Pharmaceutical 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. An oleaginous pharmaceutical carrier comprising:
a mixture comprising, by weight:
75-99 percent of a hydrophobic solvent, and
1-25 percent of a solidifying agent, wherein said solidifying agent is selected from the group consisting of (i) at least one long chain fatty alcohol having at least 15 carbon atoms in its carbon backbone (ii) at least one fatty acid having at least 18 carbons in its carbon backbone, and (iii) a mixture thereof
wherein the pharmaceutical carrier is semi-solid at rest and liquefies upon application of shear forces thereto; and
wherein the carrier is free of a netted framework of solidifying agent.
2. A pharmaceutical composition, comprising the carrier of claim 1 , further comprising a therapeutically effective amount of a biologically active substance.
3. The pharmaceutical composition of claim 2 , 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 anti-inflammatory drug, an immunosuppressant, an antihistamine agent, an anti-inflammatory agent, a retinoid agent, a tar agent, an antipruritics agent and a scabicide agent.
4. The pharmaceutical composition of claim 3 , wherein the antibiotic agent comprises a tetracycline antibiotic.
5. The pharmaceutical composition of claim 2 , wherein said 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 jojoba oil.
6. The pharmaceutical composition of claim 2 , wherein said hydrophobic solvent includes an oil selected from the group consisting of marine animal derived oils, terrestrial animal derived oils, mineral oils, silicone oils and plant-derived oils.
7. The pharmaceutical composition of claim 2 , wherein said hydrophobic solvent includes an oil selected from the group consisting of omega-3 oil and omega-6 oil.
8. The pharmaceutical composition of claim 2 , wherein the hydrophobic solvent comprises a silicone oil.
9. The pharmaceutical composition of claim 2 , wherein the carrier provides a protective moisture barrier.
10. The pharmaceutical composition of claim 2 , wherein the composition spreads easily and is non sticky.
11. The pharmaceutical composition of claim 2 , wherein said solidifying agent includes a 12-hydroxy fatty acid and or behenyl alcohol.
12. The pharmaceutical composition of claim 2 ,
wherein the solidifying agent is solid at ambient temperature; and
wherein the biologically active substance comprises a tetracycline antibiotic in a therapeutically effective amount to treat a disease or disorder of the skin or mucosal membrane.
13. A method of applying:
a pharmaceutical composition to a skin or a mucosal membrane having a disease or disorder, comprising topically administering the pharmaceutical composition to the skin or the mucosal membrane surface, said pharmaceutical composition comprising, by weight, a mixture of:
75-99 percent of a hydrophobic solvent,
1-25 percent of a solidifying agent, wherein said solidifying agent is selected from the group consisting of (i) at least one long chain fatty alcohol having at least 15 carbon atoms in its carbon backbone (ii) at least one fatty acid having at least 18 carbons in its carbon backbone and (iii) a mixture thereof; and
a biologically active agent,
wherein the composition is semi-solid at rest and liquefies upon application of shear forces thereto; and
wherein the composition is free of a netted framework of solidifying agent.
14. The method of claim 13 , wherein on application the composition freely spreads on the skin surface or mucosal membrane and is rapidly absorbed.
15. The method of claim 14 , wherein the composition spreads without film formation.
16. The method of claim 13 , wherein the composition is adapted to facilitate enhanced penetration of the active agent.
17. The method of claim 13 , 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.
18. The method of claim 13 , wherein said 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 anti-inflammatory drug, an immunosuppressant, an antihistamine agent, an anti-inflammatory agent, a retinoid agent, a tar agent, an antipruritic agent and a scabicide agent.
19. The method of claim 13 , wherein the biologically active agent comprises a tetracycline antibiotic.
20. The method of claim 13 , wherein said 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 jojoba oil.
21. The method of claim 13 , wherein said hydrophobic solvent includes an oil selected from the group consisting of marine animal derived oils, terrestrial animal derived oils, mineral oils, silicone oils and plant-derived oils.
