Delivery of antipsychotics through an inhalation route
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-009/12
A61K-009/14
A61M-015/00
출원번호
US-0750303
(2003-12-30)
발명자
/ 주소
Rabinowitz,Joshua D.
Zaffaroni,Alejandro C.
출원인 / 주소
Alexza Pharmaceuticals, Inc.
대리인 / 주소
Swanson &
인용정보
피인용 횟수 :
51인용 특허 :
79
초록▼
The present invention relates to the delivery of antipsychotics through an inhalation route. Specifically, it relates to aerosols containing antipsychotics that are used in inhalation therapy. In a method aspect of the present invention, an antipsychotic is delivered to a patient through an inhalat
The present invention relates to the delivery of antipsychotics through an inhalation route. Specifically, it relates to aerosols containing antipsychotics that are used in inhalation therapy. In a method aspect of the present invention, an antipsychotic is delivered to a patient through an inhalation route. The method comprises: a) heating a composition, wherein the composition comprises an antipsychotic, to form a vapor; and, b) allowing the vapor to cool, thereby forming a condensation aerosol comprising particles with less than 5% antipsychotic drug degradation products. In a kit aspect of the present invention, a kit for delivering an antipsychotic through an inhalation route is provided which comprises: a) a thin coating of an antipsychotic composition and b) a device for dispensing said thin coating as a condensation aerosol.
대표청구항▼
What is claimed is: 1. A method of treating psychosis 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 olanzapine, trifluoperazine, haloperidol, loxapine, risperidone, cl
What is claimed is: 1. A method of treating psychosis 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 olanzapine, trifluoperazine, haloperidol, loxapine, risperidone, clozapine, quetiapine, promazine, thiothixene, chlorpromazine, droperidol, prochlorperazine and fluphenazine, 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 peak plasma drug concentration is reached in less than 0.1 hours. 4. The method according to claim 1, wherein the condensation aerosol is formed at a rate greater than 0.5 mg/second. 5. The method according to claim 1, wherein at least 50% by weight of the condensation aerosol is amorphous in form. 6. The method according to claim 1, wherein the therapeutic amount of a drug condensation aerosol comprises between 0.2 mg and 20 mg of olanzapine 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 10 mg of trifluoperazine delivered in a single inspiration. 8. The method according to claim 1, wherein the therapeutic amount of a drug condensation aerosol comprises between 0.2 mg and 10 mg of haloperidol delivered in a single inspiration. 9. The method according to claim 1, wherein the therapeutic amount of a drug condensation aerosol comprises between 2 mg and 100 mg of loxapine delivered in a single inspiration. 10. The method according to claim 1, wherein the therapeutic amount of a drug condensation aerosol comprises between 0.1 mg and 5 mg of risperidone delivered in a single inspiration. 11. The method according to claim 1, wherein the therapeutic amount of a drug condensation aerosol comprises between 2 mg and 200 mg of clozapine delivered in a single inspiration. 12. The method according to claim 1, wherein the therapeutic amount of a drug condensation aerosol comprises between 2 mg and 200 mg of quetiapine delivered in a single inspiration. 13. The method according to claim 1, wherein the therapeutic amount of a drug condensation aerosol comprises between 2 mg and 200 mg of promazine delivered in a single inspiration. 14. The method according to claim 1, wherein the therapeutic amount of a drug condensation aerosol comprises between 0.5 mg and 20 mg of thiothixene delivered in a single inspiration. 15. The method according to claim 1, wherein the therapeutic amount of a drug condensation aerosol comprises between 2 mg and 200 mg of chlorpromazine delivered in a single inspiration. 16. The method according to claim 1, wherein the therapeutic amount of a drug condensation aerosol comprises between 0.2 mg and 20 mg of droperidol delivered in a single inspiration. 17. The method according to claim 1, wherein the therapeutic amount of a drug condensation aerosol comprises between 0.5 mg and 20 mg of prochlorperazine delivered in a single inspiration. 18. The method according to claim 1, wherein the therapeutic amount of a drug condensation aerosol comprises between 0.1 mg and 10 mg of fluphenazine delivered in a signal inspiration. 