The subject invention provides improved testosterone gel formulations.
대표청구항▼
1. A transdermal or transmucosal formulation comprising: 2% wt of testosterone,at least one C2 to C4 alkanol,15-30% wt polyalcohol, wherein the polyalcohol is one or more of a C2 to C6 alkane or C2 to C6 alkene, substituted with two or more hydroxyl groups, andmonoalkyl ether of diethylene glycol, w
1. A transdermal or transmucosal formulation comprising: 2% wt of testosterone,at least one C2 to C4 alkanol,15-30% wt polyalcohol, wherein the polyalcohol is one or more of a C2 to C6 alkane or C2 to C6 alkene, substituted with two or more hydroxyl groups, andmonoalkyl ether of diethylene glycol, wherein said formulation is substantially free of long-chain fatty alcohols, long-chain fatty acids, and long-chain fatty esters. 2. The transdermal or transmucosal formulation according to claim 1, further comprising at least one of: gelling agent,neutralizing agent,chelating agent andsolvent or any combinations thereof. 3. The formulation of claim 2, wherein the alkanol is present in an amount between about 5-50% wt, the permeation enhancer is present in an amount of between about 0.2-25% wt, the gelling agent is present in an amount between about 0.05-4% wt, the neutralizing agent is present in an amount between about 0.05-1% wt, and the chelating agent is present in an amount between about 0.001-5.0% wt. 4. The formulation of claim 1, wherein the at least one alkanol is chosen from ethanol, isopropanol n-propanol, and combinations thereof. 5. The formulation of claim 1, wherein the at least one alkanol is ethanol. 6. The formulation of claim 1, wherein the alkanol is ethanol, present in an amount of about 44.0% wt. 7. The formulation of claim 1, wherein the polyalcohol is propylene glycol. 8. The formulation of claim 7, wherein the propylene glycol is present in an amount of about 20.0% wt. 9. The formulation of claim 1, wherein the monoalkyl ether of diethylene glycol is chosen from diethylene glycol monoethyl ether, diethylene glycol monomethyl ether, and combination thereof. 10. The formulation of claim 9, wherein diethylene glycol monoethyl ether is present in an amount of 5.0% wt. 11. The formulation of claim 2, wherein the gelling agent is carbomer. 12. The formulation of claim 11, wherein the carbomer is present in an amount of 1.20% wt. 13. The formulation of claim 2, wherein the gelling agent is poly(acrylic acid), present in an amount of 1.20% wt. 14. The formulation of claim 2, wherein the neutralizing agent is triethanolamine. 15. The formulation of claim 14, wherein the triethanolamine is present in an amount of 0.35% wt. 16. The formulation of claim 2, wherein the chelating agent is edetate disodium. 17. The formulation of claim 16, wherein the edetate disodium is present in an amount of 0.06% wt. 18. The formulation of claim 2, wherein the solvent is water. 19. A transdermal or transmucosal formulation comprising: 2% wt of testosterone, 44.0% wt of ethanol, 20.0% wt of propylene glycol, and 5.0% wt of diethylene glycol monoethyl ether, wherein said formulation is substantially free of long-chain fatty alcohols, long-chain fatty acids, and long-chain fatty esters. 20. A transdermal or transmucosal formulation comprising: 2% wt of testosterone, 44.0% wt of ethanol, 20.0% wt of propylene glycol, 5.0% wt of diethylene glycol monoethyl ether, 1.20% wt of carbomer, 0.35% wt of triethanolamine, 0.06% wt of edetate disodium and water wherein said formulation is substantially free of long-chain fatty alcohols, long-chain fatty acids, and long-chain fatty esters. 21. A transdermal or transmucosal formulation consisting of 2% wt of testosterone, 44.0% wt of ethanol, 20.0% wt of propylene glycol, 5.0% wt of diethylene glycol monoethyl ether, 1.20% wt of carbomer, 0.35% wt of triethanolamine, 0.06% wt of edetate disodium and water. 22. The formulation of claim 1, wherein the formulation is in the form chosen from a gel, lotion, cream, spray, aerosol, ointment, emulsion, suspension, liposomal system, lacquer, patch, bandage, buccal tablet, sublingual tablet, suppository, vaginal dosage form or occlusive dressing. 