Delivery of physiologically active compounds 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-0769051
(2004-01-30)
발명자
/ 주소
Rabinowitz,Joshua D.
Zaffaroni,Alejandro C.
출원인 / 주소
Alexza Pharmaceuticals, Inc.
대리인 / 주소
Swanson &
인용정보
피인용 횟수 :
48인용 특허 :
94
초록▼
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 activ
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.
대표청구항▼
What is claimed is: 1. A condensation aerosol for delivery of a drug selected from the group consisting of chlordiazepoxide, betahistine, clonidine, testosterone, a conjugated estrogen, an estrogen ester, estradiol, an estradiol ester, ethinyl estradiol, an ethinyl estradiol ester and hyoscyamine,
What is claimed is: 1. A condensation aerosol for delivery of a drug selected from the group consisting of chlordiazepoxide, betahistine, clonidine, testosterone, a conjugated estrogen, an estrogen ester, estradiol, an estradiol ester, ethinyl estradiol, an ethinyl estradiol ester and hyoscyamine, 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 condensation aerosol according to claim 1, wherein the condensation aerosol is formed at a rate greater than 109 particles per second. 3. The condensation aerosol according to claim 2, wherein the condensation aerosol is formed at a rate greater than 1010 particles per second. 4. A method of producing a drug selected from the group consisting of chlordiazepoxide, betahistine, clonidine, testosterone, a conjugated estrogen, an estrogen ester, estradiol, an estradiol ester, ethinyl estradiol, an ethinyl estradiol ester and hyoscyamine in an aerosol form comprising: a. heating a thin layer containing the drug, on a solid support, to produce a vapor of the drug, and b. providing an air flow through 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. 5. The method according to claim 4, wherein the condensation aerosol is formed at a rate greater than 109 particles per second. 6. The method according to claim 5, wherein the condensation aerosol is formed at a rate greater than 1010 particles per second. 7. The condensation aerosol according to claim 1, wherein the condensation aerosol is characterized by an MMAD of 0.1 to 5 microns. 8. The condensation aerosol according to claim 1, wherein the condensation aerosol is characterized by an MMAD of less than 3 microns. 9. The condensation aerosol according to claim 1, wherein the condensation aerosol is characterized by an MMAD of about 0.2 to about 3 microns. 10. The condensation aerosol according to claim 1, wherein the condensation aerosol is characterized by less than 5% drug degradation products by weight. 11. The condensation aerosol according to claim 1, wherein the condensation aerosol is characterized by less than 2.5% drug degradation products by weight. 12. The condensation aerosol according to claim 1, wherein the solid support is a metal foil. 13. The condensation aerosol according to claim 1, wherein the drug is chlordiazepoxide. 14. The condensation aerosol according to claim 1, wherein the drug is betahistine. 15. The condensation aerosol according to claim 1, wherein the drug is clonidine. 16. The condensation aerosol according to claim 1, wherein the drug is testosterone. 17. The condensation aerosol according to claim 1, wherein the drug is a conjugated estrogen. 18. The condensation aerosol according to claim 1, wherein the drug is an estrogen ester. 19. The condensation aerosol according to claim 1, wherein the drug is estradiol. 20. The condensation aerosol according to claim 1, wherein the drug is an estradiol ester. 21. The condensation aerosol according to claim 1, wherein the drug is ethinyl estradiol. 22. The condensation aerosol according to claim 1, wherein the drug is an ethinyl estradiol ester. 23. The condensation aerosol according to claim 1, wherein the drug is hyoscyamine. 24. The method according to claim 4, wherein the condensation aerosol is characterized by an MMAD of 0.1 to 5 microns. 25. The method according to claim 4, wherein the condensation aerosol is characterized by an MMAD of less than 3 microns. 26. The method according to claim 4, wherein the condensation aerosol is characterized by an MMAD of about 0.2 to 3 microns. 27. The method according to claim 4, wherein the condensation aerosol is characterized by less than 5% drug degradation products by weight. 28. The method according to claim 27, wherein the condensation aerosol is characterized by less than 2.5% drug degradation products by weight. 