Anticipate generic drug launch
Proactively manage your pharmacy inventory
Find generic entry opportunities
Drug patents …
… from Kazakhstan to Kalamazoo
Deep knowledge on
small-molecule drugs and
the 110,000 global patents
Manage your formulary budget
Flat-rate pricing for predictable budgeting
Short-term plans for project- or client-based billing
|Title:||Stable, crystalline flunisolide|
|Abstract:||A unique crystalline polymorphic form of flunisolide is disclosed which is stable in aerosols such as Freon.RTM. mixtures and is valuable in the treatment of respiratory diseases, particularly bronchial asthma and allergic rhinitis.|
|Inventor(s):||Jones; Richard E. (Palo Alto, CA), Haringer; Gisela T. (Watsonville, CA)|
|Assignee:||Syntex Pharmaceuticals International Limited (Hamilton, BM)|
1. A compound of the formula ##STR3## i.e. 6.alpha.-fluoro-11.beta.,21-dihydroxy-16.alpha.,17.alpha.-isopropylidene dioxypregna-1,4-diene-3,20-dione hemihydrate.
2. A method for treating a respiratory disease in a mammal which comprises administering to said mammal by inhalation a therapeutically effective amount of the compound of claim 1 as an aerosol.
3. The method of claim 2 wherein the compound of claim 1 is administered as an aerosol formed from a mixture comprising a therapeutically effective amount of said crystalline form suspended in a pharmaceutically acceptable propellant containing an effective amount of a surfactant.
4. The method of claim 3 wherein said propellant comprises monofluorotrichloromethane, dichlorodifluoromethane, dichlorotetrafluoroethane or mixtures thereof.
5. The method of claim 4 wherein at least one pharmaceutically acceptable, propellant, in addition to those set forth in claim 4, is included in said aerosol.
6. A composition useful for treating a respiratory disease in a mamal comprising (a) 0.01 to about 20% by weight of a compound of the formula ##STR4## i.e. 6.alpha.-fluoro-11.beta.,21-dihydroxy-16.alpha.,17.alpha.-isopropylidene dioxypregna-1,4-diene-3,20-dione hemihydrate having a particle size less than 100 microns,
(b) about 0.1 to about 20% by weight of a suitable surfactant, and
(c) the remainder a pharmaceutically acceptable, liquid aerosol propellant.
7. The composition of claim 6 wherein said aerosol propellant is a pharmaceutically acceptable fluorinated or fluorochlorinated lower alkane.
8. The composition of claim 3 wherein said lower alkane is chosen from the group consisting of monofluorotrichloromethane, dichlorodifluoromethane, dichlorotetrafluoroethane, and mixtures thereof.
9. The composition of claim 6 wherein said composition is kept under pressure as an aerosol bomb.
10. The composition of claim 2 which comprises
(a) about 0.04% w to about 1.0% w of the compound of claim 1 having a particle size less than 25 microns;
(b) about 97.5% w to about 99.21% w of said propellant; and
(c) about 0.25% w to 1.5% w of sorbitan trioleate.
11. The composition of claim 10 wherein said propellant consists of 50% by weight dichlorodifluoromethane, 25% by weight trichloromonofluoromethane, and 25% by weight dichlorotetrafluoroethane.