Delivery of physiologically active compounds through an inhalation route
First Claim
1. A condensation aerosol for delivery of chlordiazepoxide formed by heating a composition containing chlordiazepoxide coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of chlordiazepoxide and less than 5 percent by weight of chlordiazepoxide degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
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Abstract
The present invention relates to the delivery of physiologically active compounds through an inhalation route. Specifically, it relates to aerosols containing physiologically active compounds that are used in inhalation therapy. In a method aspect of the present invention, the physiologically active compound is delivered to a patient through an inhalation route. The method comprises: a) heating a coating of a physiologically active compound, on a solid support, to form a vapor; and, b) passing air through the heated vapor to produce aerosol particles having less than 5% physiologically active compound degradation products. In a kit aspect of the present invention, a kit for delivering a physiologically active compound through an inhalation route is provided which comprises: a) a thin coating of a physiologically active compound, and b) a device for dispensing said thin coating as a condensation aerosol.
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Citations
77 Claims
- 1. A condensation aerosol for delivery of chlordiazepoxide formed by heating a composition containing chlordiazepoxide coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of chlordiazepoxide and less than 5 percent by weight of chlordiazepoxide degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
- 4. A condensation aerosol for delivery of betahistine formed by heating a composition containing betahistine coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of betahistine and less than 5 percent by weight of betahistine degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
- 7. A condensation aerosol for delivery of clonidine formed by heating a composition containing clonidine coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of clonidine and less than 5 percent by weight of clonidine degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
- 10. A condensation aerosol for delivery of testosterone formed by heating a composition containing testosterone coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of testosterone and less than 5 percent by weight of testosterone degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
- 13. A condensation aerosol for delivery of a conjugated estrogen formed by heating a composition containing the conjugated estrogen coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of the conjugated estrogen and less than 5 percent by weight of the conjugated estrogen degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
- 16. A condensation aerosol for delivery of estradiol formed by heating a composition containing estradiol coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of estradiol and less than 5 percent by weight of estradiol degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
- 19. A condensation aerosol for delivery of ethinyl estradiol formed by heating a composition containing ethinyl estradiol coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of ethinyl estradiol and less than 5 percent by weight of ethinyl estradiol degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
- 22. A condensation aerosol for delivery of hyoscyamine formed by heating a composition containing hyoscyamine coated on a solid support to form a vapor and condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise at least 10 percent by weight of hyoscyamine and less than 5 percent by weight of hyoscyamine degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
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25. A method of forming a chlordiazepoxide containing aerosol comprising:
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(a) heating a composition containing chlordiazepoxide coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of chlordiazepoxide degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (26, 27, 63)
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28. A method of forming a betahistine containing aerosol comprising:
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(a) heating a composition containing betahistine coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of betahistine degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (29, 30, 64)
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31. A method of forming a clonidine containing aerosol comprising:
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(a) heating a composition containing clonidine coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of clonidine degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (32, 33, 65)
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34. A method of forming a testosterone containing aerosol comprising:
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(a) heating a composition containing testosterone coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of testosterone degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (35, 36, 66)
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37. A method of forming a conjugated estrogen containing aerosol comprising:
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(a) heating a composition containing the conjugated estrogen coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of the conjugated estrogen degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (38, 39, 67)
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40. A method of forming an estradiol containing aerosol comprising:
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(a) heating a composition containing estradiol coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of estradiol degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (41, 42, 68)
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43. A method of forming an ethinyl estradiol containing aerosol comprising:
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(a) heating a composition containing ethinyl estradiol coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of ethinyl estradiol degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (44, 45, 69)
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46. A method of forming a hyoscyamine containing aerosol comprising:
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(a) heating a composition containing hyoscyamine coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of hyoscyamine degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (47, 48, 70)
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49. A method of forming a drug containing aerosol comprising:
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(a) heating a composition containing the drug and a pharmaceutically acceptable excipient coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the drug is selected from the group consisting of chlordiazepoxide, betahistine, clonidine, testosterone, conjugated estrogens, estradiol, ethinyl estradiol, and hyoscyamine, and wherein the particles comprise at least 10 percent by weight of the drug and less than 5 percent by weight of the drug degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (50, 51, 71)
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52. A method of forming a drug containing aerosol comprising:
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(a) heating a composition containing a salt form of the drug coated on a solid support to form a vapor; and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the drug is selected from the group consisting of chlordiazepoxide, betahistine, clonidine, testosterone, conjugated estrogens, estradiol, ethinyl estradiol, and hyoscyamine, and wherein the particles comprise at least 10 percent by weight of the drug and less than 5 percent by weight of the drug degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (53, 54, 72)
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73. A method of forming a drug containing aerosol comprising:
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(a) heating a composition containing the drug coated on a solid support to form a vapor, and (b) condensing the vapor to form a condensation aerosol comprising particles, wherein the drug is selected from the group consisting of chlordiazepoxide, betahistine, clonidine, testosterone, conjugated estrogens, estradiol, ethinyl estradiol, and hyoscyamine, wherein the condensation aerosol is formed at a rate greater than 0.5 mg/second, and wherein the particles comprise at least 10 percent by weight of the drug and less than 5 percent by weight of the drug degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (74, 75, 76, 77)
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Specification