29. The method according to claim 4, wherein the solid support is a metal foil. 30. The method according to claim 4, wherein the drug is chlordiazepoxide. 31. The method according to claim 4, wherein the drug is betahistine. 32. The method according to claim 4, wherein the drug is clonidine. 33. The method according to claim 4, wherein the drug is testosterone. 34. The method according to claim 4, wherein the drug is a conjugated estrogen. 35. The method according to claim 4, wherein the drug is an estrogen ester. 36. The method according to claim 4, wherein the drug is estradiol. 37. The method according to claim 4, wherein the drug is an estradiol ester. 38. The method according to claim 4, wherein the drug is ethinyl estradiol. 39. The method according to claim 4, wherein the drug is an ethinyl estradiol ester. 40. The method according to claim 4, wherein the drug is hyoscyamine. 41. A condensation aerosol for delivery of chlordiazepoxide, wherein the condensation aerosol is formed by heating a thin layer containing chlordiazepoxide, on a solid support, to produce a vapor of chlordiazepoxide, and condensing the vapor to form a condensation aerosol characterized by less than 5% chlordiazepoxide degradation products by weight, and an MMAD of about 0.2 to 3 microns. 42. A condensation aerosol for delivery of betahistine, wherein the condensation aerosol is formed by heating a thin layer containing betahistine, on a solid support, to produce a vapor of betahistine, and condensing the vapor to form a condensation aerosol characterized by less than 5% betahistine degradation products by weight, and an MMAD of about 0.2 to 3 microns. 43. A condensation aerosol for delivery of clonidine, wherein the condensation aerosol is formed by heating a thin layer containing clonidine, on a solid support, to produce a vapor of clonidine, and condensing the vapor to form a condensation aerosol characterized by less than 5% clonidine degradation products by weight, and an MMAD of about 0. 2 to 3 microns. 44. A condensation aerosol for delivery of testosterone, wherein the condensation aerosol is formed by heating a thin layer containing testosterone, on a solid support, to produce a vapor of testosterone, and condensing the vapor to form a condensation aerosol characterized by less than 5% testosterone degradation products by weight, and an MMAD of about 0.2 to 3 microns. 45. A condensation aerosol for delivery of a conjugated estrogen, wherein the condensation aerosol is formed by heating a thin layer containing the conjugated estrogen, on a solid support, to produce a vapor of the conjugated estrogen, and condensing the vapor to form a condensation aerosol characterized by less than 5% conjugated estrogen degradation products by weight, and an MMAD of about 0.2 to 3 microns. 46. A condensation aerosol for delivery of an estrogen ester, wherein the condensation aerosol is formed by heating a thin layer containing the estrogen ester, on a solid support, to produce a vapor of the estrogen ester, and condensing the vapor to form a condensation aerosol characterized by less than 5% estrogen ester degradation products by weight, and an MMAD of about 0.2 to 3 microns. 47. A condensation aerosol for delivery of estradiol, wherein the condensation aerosol is formed by heating a thin layer containing estradiol, on a solid support, to produce a vapor of estradiol, and condensing the vapor to form a condensation aerosol characterized by less than 5% estradiol degradation products by weight, and an MMAD of about 0. 2 to 3 microns. 48. A condensation aerosol for delivery of an estradiol ester, wherein the condensation aerosol is formed by heating a thin layer containing the estradiol ester, on a solid support, to produce a vapor of the estradiol ester, and condensing the vapor to form a condensation aerosol characterized by less than 5% estradiol ester degradation products by weight, and an MMAD of about 0.2 to 3 microns. 49. A condensation aerosol for delivery of ethinyl estradiol, wherein the condensation aerosol is formed by heating a thin layer containing ethinyl estradiol, on a solid support, to produce a vapor of ethinyl estradiol, and condensing the vapor to form a condensation aerosol characterized by less than 5% ethinyl estradiol degradation products by weight, and an MMAD of about 0.2 to 3 microns. 