Delivery of antihistamines through an inhalation route
First Claim
1. A condensation aerosol for delivery of a drug selected from the group consisting of azatadine, brompheniramine, carbinoxamine, chlorpheniramine, clemastine, cyproheptadine, loratadine, pyrilamine, hydroxyzine and promethazine,wherein the condensation aerosol is formed by heating a thin layer containing the drug, on a solid support, to produce a vapor of the drug, and condensing the vapor to form a condensation aerosol characterized by less than 10% drug degradation products by weight, and an MMAD of less than 5 microns.
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Abstract
The present invention relates to the delivery of antihistamines through an inhalation route. Specifically, it relates to aerosols containing antihistamines that are used in inhalation therapy. In a method aspect of the present invention, an antihistamine is delivered to a patient through an inhalation route. The method comprises: a) heating a thin layer of an antihistamine, on a solid support, to form a vapor; and, b) passing air through the heated vapor to produce aerosol particles having less than 5% antihistamine drug degradation products. In a kit aspect of the present invention, a kit for delivering an antihistamine through an inhalation route is provided which comprises: a) a thin layer of an antihistamine drug and b) a device for dispensing said thin layer as a condensation aerosol.
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Citations
58 Claims
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1. A condensation aerosol for delivery of a drug selected from the group consisting of azatadine, brompheniramine, carbinoxamine, chlorpheniramine, clemastine, cyproheptadine, loratadine, pyrilamine, hydroxyzine and promethazine,
wherein the condensation aerosol is formed by heating a thin layer containing the drug, on a solid support, to produce a vapor of the drug, and condensing the vapor to form a condensation aerosol characterized by less than 10% drug degradation products by weight, and an MMAD of less than 5 microns.
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4. A method of producing a drug selected from the group consisting of azatadine, brompheniramine, carbinoxamine, chlorpheniramine, clemastine, cyproheptadine, loratadine, pyrilamine, hydroxyzine and promethazine in an aerosol form comprising:
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a. heating a thin layer containing the drug, on a solid support, to produce a vapor of the drug, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 10% drug degradation products by weight, and an MMAD of less than 5 microns. - View Dependent Claims (5, 6, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38)
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39. A condensation aerosol for delivery of azatadine, wherein the condensation aerosol is formed by heating a thin layer containing azatadine, on a solid support, to produce a vapor of azatadine, and condensing the vapor to form a condensation aerosol characterized by less than 5% azatadine degradation products by weight, and an MMAD of about 0.2 to 3 microns.
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40. A condensation aerosol for delivery of brompheniramine, wherein the condensation aerosol is formed by heating a thin layer containing brompheniramine, on a solid support, to produce a vapor of brompheniramine, and condensing the vapor to form a condensation aerosol characterized by less than 5% brompheniramine degradation products by weight, and an MMAD of about 0.2 to 3 microns.
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41. A condensation aerosol for delivery of carbinoxamine, wherein the condensation aerosol is formed by heating a thin layer containing carbinoxamine, on a solid support, to produce a vapor of carbinoxamine, and condensing the vapor to form a condensation aerosol characterized by less than 5% carbinoxamine degradation products by weight, and an MMAD of about 0.2 to 3 microns.
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42. A condensation aerosol for delivery of chlorpheniramine, wherein the condensation aerosol is formed by heating a thin layer containing chlorpheniramine, on a solid support, to produce a vapor of chlorpheniramine, and condensing the vapor to form a condensation aerosol characterized by less than 5% chlorpheniramine degradation products by weight, and an MMAD of about 0.2 to 3 microns.
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43. A condensation aerosol for delivery of clemastine, wherein the condensation aerosol is formed by heating a thin layer containing clemastine, on a solid support, to produce a vapor of clemastine, and condensing the vapor to form a condensation aerosol characterized by less than 5% clemastine degradation products by weight, and an MMAD of about 0.2 to 3 microns.
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44. A condensation aerosol for delivery of cyproheptadine, wherein the condensation aerosol is formed by heating a thin layer containing cyproheptadine, on a solid support, to produce a vapor of cyproheptadine, and condensing the vapor to form a condensation aerosol characterized by less than 5% cyproheptadine degradation products by weight, and an MMAD of about 0.2 to 3 microns.