23. The formulation claim 22, wherein the form is a gel. 24. The formulation claim 1, wherein the formulation is adapted for transdermal or transmucosal administration according to a schedule having a periodicity chosen from once to five times daily dosing, once-weekly dosing or bi-weekly dosing. 25. The formulation of claim 1, wherein the formulation is adapted for a once daily transdermal or transmucosal administration. 26. The formulation of claim 1, wherein the formulation is adapted for a once daily transdermal or transmucosal administration to the abdomen of a mammal in need thereof. 27. The formulation of claim 1, wherein the formulation is adapted for a once daily transdermal or transmucosal administration to the upper arm of a mammal in need thereof. 28. A method for administering testosterone to a mammal in need thereof comprising: transdermally administering to a skin or mucosal membrane of a mammal a formulation according to claim 1. 29. A method of treating a disease or disorder associated with reduced endogenous testosterone production comprising: transdermally administering to a skin or mucosal membrane of a mammal a formulation according to claim 1. 30. The method according to claim 28 or 29, wherein said mammal is a male. 31. A method of treating a disease or disorder associated with reduced endogenous testosterone production in a male subject comprising: transdermally administering to a skin or mucosal membrane of a male subject a formulation comprising: 1-2% wt of testosterone, C2 to C4 alkanol, 20.0% wt of propylene glycol, and monoalkyl ether of diethylene glycol, wherein said formulation is substantially free of long-chain fatty alcohols, long-chain fatty acids, and long-chain fatty esters. 32. A method of treating a disease or disorder associated with reduced endogenous testosterone production in a male subject comprising: transdermally administering to a skin or mucosal membrane of a male subject a formulation comprising: 1-2% wt of testosterone, C2 to C4 alkanol, 20.0% wt of propylene glycol, monoalkyl ether of diethylene glycol, gelling agent, neutralizing agent, chelating agent and solvent, wherein said formulation is substantially free of long-chain fatty alcohols, long-chain fatty acids, and long-chain fatty esters. 33. A method of treating a disease or disorder associated with reduced endogenous testosterone production in a male subject comprising: transdermally administering to a skin or mucosal membrane of a male subject a formulation comprising 1-2% wt of testosterone, 44% wt of ethanol, 20.0% wt of propylene glycol, 5% wt of monoethyl ether of diethylene glycol, 1.20% wt of carbomer, 0.35% wt of triethanolamine, 0.06% wt of edetate disodium and water wherein the formulation is substantially free of long-chain fatty alcohols, long-chain fatty acids, and long-chain fatty esters. 34. A method of treating a disease or disorder associated with reduced endogenous testosterone production in a male subject comprising: transdermally administering to a skin or mucosal membrane of a male subject a formulation consisting of 1-2% wt of testosterone, 44% wt of ethanol, 20.0% wt of propylene glycol, 5% wt of monoethyl ether of diethylene glycol, 1.20% wt of carbomer, 0.35% wt of triethanolamine, 0.06% wt of edetate disodium and water. 35. The method according to claim 29, wherein the disease or disorder associated with reduced endogenous testosterone production is hypogonadism. 36. The method according to claim 29, further comprising administering another treatment. 37. A kit comprising at least one container comprising a formulation according to claim 1, and instructions for use thereof. 38. A kit according to claim 37, wherein said container is adapted for dispensing a predetermined measured amount of the formulation.
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이 특허에 인용된 특허 (10)
Carrara,Dario Norberto R.; Grenier,Arnaud; Besse,Celine; Simes,Stephen M.; Lehman,Leah M., Formulations for transdermal or transmucosal application.
Rivier Jean E. F. (La Jolla CA) Porter John S. (Leucadia CA) Hoeger Carl A. (San Marcos CA) Jiang Guangcheng (La Jolla CA) Rivier Catherine L. (La Jolla CA), GNRH antagonists XIII.
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