19. A method of administering a drug condensation aerosol to a patient comprising administering the condensation aerosol to the patient by inhalation, wherein the drug is selected from the group consisting of olanzapine, trifluoperazine, haloperidol, loxapine, risperidone, clozapine, quetiapine, promazine, thiothixene, chlorpromazine, droperidol, prochlorperazine and fluphenazine, 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. 20. A kit for delivering a drug condensation aerosol comprising: a. thin layer containing the drug, on a solid support, wherein the drug is selected from the group consisting of olanzapine, trifluoperazine, haloperidol, loxapine, risperidone, clozapine, quetiapine, promazine, thiothixene, chlorpromazine, droperidol, prochlorperazine and fluphenazine, 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. 21. The kit according to claim 20, 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 though the enclosure is effective to condense the vapor to form the condensation aerosol. 22. The kit according to claim 21, wherein the heat for heating the solid support is generated by an exothermic chemical reaction. 23. The kit according to claim 22, wherein the exothermic chemical reaction is oxidation of combustible materials. 24. The kit according to claim 21, wherein the heat for heating the solid support is generated by passage of current through an electrical resistance element. 25. The kit according to claim 21, wherein the solid support has a surface area dimensioned to accommodate a therapeutic dose of the drug. 26. The kit according to claim 20, wherein peak plasma drug concentration is reached in less than 0.1 hours. 27. The kit according to claim 20, further including instructions for use. 28. The method according to claim 1, wherein the condensation aerosol is characterized by an MMAD of 0.1 to 5 microns. 29. The method according to claim 2, wherein the condensation aerosol is characterized by an MMAD of about 0.2 to about 3 microns. 30. The method according to claim 19, wherein the drug is olanzapine. 31. The method according to claim 19, wherein the drug is trifluoperazine. 32. The method according to claim 19, wherein the drug is haloperidol. 33. The method according to claim 19, wherein the drug is loxapine. 34. The method according to claim 19, wherein the drug is risperidone. 35. The method according to claim 19, wherein the drug is clozapine. 36. The method according to claim 19, wherein the drug is quetiapine. 37. The method according to claim 19, wherein the drug is promazine. 38. The method according to claim 19, wherein the drug is thiothixene. 39. The method according to claim 19, wherein the drug is chlorpromazine. 40. The method according to claim 19, wherein the drug is droperidol. 41. The method according to claim 19, wherein the drug is prochlorperazine. 42. The method according to claim 19, wherein the drug is fluphenazine. 43. The kit according to claim 20, wherein the condensation aerosol is characterized by an MMAD of less than 3 microns. 44. The kit according to claim 20, wherein the condensation aerosol is characterized by an MMAD of 0.1 to 5 microns. 45. The kit according to claim 43, wherein the condensation aerosol is characterized by an MMAD of about 0.2 to about 3 microns. 46. The kit according to claim 20, wherein the drug is olanzapine. 47. The kit according to claim 20, wherein the drug is trifluoperazine. 48. The kit according to claim 20, wherein the drug is haloperidol. 49. The kit according to claim 20, wherein the drug is loxapine. 50. The kit according to claim 20, wherein the drug is risperidone. 51. The kit according to claim 20, wherein the drug is clozapine. 52. The kit according to claim 20, wherein the drug is quetiapine. 53. The kit according to claim 20, wherein the drug is promazine. 54. The kit according to claim 20, wherein the drug is thiothixene. 55. The kit according to claim 20, wherein the drug is chlorpromazine. 56. The kit according to claim 20, wherein the drug is droperidol. 57. The kit according to claim 20, wherein the drug is prochlorperazine. 58. The kit according to claim 20, wherein the drug is fluphenazine. 59. The kit according to claim 21, wherein the solid support has a surface to mass ratio of greater than 1 cm2 per gram. 60. The kit according to claim 21, wherein the solid support has a surface to volume ratio of greater than 100 per meter. 61. The kit according to claim 21, wherein the solid support is a metal foil. 62. The kit according to claim 61, wherein the metal foil has a thickness of less than 0.25 mm.
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