Delivery of anti-migraine compounds through an inhalation route
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-009/12
A61K-009/14
출원번호
US-0152640
(2002-05-20)
발명자
/ 주소
Rabinowitz, Joshua D.
Zaffaroni, Alejandro C.
출원인 / 주소
ALEXZA Molecular Delivery Corporation
대리인 / 주소
Stracker, Elaine C.
인용정보
피인용 횟수 :
50인용 특허 :
19
초록▼
The present invention relates to the delivery of anti-migraine compounds through an inhalation route. Specifically, it relates to aerosols containing lidocaine, verapamil, diltiazem, isometheptene, or lisuride that are used in inhalation therapy. In a composition aspect of the present invention, the
The present invention relates to the delivery of anti-migraine compounds through an inhalation route. Specifically, it relates to aerosols containing lidocaine, verapamil, diltiazem, isometheptene, or lisuride 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 lidocaine, verapamil, diltiazem, isometheptene, or lisuride. In a method aspect of the present invention, one of lidocaine, verapamil, diltiazem, isometheptene, or lisuride 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 lidocaine, verapamil, diltiazem, isometheptene, or lisuride, 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 lidocaine, verapamil, diltiazem, isometheptene, or lisuride through an inhalation route to a mammal is provided which comprises: a) a composition comprising at least 5 percent by weight of lidocaine, verapamil, diltiazem, isometheptene, or lisuride; and, b) a device that forms a lidocaine, verapamil, diltiazem, isometheptene, or lisuride containing aerosol from the composition, for inhalation by the mammal.
대표청구항▼
1. A composition for delivery of lidocaine, verapamil, diltiazem, isometheptene, or lisuride comprising a condensation aerosol a) formed by volatilizing lidocaine, veraparmil, diltiazem, isometheptene, or lisuride comprising under conditions effective to produce a heated vapor of lidocaine, verapa
1. A composition for delivery of lidocaine, verapamil, diltiazem, isometheptene, or lisuride comprising a condensation aerosol a) formed by volatilizing lidocaine, veraparmil, diltiazem, isometheptene, or lisuride comprising under conditions effective to produce a heated vapor of lidocaine, verapamil, diltiazem, isometheptene, or lisuride and condensing the heated vapor of the lidocaine, verapamil, diltiazem, isometheptene, or lisuride to form condensation aerosol particles, b) wherein said condensation aerosol particles are characterized by less than 5% lidocaine, verapamil, diltiazem, isometheptene, or lisuride degradation products, and c) wherein the aerosol MMAD is less than 3 microns. 2. The composition according to claim 1, wherein the lidocaine, verapamil, diltiazem, isometheptene, or lisuride is in a free base form.3. The composition according to claim 1, wherein the condensation aerosol particles comprise at least 90 percent by weight of lidocaine, verapamil, diltiazem, isometheptene, or lisuride.4. The composition according to claim 3, wherein the condensation aerosol particles comprise at least 95 percent by weight of lidocaine, verapamil, diltiazem, isometheptene, or lisuride.5. A method of producing an anti-migraine drug in an aerosol form comprising: a) volatilizing an anti-migraine drug under conditions effective to produce a heated vapor of the anti-migraine drug, and b) during said volatilizing, passing air through the heated vapor to produce aerosol particles of the anti-migraine drug comprising less than 5% drug degradation products and an aerosol having an MMAD less than 3 &mgr;m. 6. The method according to claim 5, wherein said volatilizing includes heating a thin layer which includes an anti-migraine drug, selected from the group of lidocaine, verapamil, diltiazem, isometheptene, or lisuride, which is on a solid support having the surface texture of a metal foil, to a temperature sufficient to volatilize the anti-migraine drug from the thin layer.7. The method according to claim 5, wherein the aerosol particles are formed at a rate of greater than 0.5 mg/sec.8. The method according to claim 6, wherein the aerosol particles comprise at least 90 percent by weight of lidocaine, verapamil, diltiazem, isometheptene, or lisuride.9. The method according to claim 8, wherein the aerosol particles comprise at least 95 percent by weight of lidocaine, verapamil, diltiazem, isometheptene, or lisuride.10. A composition for delivery of an anti-migraine drug comprising a condensation aerosol a) formed by volatilizing an anti-migraine drug under conditions effective to produce a heated vapor of the anti-migraine drug and condensing the heated vapor of the anti-migraine drug to form condensation aerosol particles, b) wherein said condensation aerosol particles are characterized by less than 5% anti-migraine drug degradation products, and c) wherein the aerosol MMAD is less than 3 microns.
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