50. A condensation aerosol for delivery of an ethinyl estradiol ester, wherein the condensation aerosol is formed by heating a thin layer containing the ethinyl estradiol ester, on a solid support, to produce a vapor of the ethinyl estradiol ester, and condensing the vapor to form a condensation aerosol characterized by less than 5% ethinyl estradiol ester degradation products by weight, and an MMAD of about 0.2 to 3 microns. 51. A condensation aerosol for delivery of hyoscyamine, wherein the condensation aerosol is formed by heating a thin layer containing hyoscyamine, on a solid support, to produce a vapor of hyoscyamine, and condensing the vapor to form a condensation aerosol characterized by less than 5% hyoscyamine degradation products by weight, and an MMAD of about 0.2 to 3 microns. 52. A method of producing chlordiazepoxide in an aerosol form comprising: a. heating a thin layer containing chlordiazepoxide, on a solid support, to produce a vapor of chlordiazepoxide, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% chlordiazepoxide degradation products by weight, and an MMAD of about 0.2 to 3 microns. 53. A method of producing betahistine in an aerosol form comprising: a. heating a thin layer containing betahistine, on a solid support, to produce a vapor of betahistine, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% betahistine degradation products by weight, and an MMAD of about 0.2 to 3 microns. 54. A method of producing clonidine in an aerosol form comprising: a. heating a thin layer containing clonidine, on a solid support, to produce a vapor of clonidine, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% clonidine degradation products by weight, and an MMAD of about 0.2 to 3 microns. 55. A method of producing testosterone in an aerosol form comprising: a. heating a thin layer containing testosterone, on a solid support, to produce a vapor of testosterone, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% testosterone degradation products by weight, and an MMAD of about 0.2 to 3 microns. 56. A method of producing a conjugated estrogen in an aerosol form comprising: a. heating a thin layer containing the conjugated estrogen, on a solid support, to produce a vapor of the conjugated estrogen, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% conjugated estrogen degradation products by weight, and an MMAD of about 0.2 to 3 microns. 57. A method of producing an estrogen ester in an aerosol form comprising: a. heating a thin layer containing the estrogen ester, on a solid support, to produce a vapor of the estrogen ester, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% estrogen ester degradation products by weight, and an MMAD of about 0.2 to 3 microns. 58. A method of producing estradiol in an aerosol form comprising: a. heating a thin layer containing estradiol, on a solid support, to produce a vapor of estradiol, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% estradiol degradation products by weight, and an MMAD of about 0.2 to 3 microns. 59. A method of producing an estradiol ester in an aerosol form comprising: a. heating a thin layer containing the estradiol ester, on a solid support, to produce a vapor of the estradiol ester, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% estradiol ester degradation products by weight, and an MMAD of about 0.2 to 3 microns. 60. A method of producing ethinyl estradiol in an aerosol form comprising: a. heating a thin layer containing ethinyl estradiol, on a solid support, to produce a vapor of ethinyl estradiol, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% ethinyl estradiol degradation products by weight, and an MMAD of about 0.2 to 3 microns. 61. A method of producing an ethinyl estradiol ester in an aerosol form comprising: a. heating a thin layer containing the ethinyl estradiol ester, on a solid support, to produce a vapor of the ethinyl estradiol ester, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% ethinyl estradiol ester degradation products by weight, and an MMAD of about 0.2 to 3 microns. 62. A method of producing hyoscyamine in an aerosol form comprising: a. heating a thin layer containing hyoscyamine, on a solid support, to produce a vapor of hyoscyamine, and b. providing an air flow through the vapor to form a condensation aerosol characterized by less than 5% hyoscyamine degradation products by weight, and an MMAD of about 0.2 to 3 microns.
