US 12,478,577 B2
Pharmaceutical compositions for treating ocular diseases or disorders
Sanjib Kumar Das, Morrisville, NC (US); and Cheng-Wen Lin, Cary, NC (US)
Assigned to Alcon Inc., Fribourg (CH)
Filed by Alcon Inc., Fribourg (CH)
Filed on Mar. 5, 2020, as Appl. No. 16/810,149.
Claims priority of provisional application 62/814,198, filed on Mar. 5, 2019.
Prior Publication US 2020/0306182 A1, Oct. 1, 2020
Int. Cl. A61K 9/00 (2006.01); A61K 31/472 (2006.01); A61K 31/573 (2006.01); A61K 47/34 (2017.01); A61K 45/06 (2006.01)
CPC A61K 9/0024 (2013.01) [A61K 31/472 (2013.01); A61K 31/573 (2013.01); A61K 47/34 (2013.01); A61K 9/0048 (2013.01); A61K 45/06 (2013.01)] 5 Claims
 
1. A pharmaceutical composition for treating an ocular disease or disorder, comprising:
(a) a biodegradable polymer matrix consisting of a mixture of a first polymer and a second polymer, wherein:
(1) the first polymer is a biodegradable polyester amide polymer, wherein the biodegradable polyester amide polymer comprises structure (II):

OG Complex Work Unit Chemistry
and
(2) the second polymer is a combination of an ester end-capped biodegradable poly (D,L-lactide-co-glycolide) copolymer and an acid end-capped biodegradable poly (D,L-lactide-co-glycolide) copolymer; and
(b) at least one therapeutic agent, pharmaceutically acceptable salt, zwitterion, polymorph, or solvate thereof, wherein the at least one therapeutic agent is selected from gefitinib, lapatinib, erlotinib, sunitinib, sorafenib, regorafenib, afatinib, vandetanib, semaxanib, cediranib, neratinib, axitinib, lestaurtinib, tivozanib, dexamethasone, or (1R,2R)—N-(4-methylisoquinolin-6-yl)-2-(4-(N-(pyridin-2-yl)sulfamoyl)phenyl)cyclopropane-1-carboxamide;
wherein the at least one therapeutic agent, pharmaceutically acceptable salt, zwitterion, polymorph, or solvate thereof is homogenously dispersed within the biodegradable polymer matrix;
wherein the pharmaceutical composition is formulated for intravitreal administration to a subject's eye, and the pharmaceutical composition is formulated to release the at least one therapeutic agent from the pharmaceutical composition in a substantially linear manner for at least 6 months;
wherein the biodegradable polymer matrix is about 59 weight % of the pharmaceutical composition, and the at least one therapeutic agent, pharmaceutically acceptable salt, zwitterion, polymorph, or solvate thereof is about 41 weight % of the pharmaceutical composition; and
wherein the first polymer is about 60 weight % of the biodegradable polymer matrix and the second polymer is about 40 weight % of the biodegradable polymer matrix.