Delivery of alprazolam, estazolam, midazolam or triazolam through an inhalation route
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-009/12
A61K-009/14
출원번호
US-0155373
(2002-05-22)
발명자
/ 주소
Rabinowitz, Joshua D.
Zaffaroni, Alejandro C.
출원인 / 주소
Alexza Molecula Delivery Corporation
대리인 / 주소
Stracker, Elaine C.
인용정보
피인용 횟수 :
56인용 특허 :
31
초록▼
The present invention relates to the delivery of alprazolam, estazolam, midazolam or triazolam through an inhalation route. Specifically, it relates to aerosols containing alprazolam, estazolam, midazolam or triazolam that are used in inhalation therapy. In a composition aspect of the present invent
The present invention relates to the delivery of alprazolam, estazolam, midazolam or triazolam through an inhalation route. Specifically, it relates to aerosols containing alprazolam, estazolam, midazolam or triazolam that are used in inhalation therapy. In a composition aspect of the present invention, the aerosol comprises particles comprising at least 5 percent by weight of alprazolam, estazolam, midazolam or triazolam. In a method aspect of the present invention, alprazolam, estazolam, midazolam or triazolam is delivered to a mammal through an inhalation route. The method comprises: a) heating a composition, wherein the composition comprises at least 5 percent by weight of alprazolam, estazolam, midazolam or triazolam, to form a vapor; and, b) allowing the vapor to cool, thereby forming a condensation aerosol comprising particles, which is inhaled by the mammal. In a kit aspect of the present invention, a kit for delivering alprazolam, estazolam, midazolam or triazolam through an inhalation route to a mammal is provided which comprises: a) a composition comprising at least 5 percent by weight of alprazolam, estazolam, midazolam or triazolam; and, b) a device that forms an alprazolam, estazolam, midazolam or triazolam containing aerosol from the composition, for inhalation by the mammal.
대표청구항▼
1. A composition for delivery of a therapeutic compound, comprising a condensation aerosol a) formed by volatilizing a therapeutic compound selected from the group consisting of alprazolam, estazolam, midazolam or triazolam under conditions effective to produce a heated vapor of the compound, and
1. A composition for delivery of a therapeutic compound, comprising a condensation aerosol a) formed by volatilizing a therapeutic compound selected from the group consisting of alprazolam, estazolam, midazolam or triazolam under conditions effective to produce a heated vapor of the compound, and condensing the heated vapor of the compound to form condensation aerosol particles, and b) characterized by less than 5% compound degradation products, and c) aerosol MMAD is less than 3 &mgr;m. 2. The composition according to claim 1, wherein the condensation aerosol particles are characterized by less than 2.5 percent by weight of alprazolnm, estazolam, midazolam or triazolam degradation products.3. The composition according to claim 1, wherein the condensation aerosol particles comprise at least 90 percent by weight of alprazolam, estazolam, midazolam or triazolam.4. The composition according to claim 1, wherein the condensation aerosol particles comprise at least 95 percent by weight of alprazolam, estazolam, midazolam or triazolam.5. A method of producing the therapeutic compound alprazolam, estazolam, midazolam or triazolam in an aerosol form comprising: a) volatilizing a therapeutic compound selected from the group consisting of alprazolam, estazolam, midazolam or triazolam under conditions effective to produce a heated vapor of the compound, and b) during said volatilizing, passing air through the heated vapor to produce aerosol particles of the compound comprising less than 5% compound degradation products and c) aerosol MMAD is less than 3 &mgr;m. 6. The method according to claim 5, wherein the aerosol particles are formed at a rate of greater than 0.5 mg/sec.7. The method according to claim 5, wherein said volatilizing includes heating a coating of the therapeutic compound, which is formed on a solid support having the surface texture of a metal foil, to a temperature sufficient to volatilize the compound from the coating.8. The method according to claim 5, wherein the aerosol particles comprise less than 2.5 percent by weight of alprazolam, estazolam, midazolam or triazolam degradation products.9. The method according to claim 7, wherein the coating of the compound on said solid support surface has a thickness between 0.2 and 4.8 microns.10. The method according to claim 5, wherein the aerosol particles comprise at least 95 percent by weight of alprazolam, estazolam, midazolam or triazolam.
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