22. The method of claim 13 , wherein said hydrophobic solvent includes an oil selected from the group consisting of omega-3 oil and omega-6 oil.
23. The method of claim 13 , wherein the composition provides a protective moisture barrier.
24. The method of claim 15 , wherein the composition is delivered by means of a dermal patch or as a suppository.
25. The method of claim 13 , wherein said solidifying agent includes a 12-hydroxy fatty acid and or behenyl alcohol.
26. The method of claim 13 , wherein the solidifying agent is solid at ambient temperature;
wherein the biologically active substance comprises a tetracycline antibiotic in a therapeutically effective amount to treat a disease or disorder of the skin or mucosal membrane.
27. A method of preparing an oleaginous pharmaceutical carrier, the method comprising the steps of mixing a hydrophobic solvent and a solidifying agent at a temperature above a melting temperature of the solidifying agent so as to obtain a mixture containing 75-99 percent of the hydrophobic solvent by weight and 1-25 percent of the solidifying agent by weight; and cooling the mixture,
wherein said solidifying agent is selected from the group consisting of (i) at least one long chain fatty alcohol having at least 15 carbon atoms in its carbon backbone (ii) at least one fatty acid having at least 18 carbons in its carbon backbone, and (iii) a mixture thereof; and
wherein the pharmaceutical carrier is semi-solid at rest and liquefies upon application of shear forces thereto.
28. The method of claim 27 , further comprising:
mixing into the mixture a therapeutically or cosmetically effective amount of a biologically active substance.
29. The method of claim 18 , wherein the antibiotic agent is selected from the group consisting of chloramphenicol, a tetracyclines, a synthetic penicillins, a semi-synthetic penicillin, a beta-lactam, a quinolone, a fluoroquinolone, a macrolide antibiotic, a peptide antibiotic, a cyclosporine, erythromycin clyndamycin and mixtures thereof.
30. The pharmaceutical composition of claim 2 , wherein the biologically active substance is selected from the group consisting of chloramphenicol, a tetracyclines, a synthetic penicillin, semi-synthetic penicillins, a beta-lactam, a quinolone, a fluoroquinolone, a macrolide antibiotic, a peptide antibiotic, a cyclosporine, erythromycin, clyndamycin and mixtures thereof.
31. A method of treating a disease or disorder of a skin or a mucosal membrane comprising:
topically administering a pharmaceutical composition to the skin or the mucosal membrane, said pharmaceutical composition comprising, by weight, a mixture of:
75-99 percent of a hydrophobic solvent,
1-25 percent of a solidifying agent, wherein said solidifying agent is selected from the group consisting of (i) at least one long chain fatty alcohol having at least 15 carbon atoms in its carbon backbone (ii) at least one fatty acid having at least 18 carbons in its carbon backbone and (iii) a mixture thereof; and
a biologically active agent selected from the group consisting of an antibiotic agent, a free radical generating agent, an antifungal agent, an antiviral agent, a non-steroidal anti-inflammatory drug, an immunosuppressant, an antihistamine agent, an anti-inflammatory agent, a retinoid agent, a tar agent, an antipruritics agent, and a scabicide agent and wherein the antibiotic agent is selected from the group consisting of chloramphenicol, tetracyclines, synthetic and semi-synthetic penicillins, beta-lactams, quinolones, fluoroquinolones, macrolide antibiotics, peptide antibiotics, cyclosporines, erythromycin, clyndamycin, and mixtures thereof;
wherein the composition is semi-solid at rest and liquefies upon application of shear forces thereto;
wherein the composition is free of a netted framework of solidifying agent; and
wherein the disease or disorder is selected from the group consisting of psoriasis, acne, seborrhea, seborrheic dermatitis, alopecia, excessive hair growth, ichthyosis, infection, inflammation, wounds, burns, cuts, ulcers, psoriasis, seborrheic dermatitis of the face and trunk, seborrheic blepharitis, contact dermatitis, stasis dermatitis, and exfoliative dermatitis.