US 12,239,687 B2
Sustained release formulations using non-aqueous membrane emulsification
Hunter Chen, New York, NY (US); and Yiming Zhao, Great Neck, NY (US)
Assigned to Regeneron Pharmaceuticals, Inc., Tarrytown, NY (US)
Filed by Regeneron Pharmaceuticals, Inc., Tarrytown, NY (US)
Filed on Nov. 24, 2021, as Appl. No. 17/535,267.
Claims priority of provisional application 63/118,264, filed on Nov. 25, 2020.
Prior Publication US 2022/0160828 A1, May 26, 2022
Int. Cl. A61K 38/17 (2006.01); A61K 9/16 (2006.01)
CPC A61K 38/179 (2013.01) [A61K 9/1658 (2013.01); A61K 9/1694 (2013.01)] 20 Claims
OG exemplary drawing
 
1. A method of producing encapsulation efficient polymer-coated microparticles, wherein the method comprises:
combining micronized protein powder and a polymer into a hydrocarbon solvent to form a non-aqueous first solution, wherein the micronized protein powder comprises at least one selected from the group consisting of an antibody and an Fc-fusion protein;
agitating the first non-aqueous solution to form a suspension;
feeding the suspension to a dispersion cell, wherein the suspension is infused through a porous membrane into a continuous phase comprising a fluorocarbon liquid and a fluorosurfactant under a tangent flow of the continuous phase to form a hydrocarbon-in-fluorocarbon emulsion;
adding a hydrofluoroether to the hydrocarbon-in-fluorocarbon emulsion;
removing the hydrocarbon solvent to provide hardened microparticles; and
removing the fluorocarbon liquid to isolate the microparticles, wherein the microparticles comprise protein encapsulated within a matrix of polymer, wherein the protein is encapsulated at an efficiency of about 80% measured by protein loading in the polymer-coated microparticles or the theoretical protein loading from the first non-aqueous solution.