US 12,005,060 B2
Ophthalmic formulations of methotrexate
Dean Eliott, Carlsbad, CA (US); Stephen Gitu Machatha, Wilmington, MA (US); Pramod Sarpotdar, Roseville, CA (US); and Tomasz Stryjewski, Somerville, MA (US)
Assigned to Aldeyra Therapeutics, Inc., Lexington, MA (US)
Filed by Aldeyra Therapeutics, Inc., Lexington, MA (US)
Filed on Sep. 15, 2022, as Appl. No. 17/932,426.
Application 17/932,426 is a continuation of application No. 17/753,721, previously published as PCT/US2020/050565, filed on Sep. 11, 2020.
Claims priority of provisional application 63/044,288, filed on Jun. 25, 2020.
Claims priority of provisional application 62/900,060, filed on Sep. 13, 2019.
Prior Publication US 2023/0018197 A1, Jan. 19, 2023
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 31/519 (2006.01); A61K 9/00 (2006.01); A61K 47/02 (2006.01); A61K 47/26 (2006.01)
CPC A61K 31/519 (2013.01) [A61K 9/0048 (2013.01); A61K 47/02 (2013.01); A61K 47/26 (2013.01)] 16 Claims
 
1. A composition suitable for intravitreal administration, comprising:
methotrexate, a density enhancing agent, and a phosphate buffer, wherein the composition has a transit rate of less than 10 min in 1 mL of silicone oil (SiO) having a viscosity of at least 1000 centistoke and depth of 1 cm; the methotrexate is at a concentration of about 7 mg/mL to about 9 mg/mL, the density enhancing agent comprises sucrose at a concentration of about 7.0% w/v to about 8.0% w/v; the phosphate buffer is sodium phosphate dibasic dihydrate at a concentration of about 0.113 mg/mL to 0.142 mg/mL, and the composition is in a pre-filled syringe and has an administration volume of about 40 μL, about 45 μL, about 50 μL, or about 60 μL.