연구과제 타임라인
LOADING...
LOADING...
LOADING...
LOADING...
LOADING...
이 특허에 인용된 특허 (94)
Sands George H., 5HT 1 receptor agonists and metoclopramide for the treatment of migraine.
Edwards David A. ; Caponetti Giovanni,ITX ; Hrkach Jeffrey S. ; Lotan Noah,ILX ; Hanes Justin ; Ben-Jebria Abdell Aziz ; Langer Robert S., Aerodynamically light particles for pulmonary drug delivery.
Clearman Jack F. (Blakely GA) Chiou Joseph J. (Clemmons NC) Williams Darrell D. (Winston-Salem NC) Casey William J. (Clemmons NC) Gentry Thomas L. (Winston-Salem NC) Squires William C. (Winston-Salem, Aerosol delivery article.
Roberts Donald L. (Winston-Salem NC) Morrison Carl C. (Winston-Salem NC) Brooks Johnny L. (Winston-Salem NC) Crooks Evon L. (Winston-Salem NC) Ingebrethsen Bradley J. (Winston-Salem NC), Aerosol delivery article.
Horvath, Raymond F.; Tran, Jennifer; De Lombaert, Stephane; Hodgetts, Kevin J.; Carpino, Philip A.; Griffith, David A., Certain alkylene diamine-substituted heterocycles.
Reed Barry Leonard,AUX ; Morgan Timothy Matthias,AUX ; Finnin Barrie Charles,AUX, Dermal penetration enhancers and drug delivery systems involving same.
Potter Dennis L. (Kernersville NC) Raker Mark L. (Clemmons NC) Ridings Henry T. (Lewisville NC) Sensabaugh ; Jr. Andrew J. (Winston-Salem NC) Westmoreland Amos E. (Winston-Salem NC) Woods Donna K. (W, Drug delivery article.
Brooks Johnny L. (Winston-Salem NC) Roberts Donald L. (Winston-Salem NC) Simmons Jerry S. (Rural Hall NC), Drug delivery articles utilizing electrical energy.
Hodson Peter David (Trowell Park GB3) Smith David Keith (Loughborough GB3) Wass Anthony Charles Lammond (Duddington GB3), Dry powder inhalation device having deagglomeration/aerosolization structure responsive to patient inhalation.
Sprinkel F. Murphy (Glen Allen VA) Das Amitabh (Midlothian VA) Fleischhauer Grier S. (Midlothian VA) Grollimund Everett C. (Midlothian VA) Houck ; Jr. Willie G. (Richmond VA) Lipowicz Peter J. (Midlo, Electrical lighter with a rotatable tobacco supply.
Higgins Charles T. (Richmond VA) Raymond Wynn R. (Chesterfield VA) Sprinkel Francis M. (Glen Allen VA), Electrical smoking article using liquid tobacco flavor medium delivery system.
Brooks Johnny L. (Winston-Salem NC) Roberts Donald L. (Winston-Salem NC) Simmons Jerry S. (Rural Hall NC), Flavor delivery articles utilizing electrical energy.
Counts Mary E. (Richmond VA) LaRoy Bernard C. (Richmond VA) Losee ; Jr. D. Bruce (Richmond VA) Morgan Constance H. (Midlothian VA) Smith Ulysses (Midlothian VA) Sprinkel ; Jr. F. Murphy (Glen Allen V, Flavor generating article.
Counts Mary E. (Richmond VA) Hajaligol Mohammad R. (Richmond VA) Morgan Constance H. (Midlothian VA) Smith Ulysses (Midlothian VA) Sprinkel Francis M. (Glen Allen VA) Utsch Francis V. (Midlothian VA), Flavor-delivery article.
Weers Jeffry G. ; Dellamary Luis A. ; Tarara Thomas E. ; Trevino Leo A. ; Ranney Helen M., Fluorochemical solutions for the delivery of lipophilic pharmaceutical agents.
