US 12,268,779 B2
Ophthalmic emulsion
Howard Allen Ketelson, Dallas, TX (US); and David L. Meadows, Colleyville, TX (US)
Assigned to Alcon Inc., Fribourg (CH)
Filed by Alcon Inc., Fribourg (CH)
Filed on May 18, 2023, as Appl. No. 18/319,794.
Application 18/319,794 is a continuation of application No. 17/200,043, filed on Mar. 12, 2021, granted, now 11,690,802.
Application 17/200,043 is a continuation of application No. 16/811,461, filed on Mar. 6, 2020, granted, now 11,234,929, issued on Feb. 1, 2022.
Application 16/811,461 is a continuation of application No. 16/405,180, filed on May 7, 2019, granted, now 10,624,848, issued on Apr. 21, 2020.
Application 16/405,180 is a continuation of application No. 15/989,383, filed on May 25, 2018, granted, now 10,328,025, issued on Jun. 25, 2019.
Application 15/989,383 is a continuation of application No. 15/228,589, filed on Aug. 4, 2016, granted, now 10,004,685, issued on Jun. 26, 2018.
Application 15/228,589 is a continuation of application No. 12/958,763, filed on Dec. 2, 2010, abandoned.
Claims priority of provisional application 61/266,207, filed on Dec. 3, 2009.
Prior Publication US 2023/0285289 A1, Sep. 14, 2023
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 9/107 (2006.01); A61K 9/00 (2006.01); C09K 23/00 (2022.01); C09K 23/14 (2022.01); C09K 23/34 (2022.01)
CPC A61K 9/107 (2013.01) [A61K 9/0048 (2013.01); C09K 23/017 (2022.01); C09K 23/14 (2022.01); C09K 23/34 (2022.01)] 16 Claims
 
1. An ophthalmic emulsion, the emulsion comprising:
water forming an aqueous phase;
oil forming an oil phase, wherein the oil is a hydrocarbon selected from mineral oil, paraffin oil and petrolatum, wherein the oil is at least 0.1 w/v % and no greater than 5 w/v %;
a hydrophilic surfactant having an HLB value of at least 8;
a hydrophobic surfactant having an HLB value of below 8;
an anionic phospholipid, wherein the anionic phospholipid is present in the emulsion in a concentration from 0.05 to 7.0 percent by weight;
borate;
a mucoadhesive galactomannan polymer, wherein the mucoadhesive galactomannan polymer is present in the emulsion in a concentration of at least 0.01 w/v %, but no greater than 1.0 w/v %;
an ophthalmic therapeutic agent for the treatment of ophthalmic diseases;
wherein the emulsion is free of a benzalkonium chloride,
wherein:
i. the oil phase is in droplets within the aqueous phase and the droplets have an average diameter that is no greater than about 1000 nm, but is at least 10 nm, wherein the average diameter is corresponding to 90% of the cumulative undersize distribution by volume measured using a Microtrac S3500 Particle Size Analyzer (Software Version 10.3.1); and
ii. the borate and galactomannan polymer cooperatively act to form a gel upon instillation of the emulsion in an eye of an individual.