Drug – bio-affecting and body treating compositions – Effervescent or pressurized fluid containing – Organic pressurized fluid
Reexamination Certificate
2002-05-20
2004-11-09
Hartley, Michael G. (Department: 1616)
Drug, bio-affecting and body treating compositions
Effervescent or pressurized fluid containing
Organic pressurized fluid
C424S046000, C424S043000, C424S489000, C424S780000, C514S220000, C514S252010, C128S203150, C128S200240, C125S011020
Reexamination Certificate
active
06814954
ABSTRACT:
FIELD OF THE INVENTION
The present invention relates to the delivery of compounds for the treatment of Parkinsons through an inhalation route. Specifically, it relates to aerosols containing antiparkinsonian drugs that are used in inhalation therapy.
BACKGROUND OF THE INVENTION
There are a number of compositions currently marketed for the treatment of Parkinsons. The compositions contain at least one active ingredient that provides for observed therapeutic effects. Among the active ingredients given in such antiparkinsoniam compositions are benzotropine, pergolide, ropinerole, amantadine and deprenyl.
It is desirable to provide a new route of administration for antiparkinsonian drugs that rapidly produces peak plasma concentrations of the compounds. The provision of such a route is an object of the present invention.
SUMMARY OF THE INVENTION
The present invention relates to the delivery of compounds for the treatment of Parkinsons through an inhalation route. Specifically, it relates to aerosols containing antiparkinsonian drugs 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 an antiparkinsonian drug. Preferably, the particles comprise at least 10 percent by weight of an antiparkinsonian drug. More preferably, the particles comprise at least 20 percent, 30 percent, 40 percent, 50 percent, 60 percent, 70 percent, 80 percent, 90 percent, 95 percent, 97 percent, 99 percent, 99.5 percent or 99.97 percent by weight of an antiparkinsonian drug.
Typically, the aerosol has a mass of at least 10 &mgr;g. Preferably, the aerosol has a mass of at least 100 &mgr;g. More preferably, the aerosol has a mass of at least 0.200 &mgr;g.
Typically, the particles comprise less than 10 percent by weight of antiparkinsonian drug degradation products. Preferably, the particles comprise less than 5 percent by weight of antiparkinsonian drug degradation products. More preferably, the particles comprise less than 2.5, 1, 0.5, 0.1 or 0.03 percent by weight of antiparkinsonian drug degradation products.
Typically, the particles comprise less than 90 percent by weight of water. Preferably, the particles comprise less than 80 percent by weight of water. More preferably, the particles comprise less than 70 percent, 60 percent, 50 percent, 40 percent, 30 percent, 20 percent, 10 percent, or 5 percent by weight of water.
Typically, at least 50 percent by weight of the aerosol is amorphous in form, wherein crystalline forms make up less than 50 percent by weight of the total aerosol weight, regardless of the nature of individual particles. Preferably, at least 75 percent by weight of the aerosol is amorphous in form. More preferably, at least 90 percent by weight of the aerosol is amorphous in form.
Typically, the aerosol has an inhalable aerosol particle density greater than 10
6
particles/mL. Preferably, the aerosol has an inhalable aerosol particle density greater than 10
7
particles/mL or 10
8
particles/mL.
Typically, the aerosol particles have a mass median aerodynamic diameter of less than 5 microns. Preferably, the particles have a mass median aerodynamic diameter of less than 3 microns. More preferably, the particles have a mass median aerodynamic diameter of less than 2 or 1 micron(s).
Typically, the geometric standard deviation around the mass median aerodynamic diameter of the aerosol particles is less than 3.0. Preferably, the geometric standard deviation is less than 2.5. More preferably, the geometric standard deviation is less than 2.3.
Typically, the aerosol is formed by heating a composition containing an antiparkinsonian drug to form a vapor and subsequently allowing the vapor to condense into an aerosol.
In another composition aspect of the present invention, the aerosol comprises particles comprising at least 5 percent by weight of benzotropine, pergolide, ropinerole, amantadine or deprenyl. Preferably, the particles comprise at least 10 percent by weight of benzotropine, pergolide, ropinerole, amantadine or deprenyl. More preferably, the particles comprise at least 20 percent, 30 percent, 40 percent, 50 percent, 60 percent, 70 percent, 80 percent, 90 percent, 95 percent, 97 percent, 99 percent, 99.5 percent or 99.97 percent by weight of benzotropine, pergolide, ropinerole, amantadine or deprenyl.