Rubsamen Reid M. (Berkeley CA) Lloyd Lester J. (Orinda CA) Johansson Eric T. (Dublin CA), Lockout device for controlled release of drug from patient-activated dispenser.
Clearman Jack F. (Blakely GA) Furin Olivia P. (Clemmons NC) Chiou Joseph J. (Clemmons NC) Squires William C. (Winston-Salem NC), Low CO smoking article.
Radhakrishnan Ramachandran (Fremont CA) Mihalko Paul J. (Fremont CA) Abra Robert M. (San Francisco CA), Method and apparatus for administering dehydrated liposomes by inhalation.
Banerjee Chandra K. (Pfafftown NC) Farrier Ernest G. (Winston-Salem NC) Ridings Henry T. (Lewisville NC) Sensabaugh ; Jr. Andrew J. (Winston-Salem NC) Shannon Michael D. (Lewisville NC) Shelar Gary R, Method for making aerosol generating cartridge.
Olsson Sven-Gunnar,SEX ; Rydgren Goran,SEX ; Larsson Anders,SEX ; Niininen Tarmo,SEX, Method for vaporizing an anesthetic liquid and vaporizer operating according to the method.
Banerjee Chandra K. (1 Pfafftown NC) Farrier Ernest G. (1 Winston-Salem NC) Reynolds ; IV John H. (1 Winston-Salem NC) Ridings Henry T. (Lewisville NC) Sensabaugh ; Jr. Andrew J. (Winston-Salem NC) S, Smoking article.
Banerjee Chandra K. (Pfafftown NC) Farrier Ernest G. (Winston-Salem NC) Harris James L. (Westfield NC) Norman Alan B. (Clemmons NC) Resce James L. (Yadkinville NC) Reynolds ; IV John H. (Winston-Sale, Smoking article.
Serrano Mark A. (Greenwich CT) Houghton Kenneth S. (Midlothian VA) Lanzillotti Harry V. (Midlothian VA) Sanders Edward B. (Richmond VA) Lilly ; Jr. A. Clifton (Chesterfield VA) Hayward Charles R. (Mi, Smoking article.
Clearman Jack F. (Blakely GA) Resce James L. (Yadkinville NC) Farrier Ernest G. (Winston-Salem NC) Norman Alan B. (Clemmons NC) Furin Olivia P. (Clemmons NC) Squires William C. (Winston-Salem NC), Smoking article with improved fuel element.
Brooks Johnny L. (Winston-Salem NC) Roberts Donald L. (Winston-Salem NC) Simmons Jerry S. (Rural Hall NC), Smoking articles utilizing electrical energy.
Sutton Andrew D.,GBX ; Johnson Richard A.,GBX ; Senior Peter J.,GBX ; Heath David,GBX, Spray-dried microparticles and their use as therapeutic vehicles.
Lloyd Lester J. (Orinda CA) Lloyd Peter M. (Oakland CA) Rubsamen Reid M. (Berkeley CA) Schuster Jeffrey A. (Berkeley CA), Systems for the intrapulmonary delivery of aerosolized aqueous formulations.
Hale, Ron L.; Lei, Mingzu; Lloyd, Peter M.; Munzar, Patrik; Sharma, Krishnamohan; Solas, Dennis W.; Stracker, Matthew D., Aerosol drug delivery device incorporating percussively activated heat packages.
Hale,Ron L.; Rabinowitz,Joshua D.; Solas,Dennis W.; Zaffaroni,Alejandro C., Delivery of compounds for the treatment of headache through an inhalation route.
Hale, Ron L.; Hodges, Craig C.; Lloyd, Peter M.; Lu, Amy T.; Myers, Daniel J.; Rabinowitz, Joshua D.; Wensley, Martin J.; McKinney, Jeffrey A.; Zaffaroni, Alejandro C., Drug condensation aerosols and kits.
