US 11,850,249 B2
Methods of efficiently reducing intraocular pressure
Mandar V. Shah, Rockaway, NJ (US); Ilango Subramanian, Warren, NJ (US); Veerappan Subramanian, Warren, NJ (US); and Aman Trehan, Hillsborough, NJ (US)
Assigned to Somerset Therapeutics, LLC, Hollywood, FL (US)
Filed by Somerset Therapeutics, LLC, Hollywood, FL (US)
Filed on Oct. 5, 2021, as Appl. No. 17/494,681.
Claims priority of provisional application 63/087,657, filed on Oct. 5, 2020.
Prior Publication US 2022/0105102 A1, Apr. 7, 2022
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 31/542 (2006.01); A61K 31/498 (2006.01); A61K 9/00 (2006.01); A61K 47/02 (2006.01); A61K 47/10 (2017.01); A61K 47/18 (2017.01); A61K 9/08 (2006.01); A61K 47/32 (2006.01); A61K 47/34 (2017.01)
CPC A61K 31/542 (2013.01) [A61K 9/0048 (2013.01); A61K 9/08 (2013.01); A61K 31/498 (2013.01); A61K 47/02 (2013.01); A61K 47/10 (2013.01); A61K 47/186 (2013.01); A61K 47/32 (2013.01); A61K 47/34 (2013.01)] 14 Claims
 
1. A method of treating elevated intraocular pressure (IOP) in a mammalian eye comprising administering an effective amount of a pharmaceutically acceptable and ophthalmologically suitable composition to the eye no more than twice per 24-hour period, the composition comprising:
(a) a pharmaceutically acceptable and ophthalmologically suitable brinzolamide compound in an amount of about 1 wt. %-about 10 wt. % of the composition; and
(b) a pharmaceutically acceptable and ophthalmologically suitable brimonidine compound in an amount of about 0.02 wt. %-about 0.5 wt. % of the composition, and
(c) benzalkonium chloride in an amount of 0.007 wt. %-about 0.02 wt. % of the composition, and
(d) a pharmaceutically acceptable and ophthalmologically suitable borate-polyol complex in an amount of about 0.5 wt. %-about 6 wt. % of the composition wherein the borate-polyol complex comprises two or more polyol compounds, and wherein the ratio of the benzalkonium chloride to the boric acid is between about 1:14 and about 1:43,
wherein the composition comprises less than 1% non-ionic surfactant, and further wherein performing the method results in an effect that (1) is bioequivalent to or (2) results in a greater bioavailability of the brinzolamide compound, the brimonidine compound, or both, than the administration of a reference product comprising the same amount of a brinzolamide compound and the same amount of a brimonidine compound that is administered three times per 24-hour period; and wherein the composition is in the form of an ophthalmic suspension.