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US 2020/0390767 A1Published application
Formulations of 4-(7-Hydroxy-2-isopropyl-4-oxo-4H-quinazolin-3-yl)-benzonitrile
AssigneeNovartis AG
InventorsJoseph Paul BULLOCK, Chinmay MAHESHWARI, Quintus MEDLEY, Muneto MOGI, Michela MONTECCHI-PALMER, Kali STASI
Life of this patent
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Abstract
The present invention provides formulations of 4-(7-hydroxy-2-isopropyl-4-oxo-4H-quinazolin-3-yl)-benzonitrile (compound I) and methods for treating ocular surface pain by administering such formulations. The present invention also provides methods for treating dry eye disease and ocular hyperemia by administering formulations of 4-(7-hydroxy-2-isopropyl-4-oxo-4H-quinazolin-3-yl)-benzonitrile.
Claims18
-94. (canceled)
A formulation, comprising:
- a suspension of 4-(7-Hydroxy-2-isopropyl-4-oxo-4H-quinazolin-3-yl)-benzonitrile (compound I) or a salt, co-crystal, or polymorph thereof, in an amount of about 0.5% w/v to about 3.5% w/v,
- a non-ionic surfactant selected from the group consisting of a polysorbate surfactant, a block copolymer of ethylene oxide, propylene oxide surfactant, poloxamer, tyloxapol, and combinations thereof;
- a suspending agent selected from the group consisting of carbomer, hydroxypropyl methyl cellulose (hypromellose), polyethylene glycol, and combinations thereof;
- a tonicity agent selected from the group selected from mannitol, glycerin, xylitol, sorbitol and propylene glycol, and combinations thereof;
- a buffer;
- optionally, a salt;
- optionally, a preservative;
- and
- water in quantity sufficient (qs) to 100%.
6 more elements
A formulation, comprising:
- a suspension of polymorphic form B of 4-(7-Hydroxy-2-isopropyl-4-oxo-4H-quinazolin-3-yl)-benzonitrile (compound I), in an amount of about 0.5% w/v to about 2.5% w/v,
- tyloxapol in an amount of about 0.04 w/v to about 0.06% w/v;
- carbomer homopolymer Type B in an amount from about 0.05% w/v to about 0.4% w/v;
- glycerin in an amount of from about 0.5% w/v to about 5% w/v;
- a buffer selected from edetate, phosphate, borate, tromethamine, or combinations thereof;
- sodium chloride in an amount of from 0.01% w/v to about 1% w/v;
- and
- water qs to 100%;
- wherein the formulation has a pH in the range of from about 5.5 to about 8.0.
6 more elements
Dependencies are inferred from the claim text.