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Last Updated: March 28, 2024

Details for Patent: 7,018,620


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Title:Delivery of beta-blockers through an inhalation route
Abstract: The present invention relates to the delivery of atenolol, pindolol, esmolol, propranolol, or metoprolol through an inhalation route. Specifically, it relates to aerosols containing atenolol, pindolol, esmolol, propranolol, or metoprolol that are used in inhalation therapy. In a method aspect of the present invention, atenolol, pindolol, esmolol, propranolol, or metoprolol is administered to a patient through an inhalation route. The method comprises: a) heating a composition of atenolol, pindolol, esmolol, propranolol, or metoprolol, to form a vapor; and, b) allowing the vapor to cool, thereby forming a condensation aerosol comprising particles with less than 5% drug degradation products. In a kit aspect of the present invention, a kit for delivering 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.
Inventor(s): Rabinowitz; Joshua D. (Mountain View, CA), Zaffaroni; Alejandro C. (Atherton, CA)
Assignee: Alexza Pharmaceuticals, Inc. (Palo Alto, CA)
Filing Date:Feb 09, 2004
Application Number:10/775,583
Claims:1. A method of treating hypertension, acute myocardial infarction, cardiac arrhythmias or side effects of situational anxiety in a patient comprising administering a therapeutic amount of a drug condensation aerosol to the patient by inhalation, wherein the drug is selected from the group consisting of atenolol, pindolol, esmolol, propranolol and metoprolol, and 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.

2. The method according to claim 1, wherein the condensation aerosol is characterized by an MMAD of less than 3 microns.

3. The method according to claim 1, wherein the condensation aerosol is formed at a rate greater than 0.5 mg/second.

4. The method according to claim 1, wherein the therapeutic amount of a drug condensation aerosol comprises between 0.1 mg and 20 mg of atenolol delivered in a single inspiration.

5. The method according to claim 1, wherein the therapeutic amount of a drug condensation aerosol comprises between 0.1 mg and 20 mg of pindolol delivered in a single inspiration.

6. The method according to claim 1, wherein the therapeutic amount of a drug condensation aerosol comprises between 4 mg and 100 mg of esmolol delivered in a single inspiration.

7. The method according to claim 1, wherein the therapeutic amount of a drug condensation aerosol comprises between 0.2 mg and 50 mg of propranolol delivered in a single inspiration.

8. The method according to claim 1, wherein the therapeutic amount of a drug condensation aerosol comprises between 1 mg and 30 mg of metoprolol delivered in a single inspiration.

9. The method according to claim 1, wherein peak plasma drug concentration is reached in less than 0.1 hours.

10. The method according to claim 1, wherein at least 50% by weight of the condensation aerosol is amorphous in form.

11. A method of administering a drug condensation aerosol to a patient comprising administering the drug condensation aerosol to the patient by inhalation, wherein the drug is selected from the group consisting of atenolol, pindolol, esmolol, propranolol and metoprolol, and wherein the drug 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.

12. A kit for delivering a drug condensation aerosol comprising: a. a thin layer containing the drug, on a solid support, wherein the drug is selected from the group consisting of atenolol, pindolol, esmolol, propranolol and metoprolol, and b. a device for providing the condensation aerosol, wherein the condensation aerosol is formed by heating the thin layer 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.

13. The kit according to claim 12, wherein the thin layer has a thickness between 5.2 and 6.5 microns.

14. The kit according to claim 12, wherein the device comprises: a. a flow through enclosure containing the solid support, b. a power source that can be activated to heat the solid support, and c. at least one portal through which air can be drawn by inhalation, wherein activation of the power source is effective to produce a vapor of the drug, and drawing air through the enclosure is effective to condense the vapor to form the condensation aerosol.

15. The kit according to claim 14, wherein the heat for heating the solid support is generated by an exothermic chemical reaction.

16. The kit according to claim 15, wherein the exothermic chemical reaction is oxidation of combustible materials.

17. The kit according to claim 14, wherein the heat for heating the solid support is generated by passage of current through an electrical resistance element.

18. The kit according to claim 14, wherein the solid support has a surface area dimensioned to accommodate a therapeutic dose of the drug.

19. The kit according to claim 12, wherein peak plasma drug concentration is reached in less than 0.1 hours.

20. The kit according to claim 12, further including instructions for use.

21. The method according to claim 1, wherein the condensation aerosol is characterized by an MMAD of 0.1 to 5 microns.

22. The method according to claim 2, wherein the condensation aerosol is characterized by an MMAD of about 0.2 to about 3 microns.

23. The method according to claim 1, wherein the thin layer has a thickness between 5.2 and 6.5 microns.

24. The method according to claim 11, wherein the drug is atenolol.

25. The method according to claim 11, wherein the drug is pindolol.

26. The method according to claim 11, wherein the drug is esmolol.

27. The method according to claim 11, wherein the drug is propranolol.

28. The method according to claim 11, wherein the drug is metoprolol.

29. The kit according to claim 12, wherein the condensation aerosol is characterized by an MMAD of less than 3 microns.

30. The kit according to claim 12, wherein the condensation aerosol is characterized by an MMAD of 0.1 to 5 microns.

31. The kit according to claim 33, wherein the condensation aerosol is characterized by an MMAD of about 0.2 to about 3 microns.

32. The kit according to claim 12, wherein the drug is atenolol.

33. The kit according to claim 12, wherein the drug is pindolol.

34. The kit according to claim 12, wherein the drug is esmolol.

35. The kit according to claim 12, wherein the drug is propranolol.

36. The kit according to claim 12, wherein the drug is metoprolol.

37. The kit according to claim 14, wherein the solid support has a surface to mass ratio of greater than 1 cm.sup.2 per gram.

38. The kit according to claim 14, wherein the solid support has a surface to volume ratio of greater than 100 per meter.

39. The kit according to claim 14, wherein the solid support is a metal foil.

40. The kit according to claim 39, wherein the metal foil has a thickness of less than 0.25 mm.

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