Delivery of nonsteroidal antiinflammatory drugs through an inhalation route
First Claim
1. A condensation aerosol for delivery of indomethacin formed by heating a composition containing indomethacin 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 indomethacin and less than 5 percent by weight of indomethacin 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 nonsteroidal antiinflammatory drugs (NSAIDs) through an inhalation route. Specifically, it relates to aerosols containing NSAIDs that are used in inhalation therapy. In a method aspect of the present invention, an NSAID is delivered to a patient through an inhalation route. The method comprises: a) heating a coating of an NSAID, on a solid support, to form a vapor; and, b) passing air through the heated vapor to produce aerosol particle having less than 5% NSAID degradation products. In a kit aspect of the present invention, a kit for delivering an NSAID through an inhalation route is provided which comprises: a) a coating of an NSAID composition and b) a device for dispensing said coating as a condensation aerosol.
247 Citations
110 Claims
- 1. A condensation aerosol for delivery of indomethacin formed by heating a composition containing indomethacin 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 indomethacin and less than 5 percent by weight of indomethacin degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
- 4. A condensation aerosol for delivery of ketoprofen formed by heating a composition containing ketoprofen 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 ketoprofen and less than 5 percent by weight of ketoprofen degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
- 7. A condensation aerosol for delivery of celecoxib formed by heating a composition containing celecoxib 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 celecoxib and less than 5 percent by weight of celecoxib degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
- 10. A condensation aerosol for delivery of rofecoxib formed by heating a composition containing rofecoxib 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 rofecoxib and less than 5 percent by weight of rofecoxib degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
- 13. A condensation aerosol for delivery of meclofenamic acid formed by heating a composition containing meclofenamic acid 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 meclofenamic acid and less than 5 percent by weight of meclofenamic acid degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
- 16. A condensation aerosol for delivery of fenoprofen formed by heating a composition containing fenoprofen 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 fenoprofen and less than 5 percent by weight of fenoprofen degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
- 19. A condensation aerosol for delivery of diflunisal formed by heating a composition containing diflunisal 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 diflunisal and less than 5 percent by weight of diflunisal degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
- 22. A condensation aerosol for delivery of naproxen formed by heating a composition containing naproxen 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 naproxen and less than 5 percent by weight of naproxen degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
- 25. A condensation aerosol for delivery of ibuprofen formed by heating a composition containing ibuprofen 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 ibuprofen and less than 5 percent by weight of ibuprofen degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
- 28. A condensation aerosol for delivery of flurbiprofen formed by heating a composition containing flurbiprofen 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 flurbiprofen and less than 5 percent by weight of flurbiprofen degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
- 31. A condensation aerosol for delivery of nabumetone formed by heating a composition containing nabumetone 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 nabumetone and less than 5 percent by weight of nabumetone degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
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34. A method of forming an indomethacin containing aerosol comprising:
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(a) heating a composition containing indomethacin 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 indomethacin degradation products and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (35, 36, 91)
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37. A method of forming a ketoprofen containing aerosol comprising:
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(a) heating acomposition containing ketoprofen 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 ketoprofen degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (38, 39, 92)
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40. A method of forming a celecoxib containing aerosol comprising:
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(a) heating a composition containing celecoxib 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 os celecoxib degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (41, 42, 93)
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43. A method of forming a rofecoxib containing aerosol comprising:
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(a) heating a composition containing rofecoxib 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 rofecoxib degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (44, 45, 94)
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46. A method of forming a meclofenamic acid containing aerosol comprising:
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(a) heating a composition containing meclofenamic acid 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 meclofenamic acid degradation Products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (47, 48, 95)
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49. A method of forming a fenoprofen containing aerosol comprising:
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(a) heating a compostion containing fenoprofen 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 fenoprofen degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (50, 51, 96)
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52. A method of forming a diflunisal containing aerosol comprising:
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(a) heating a composition containing diflunisal 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 diflunisal degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (53, 54, 97)
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55. A method of forming a naproxen containing aerosol comprising:
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(a) heating a composition containing naproxen 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 naproxen of degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (56, 57, 98)
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58. A method of forming an ibuprofen containing aerosol comprising:
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(a) heating a composition containing ibuprofen 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 ibuprofen degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (59, 60, 99)
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61. A method of forming a flurbiprofen containing aerosol comprising:
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(a) heating a composition containing flurbiprofen 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 flurbiprofen degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (62, 63, 100)
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64. A method of forming a nabumetone containing aerosol comprising:
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(a) heating a composition containing nabumetone coated on a solid support to form a vapor; and (b) condensing the vapor to produce a condensation aerosol comprising particles, wherein the particles comprise less than 5 percent by weight of nabumetone degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (65, 66, 101)
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67. A method of forming a tolfenamic acid containing aerosol comprising:
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(a) heating a composition containing tolfenamic acid 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 tolfenamic acid degradation products, and the condensation aerosol has an MMAD of less than 5 microns. - View Dependent Claims (68, 69, 102)
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70. 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 indomethacin, ketoprofen, celecoxib, rofecoxib, meclofenamic acid, fenoprofen, diflunisal, tolfenamic acid, naproxen, ibuprofen, flurbiprofen, and nabumetone, 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 (71, 72, 103)
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73. 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 indomethacin, ketoprofen, celecoxib, rofecoxib, meclofenamic acid, fenoprofen, diflunisal, tolfenamic acid, naproxen, ibuprofen, flurbiprofen, and nabumetone, 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, 104)
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- 76. A condensation aerosol for delivery of tolfenamic acid formed by heating a composition containing tolfenamic acid 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 tolfenamic acid and less than 5 percent by weight of tolfenamic acid degradation products, and the condensation aerosol has an MMAD of less than 5 microns.
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105. 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 indomethacin, ketoprofen, celecoxib, rofecoxib, meclofenamic acid, fenoprofen, diflunisal, tolfenamic acid, naproxen, ibuprofen, flurbiprofen, and nabumetone, 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 (106, 107, 108, 109, 110)
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Specification