Generated: May 26, 2017
|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.
Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.