepharitis, contact dermatitis, stasis dermatitis and exfoliative dermatitis.
24. The method of claim 23 , wherein the statis dermatitis is selected from the group consisting of gravitational eczema, varicose eczema and further wherein the exfoliative dermatitis is erythroderma.
25. The method of claim 12 , wherein the biologically active substance is selected from the group of consisting of an antibiotic agent, a free radical generating agent, an antifungal agent, an antiviral agent, a non-steroidal antiinflammatory drug, an immunosuppressant, an antihistamine agent, an antiinflammatory agent, a retinoid agent, a tar agent, an antipruritics agent and a scabicide agent.
26. The method of claim 25 , wherein:
(a) the antibiotic agent is selected from the group consisting of chloramphenicol, tetracyclines, synthetic and semi-synthesic penicillins, beta-lactames, quinolones, fluoroquinolnes, macrolide antibiotics, peptide antibiotics, cyclosporines, erytromycin and clinndamycin;
(b) the free radical generating agent is benzoyl peroxide;
(c) the antifungal agent is selected from the group consisting of azoles, diazoles, triazoles, miconazole, fiuconazole, ketoconazole, clotrimazole, itraconazole griseofulvin, ciclopirox, amorolfine, terbinafine, Amphotericin B and potassium iodide;
(d) the antiviral agent is selected from the group consisting of flucytosine (5FC), Vidarabine, acyclovir and Gancyclovir;
(e) the immunosuppressant is selected from the group consisting of Clobetasol proprionate, Halobetasol proprionate, Betamethasone diproprionate, Betamethasone valerate, Fluocinolone acetonide, Halcinonide, Betamethasone valerate, Fluocinolone acetonide, Hydrocortisone valerate, Triamcinolone acetonide, Hydrocortisone and hexachlorobenzene;
(f) the antiinflammatory agent is a vitamin B3;
(g) the retinoid agent is selected from the group consisting of isotretinoin, adapalene and tretinoin;
(h) the tar agent is selected from the group consisting of coal tar and cade oil;
(i) the antihistamine agent is doxepine hydrochloride;
(j) the antipruritic agent is crotampiton; and
(k) the scabicide agent is selected from the group consisting of benzyl benzoate, malathion and crotamiton.
27. A method of treating dermatosis of a skin or a mucosal membrane comprising the step of topically administering to the skin or the mucosal membrane a pharmaceutical or cosmetic composition containing,
(a) a carrier comprising, by weight, 1–12 percent of a solidifying agent consisting essentially of long chain fatty alcohols having 18–22 carbons atoms in its carbon backbone and long chain fatty acids having 18–22 carbon atoms in its carbon backbone and 75–99 percent of a triglyeride hydrophobic solvent; and
(b) a therapeutic or cosmetically effective amount of a biologically active substance that treats a symptom of dermatosis.
28. The method of claim 27 , wherein the dermatosis is an inflammation caused by a fungal inflammatory agent.
29. The method of claim 27 , wherein the biologically active agent is an antimicrobial agent.