Typically, the aerosol has a mass of at least 10 &mgr;g. Preferably, the aerosol has a mass of at least 100 &mgr;g. More preferably, the aerosol has a mass of at least 200 &mgr;g.
Typically, the particles comprise less than 10 percent by weight of benzotropine, pergolide, ropinerole, amantadine or deprenyl degradation products. Preferably, the particles comprise less than 5 percent by weight of benzotropine, pergolide, ropinerole, amantadine or deprenyl degradation products. More preferably, the particles comprise less than 2.5, 1, 0.5, 0.1 or 0.03 percent by weight of benzotropine, pergolide, ropinerole, amantadine or deprenyl degradation products.
Typically, the particles comprise less than 90 percent by weight of water. Preferably, the particles comprise less than 80 percent by weight of water. More preferably, the particles comprise less than 70 percent, 60 percent, 50 percent, 40 percent, 30 percent, 20 percent, 10 percent, or 5 percent by weight of water.
Typically, at least 50 percent by weight of the aerosol is amorphous in form, wherein crystalline forms make up less than 50 percent by weight of the total aerosol weight, regardless of the nature of individual particles. Preferably, at least 75 percent by weight of the aerosol is amorphous in form. More preferably, at least 90 percent by weight of the aerosol is amorphous in form.
Typically, where the aerosol comprises benzotropine, the aerosol has an inhalable aerosol drug mass density of between 0.1 mg/L and 4 mg/L. Preferably, the aerosol has an inhalable aerosol drug mass density of between 0.2 mg/L and 3 mg/L. More preferably, the aerosol has an inhalable aerosol drug mass density of between 0.3 mg/L and 2 mg/L.
Typically, where the aerosol comprises pergolide, the aerosol has an inhalable aerosol drug mass density of between 0.01 mg/L and 2.5 mg/L. Preferably, the aerosol has an inhalable aerosol drug mass density of between 0.02 mg/L and 1 mg/L. More preferably, the aerosol has an inhalable aerosol drug mass density of between 0.05 mg/L and 0.5 mg/L.
Typically, where the aerosol comprises ropinerole, the aerosol has an inhalable aerosol drug mass density of between 0.02 mg/L and 4 mg/L. Preferably, the aerosol has an inhalable aerosol drug mass density of between 0.04 mg/L and 2 mg/L. More preferably, the aerosol has an inhalable aerosol drug mass density of between 0.10 mg/L and 1.0 mg/L.
Typically, where the aerosol comprises amantadine, the aerosol has an inhalable aerosol drug mass density of between 5 mg/L and 500 mg/L. Preferably, the aerosol has an inhalable aerosol drug mass density of between 10 mg/L and 200 mg/L. More preferably, the aerosol has an inhalable aerosol drug mass density of between 20 mg/L and 150 mg/L.
Typically, where the aerosol comprises deprenyl, the aerosol has an inhalable aerosol drug mass density of between 0.5 mg/L and 12.5 mg/L. Preferably, the aerosol has an inhalable aerosol drug mass density of between 1 mg/L and 10 mg/L. More preferably, the aerosol has an inhalable aerosol drug mass density of between 2 mg/L and 7.5 mg/L.
Typically, the aerosol has an inhalable aerosol particle density greater than 10
6
particles/mL. Preferably, the aerosol has an inhalable aerosol particle density greater than 10
7
particles/mL or 10
8
particles/mL.
Typically, the aerosol particles have a mass median aerodynamic diameter of less than 5 microns. Preferably, the particles have a mass median aerodynamic diameter of less than 3 microns. More preferably, the particles have a mass median aerodynamic diameter of less than 2 or 1 micron(s).
Typically, the geometric standard deviation around the mass median aerodynamic diameter of the aerosol particles is less than 3.0. Preferably, the geometric standar
Rabinowitz Joshua D.
Zaffaroni Alejandro C.
Alexza Molecular Delivery Corporation
Haghighatian Mina
Hartley Michael G.
Stracker Elaine C.
LandOfFree
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