The invention relates to a pharmaceutical aerosol formulation comprising a surfactant that is an alkyl-polyglycoside of formula I, wherein DP is the average degree of polymerisation and has a value of from 1 to 4, and R is an alkyl chain or a mixture of alkyl chains having a chain length of from 6 t
The invention relates to a pharmaceutical aerosol formulation comprising a surfactant that is an alkyl-polyglycoside of formula I, wherein DP is the average degree of polymerisation and has a value of from 1 to 4, and R is an alkyl chain or a mixture of alkyl chains having a chain length of from 6 to 22 carbon atoms; or a derivative thereof for the administration of a medicament for inhalation.
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What is claimed is: 1. An inhalable pharmaceutical aerosol formulation comprising a hydrofluoroalkane propellant, a medicament and a surfactant that is an alkyl-polyglycoside of formula I: or a derivative thereof; wherein DP is the average degree of polymerisation and R is an alkyl chain or a mix
What is claimed is: 1. An inhalable pharmaceutical aerosol formulation comprising a hydrofluoroalkane propellant, a medicament and a surfactant that is an alkyl-polyglycoside of formula I: or a derivative thereof; wherein DP is the average degree of polymerisation and R is an alkyl chain or a mixture of alkyl chains having a chain length of from 6 to 22 carbon atoms; wherein: R is 2-ethyl-1-hexyl and DP is 1.6; or R is a mixture of C8 and C10 alkyl chains in a ratio of 60 C8:40 C10 and DP is 1.5; or R is a mixture of C16 and C18 alkyl chains and DP is 1.2-1.3; or R is a mixture of C20 and C 22 alkyl chains and DP is 1.2-1.3; or R is C10 and DP is 2.7; or R is a mixture of C10 and C12 alkyl chains and DP is 1.4; or R is a mixture of C12 and C14 alkyl chains and DP is 1.4; or the alkylpolyglycoside is n-dodecyl β-D-maltoside (C 12G2). 2. A formulation according to claim 1 wherein: R is 2-ethyl-1-hexyl and DP is 1.6; or R is a mixture of C8 and C10 alkyl chains in a ratio of 60 C8:40 C10 and DP is 1.5; or R is C10 and DP is 2.7; or R is a mixture of C10 and C12 alkyl chains and DP is 1.4. 3. A formulation according to claim 1 wherein the propellant is HFA-134a or HFA-227ea or a mixture thereof. 4. A formulation according to claim 1 wherein the medicament is a β2-adrenoreceptor agonist, an anticholinergic bronchodilator, or a 16,17-acetal of a pregnane derivative. 5. A formulation according to claim 1 wherein the medicament is formoterol, terbutaline, budesonide or a formoterol/budesonide combination. 6. A formulation according to claim 1 wherein the medicament is a compound of formula: description="In-line Formulae" end="lead"Ar-CH 2--CH2--NH--CR1R2-A-Zdescription="In-line Formulae" end="tail" or a pharmaceutically acceptable salt, ester or solvate thereof; wherein Ar represents a group: A represents a straight or branched C1-12 alkylene chain that is interrupted or terminated by one or more groups selected from--S--,--SO--, SO2--,--O--, SO2NH, NHSO2, CR6R7, phenylmethyne,--NH--,--CONH--,--NHCO--and--NHCONH--; Z represents an aryl group of five or six atoms in a single ring system, which optionally contains from 1 to 3 heteroatoms selected from N, O and S, which single ring system is optionally substituted to form a multiple fused ring system of up to 10 atoms, the aryl group being optionally substituted by one or more groups selected from--OH, halogen, C1-6 alkyl, C1-6 alkoxy, ═O,--NR8R 9, and--NO2; or Z represents a C3-12 cycloalkyl group containing from 1 to 3 heteroatoms selected from N, O and S, optionally substituted by one or more groups selected from--OH, halogen, C1-6 alkyl, C1-6 alkoxy, ═O,--NH2 and NO2; R1, R2, R5, R6, R 7, R8 and R9 each independently represent hydrogen or C1-6 alkyl; and R3 and R4 represent hydrogen, or R3 and R4 together form a group that is--S--,--NR8--or--CH2--. 