Delivery of Beta-Blockers Through An Inhalation Route
First Claim
1. A composition for delivery of atenolol consisting of a condensation aerosol a) formed by volatilizing a thin layer of atenolol on a solid support, having the surface texture of a metal foil, to a temperature sufficient to produce a heated vapor of atenolol and condensing the heated vapor of atenolol to form condensation aerosol particles, b) wherein said condensation aerosol particles are characterized by less than 5% atenolol degradation products, and c) the condensation aerosol has an MMAD of less than 3 microns.
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Abstract
The present invention relates to aerosols containing of atenolol, pindolol, esmolol, propranolol, or metoprolol that are used in inhalation therapy. In a method aspect of the present invention, of atenolol, pindolol, esmolol, propranolol, or metoprolol is administered to a patient through an inhalation route. The method comprises: a) heating a thin layer of atenolol, pindolol, esmolol, propranolol, or metoprolol, on a solid support to form a vapor; and, b) passing air through the heated vapor to produce aerosol particles having less than 5% drug degradation products. In a kit aspect of the present invention, a kit for delivering of atenolol, pindolol, esmolol, propranolol, or metoprolol through an inhalation route is provided which comprises: a) a thin coating of an atenolol, pindolol, esmolol, propranolol, or metoprolol composition and b) a device for dispensing said thin coating as a condensation aerosol.
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Citations
30 Claims
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1. A composition for delivery of atenolol consisting of a condensation aerosol
a) formed by volatilizing a thin layer of atenolol on a solid support, having the surface texture of a metal foil, to a temperature sufficient to produce a heated vapor of atenolol and condensing the heated vapor of atenolol to form condensation aerosol particles, b) wherein said condensation aerosol particles are characterized by less than 5% atenolol degradation products, and c) the condensation aerosol has an MMAD of less than 3 microns.
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4. A composition for delivery of pindolol consisting of a condensation aerosol a) formed by volatilizing a thin layer of pindolol on a solid support, having the surface texture of a metal foil, to a temperature sufficient to produce a heated vapor of pindolol and condensing the heated vapor of pindolol to form condensation aerosol particles,
b) wherein said condensation aerosol particles are characterized by less than 5% pindolol degradation products, and c) the condensation aerosol has an MMAD of less than 3 microns.
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7. A composition for delivery of esmolol consisting of a condensation aerosol
a) formed by volatilizing a thin layer of esmolol on a solid support, having the surface texture of a metal foil, to a temperature sufficient to produce a heated vapor of esmolol and condensing the heated vapor of esmolol to form condensation aerosol particles, b) wherein said condensation aerosol particles are characterized by less than 5% esmolol degradation products, and c) the condensation aerosol has an MMAD of less than 3 microns.
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10. A composition for delivery of propranolol consisting of a condensation aerosol
a) formed by volatilizing a thin layer of propranolol on a solid support, having the surface texture of a metal foil, to a temperature sufficient to produce a heated vapor of propranolol and condensing the heated vapor of propranolol to form condensation aerosol particles, b) wherein said condensation aerosol particles are characterized by less than 5% propranolol degradation products, and c) the condensation aerosol has an MMAD of less than 3 microns.
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13. A composition for delivery of propranolol consisting of a condensation aerosol
a) formed by volatilizing a thin layer of propranolol on a solid support, having the surface texture of a metal foil, to a temperature sufficient to produce a heated vapor of propranolol and condensing the heated vapor of propranolol to form condensation aerosol particles, b) wherein said condensation aerosol particles are characterized by less than 5% propranolol degradation products, and c) the condensation aerosol has an MMAD of less than 3 microns.
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16. A method of producing atenolol in an aerosol form comprising:
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a. heating a thin layer of atenolol on a solid support, having the surface texture of a metal foil, to a temperature sufficient to volatilize the atenolol to form a heated vapor of the atenolol, and b. during said heating, passing air through the heated vapor to produce aerosol particles of the atenolol comprising less than 5% atenolol degradation products, and an aerosol having an MMAD of less than 3 microns.
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17. The method according to claim 17, wherein the aerosol particles are formed at a rate of greater than 109 particles per second.
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18. The method according to claim 18, wherein the aerosol particles are formed at a rate of greater than 1010 particles per second
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19. A method of producing pindolol in an aerosol form comprising:
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a. heating a thin layer of pindolol on a solid support, having the surface texture of a metal foil, to a temperature sufficient to volatilize the pindolol to form a heated vapor of the pindolol, and b. during said heating, passing air through the heated vapor to produce aerosol particles of the pindolol comprising less than 5% pindolol degradation products, and an aerosol having an MMAD of less than 3 microns.
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20. The method according to claim 20, wherein the aerosol particles are formed at a rate of greater than 109 particles per second.
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21. The method according to claim 21, wherein the aerosol particles are formed at a rate of greater than 1010 particles per second.
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22. A method of producing esmolol in an aerosol form comprising:
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a. heating a thin layer of esmolol on a solid support, having the surface texture of a metal foil, to a temperature sufficient to volatilize the esmolol to form a heated vapor of the esmolol, and b. during said heating, passing air through the heated vapor to produce aerosol particles of the esmolol comprising less than 5% esmolol degradation products, and an aerosol having an MMAD of less than 3 microns.
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23. The method according to claim 23, wherein the aerosol particles are formed at a rate of greater than 109 particles per second.
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24. The method according to claim 24, wherein the aerosol particles are formed at a rate of greater than 1010 particles per second.
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25. A method of producing propranolol in an aerosol form comprising:
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a. heating a thin layer of propranolol on a solid support, having the surface texture of a metal foil, to a temperature sufficient to volatilize the propranolol to form a heated vapor of the propranolol, and b. during said heating, passing air through the heated vapor to produce aerosol particles of the propranolol comprising less than 5% propranolol degradation products, and an aerosol having an MMAD of less than 3 microns.
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- 26. The method according to claim 26, wherein the aerosol particles are formed at a rate of greater than 109 particles per second.
- 27. The method according to claim 27, wherein the aerosol particles are formed at a rate of greater than 1010 particles per second.
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28. A method of producing metoprolol in an aerosol form comprising:
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a. heating a thin layer of metoprolol on a solid support, having the surface texture of a metal foil, to a temperature sufficient to volatilize the metoprolol to form a heated vapor of the metoprolol, and b. during said heating, passing air through the heated vapor to produce aerosol particles of the metoprolol comprising less than 5% metoprolol degradation products, and an aerosol having an MMAD of less than 3 microns.
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Specification