Hale, Ron L.; Hodges, Craig C.; Lloyd, Peter M.; Lu, Amy T.; Myers, Daniel J.; Rabinowitz, Joshua D.; Wensley, Martin J.; McKinney, Jeffrey A.; Zaffaroni, Alejandro C., Drug condensation aerosols and kits.
Hale, Ron L.; Hodges, Craig C.; Lloyd, Peter M.; Lu, Amy T.; Myers, Daniel J.; Rabinowitz, Joshua D.; Wensley, Martin J.; McKinney, Jeffrey A.; Zaffaroni, Alejandro C., Drug condensation aerosols and kits.
Hale, Ron L.; Hodges, Craig C.; Lloyd, Peter M.; Mufson, Daniel; Rogers, Daniel D.; Song, Soonho; Wensley, Martin J.; Myers, Daniel J.; McKinney, Jeffrey A.; Quintana, Reynaldo J.; Rabinowitz, Joshua D., Method of forming an aerosol for inhalation delivery.
Hale, Ron L.; Hodges, Craig C.; Lloyd, Peter M.; Mufson, Daniel; Rogers, Daniel D.; Song, Soonho; Wensley, Martin J.; Myers, Daniel J.; McKinney, Jeffrey A.; Quintana, Reynaldo J.; Rabinowitz, Joshua D., Method of forming an aerosol for inhalation delivery.
Hale, Ron L.; Hodges, Craig C.; Lloyd, Peter M.; Mufson, Daniel; Rogers, Daniel D.; Song, Soonho; Wensley, Martin J.; Myers, Daniel J.; McKinney, Jeffrey A.; Quintana, Reynaldo J.; Rabinowitz, Joshua D., Method of forming an aerosol for inhalation delivery.
Hale, Ron L.; Hodges, Craig C.; Lloyd, Peter M.; Mufson, Daniel; Rogers, Daniel D.; Song, Soonho; Wensley, Martin J.; Myers, Daniel J.; McKinney, Jeffrey A.; Quintana, Reynaldo J.; Rabinowitz, Joshua D., Method of forming an aerosol for inhalation delivery.
Cross, Stephen D.; Herbette, Mathieu; Kelly, Andrew J. G.; Myers, Daniel J.; Shen, William W.; Timmons, Ryan D.; Tom, Curtis; Virgili, Justin M.; Wensley, Martin J., Multiple dose condensation aerosol devices and methods of forming condensation aerosols.
Cross, Steven D.; Herbette, Mathieu; Kelly, Andrew J. G.; Myers, Daniel J.; Shen, William W.; Timmons, Ryan D.; Tom, Curtis; Virgili, Justin M.; Wensley, Martin J., Multiple dose condensation aerosol devices and methods of forming condensation aerosols.
Hale, Ron L.; Lloyd, Peter M.; Lu, Amy T.; Rabinowitz, Joshua D.; Wensley, Martin J., Respiratory drug condensation aerosols and methods of making and using them.
Damani, Ramesh; Hale, Ron L.; Myers, Daniel J.; Quintana, Reynaldo J.; Solas, Dennis W.; Song, Soonho; Soni, Pravin; Tom, Curtis; Sharma, Kirshnamohan, Self-contained heating unit and drug-supply unit employing same.
Damani, Ramesh; Hale, Ron L.; Myers, Daniel J.; Quintana, Reynaldo J.; Solas, Dennis W.; Song, Soonho; Soni, Pravin; Tom, Curtis; Sharma, Krishnamohan, Self-contained heating unit and drug-supply unit employing same.
Damani, Ramesh; Hale, Ron L.; Myers, Daniel J.; Quintana, Reynaldo J.; Solas, Dennis W.; Song, Soonho; Soni, Pravin; Tom, Curtis; Sharma, Krishnamohan, Self-contained heating unit and drug-supply unit employing same.
※ AI-Helper는 부적절한 답변을 할 수 있습니다.