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45. A condensation aerosol for delivery of loratadine, wherein the condensation aerosol is formed by heating a thin layer containing loratadine, on a solid support, to produce a vapor of loratadine, and condensing the vapor to form a condensation aerosol characterized by less than 5% loratadine degradation products by weight, and an MMAD of about 0.2 to 3 microns.
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46. A condensation aerosol for delivery of pyrilamine, wherein the condensation aerosol is formed by heating a thin layer containing pyrilamine, on a solid support, to produce a vapor of pyrilamine, and condensing the vapor to form a condensation aerosol characterized by less than 5% pyrilamine degradation products by weight, and an MMAD of about 0.2 to 3 microns.
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47. A condensation aerosol for delivery of hydroxyzine, wherein the condensation aerosol is formed by heating a thin layer containing hydroxyzine, on a solid support, to produce a vapor of hydroxyzine, and condensing the vapor to form a condensation aerosol characterized by less than 5% hydroxyzine degradation products by weight, and an MMAD of about 0.2 to 3 microns.
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48. A condensation aerosol for delivery of promethazine, wherein the condensation aerosol is formed by heating a thin layer containing promethazine, on a solid support, to produce a vapor of promethazine, and condensing the vapor to form a condensation aerosol characterized by less than 5% promethazine degradation products by weight, and an MMAD of about 0.2 to 3 microns.
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49. A method of producing azatadine in an aerosol form comprising:
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a. heating a thin layer containing azatadine, on a solid support, to produce a vapor of azatadine, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% azatadine degradation products by weight, and an MMAD of about 0.2 to 3 microns.
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50. A method of producing brompheniramine in an aerosol form comprising:
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a. heating a thin layer containing brompheniramine, on a solid support, to produce a vapor of brompheniramine, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% brompheniramine degradation products by weight, and an MMAD of about 0.2 to 3 microns.
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51. A method of producing carbinoxamine in an aerosol form comprising:
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a. heating a thin layer containing carbinoxamine, on a solid support, to produce a vapor of carbinoxamine, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% carbinoxamine degradation products by weight, and an MMAD of about 0.2 to 3 microns.
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52. A method of producing chlorpheniramine in an aerosol form comprising:
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a. heating a thin layer containing chlorpheniramine, on a solid support, to produce a vapor of chlorpheniramine, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% chlorpheniramine degradation products by weight, and an MMAD of about 0.2 to 3 microns.
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53. A method of producing clemastine in an aerosol form comprising:
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a. heating a thin layer containing clemastine, on a solid support, to produce a vapor of clemastine, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% clemastine degradation products by weight, and an MMAD of about 0.2 to 3 microns.
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54. A method of producing cyproheptadine in an aerosol form comprising:
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a. heating a thin layer containing cyproheptadine, on a solid support, to produce a vapor of cyproheptadine, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% cyproheptadine degradation products by weight, and an MMAD of about 0.2 to 3 microns.
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55. A method of producing loratadine in an aerosol form comprising:
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a. heating a thin layer containing loratadine, on a solid support, to produce a vapor of loratadine, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% loratadine degradation products by weight, and an MMAD of about 0.2 to 3 microns.
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56. A method of producing pyrilamine in an aerosol form comprising:
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a. heating a thin layer containing pyrilamine, on a solid support, to produce a vapor of pyrilamine, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% pyrilamine degradation products by weight, and an MMAD of about 0.2 to 3 microns.
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57. A method of producing hydroxyzine in an aerosol form comprising:
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a. heating a thin layer containing hydroxyzine, on a solid support, to produce a vapor of hydroxyzine, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% hydroxyzine degradation products by weight, and an MMAD of about 0.2 to 3 microns.
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58. A method of producing promethazine in an aerosol form comprising:
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a. heating a thin layer containing promethazine, on a solid support, to produce a vapor of promethazine, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% promethazine degradation products by weight, and an MMAD of about 0.2 to 3 microns.
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Specification