7. A formulation according to claim 1 wherein the medicament is: 4-hydroxy-7-[2-[2-[3-(2-phenylethoxy)propylsulphonyl] ethylamino]ethyl]-1,3-benzo-thiazol-2(3H)-one; 4-hydroxy-7-[2-[2-[3-(2-phenylethoxy)propoxy]ethylamino]ethyl]-1,3-benzo-thiazol-2(3H)-one; N-[2-[2-(4-hydroxy-2-oxo-3H-1,3-benzothiazol-7-yl)ethylamino] ethyl]-2-(phenyl-ethoxy)ethanesulphonamide; 4-hydroxy-7-[2-[3-[2-[2-(1-naphthalenyl)ethoxy]ethylsulphonyl] propylamino]ethyll]-1,3-benzothiazol-2(3H)-one; 3-[2-(4-hydroxy-2-oxo-3H-1,3-benzothiazol-7-yl)ethylamino]-N-[2-[2-(4-methylphenyl)ethoxy]ethyl]propanesulphonamide; or a pharmaceutically acceptable salt, ester or solvate thereof. 8. A formulation according to claim 1 wherein the medicament is a combination of formoterol and budesonide, formoterol and fluticasone, formoterol and mometasone, salmeterol and fluticasone, formoterol and tiotropium salt, zafirlukast and formoterol, zafirlukast and budesonide, montelukast and formoterol, montelukast and budesonide, loratadine and montelukast, loratadine and zafirlukast, tiotropium and fluticasone, tiotropium and budesonide, tiotropium and mometasone, mometasone and salmeterol, formoterol and rofleponide, salmeterol and budesonide, salmeterol and rofleponide, or tiotropium and rofleponide. 9. A formulation according to claim 1 wherein the amount of surfactant present is at least 0.001% by weight. 10. A formulation according to claim 1 wherein the amount of medicament present is from 0.01 to 1.0% by weight. 11. An inhalable medicinal aerosol containing a formulation according to claim 1. 12. A method of treatment for a patient in need of therapy, comprising administering to said patient a therapeutically effective amount of a formulation according to claim 1. 13. A method of treatment for a patient in need of therapy, comprising administering to said patient via inhalation a therapeutically effective amount of a formulation according to claim 2. 14. A method of treatment for a patient in need of therapy, comprising administering to said patient via inhalation a therapeutically effective amount of a formulation according to claim 3. 15. A method of treatment for a patient in need of therapy, comprising administering to said patient via inhalation a therapeutically effective amount of a formulation according to claim 4. 16. A method of treatment for a patient in need of therapy, comprising administering to said patient via inhalation a therapeutically effective amount of a formulation according to claim 5. 17. A method of treatment for a patient in need of therapy, comprising administering to said patient via inhalation a therapeutically effective amount of a formulation according to claim 6. 18. A method of treatment for a patient in need of therapy, comprising administering to said patient via inhalation a therapeutically effective amount of a formulation according to claim 7. 19. A method of treatment for a patient in need of therapy, comprising administering to said patient via inhalation a therapeutically effective amount of a formulation according to claim 8. 20. A method of treatment for a patient in need of therapy, comprising administering to said patient via inhalation a therapeutically effective amount of a formulation according to claim 9. 21. A method of treatment for a patient in need of therapy, comprising administering to said patient via inhalation a therapeutically effective amount of a formulation according to claim 10. 22. An aerosol canister containing a formulation according to claim 1. 23. An aerosol canister containing a formulation according to claim 2. 24. An aerosol canister containing a formulation according to claim 3. 25. An aerosol canister containing a formulation according to claim 4. 26. An aerosol canister containing a formulation according to claim 5. 27. An aerosol canister containing a formulation according to claim 6. 28. An aerosol canister containing a formulation according to claim 7. 29. An aerosol canister containing a formulation according to claim 8. 30. An aerosol canister containing a formulation according to claim 9. 31. An aerosol canister containing a formulation according to claim 10.
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Boli Zhou ; Maria G. Ochomogo ; Elias A. Shaheen ; Jessica Y. Chung, Aerosol antimicrobial compositions.
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