US 12,214,081 B2
Tablet dosage formulations of oleyl phosphocholine
Johannes Jan Platteeuw, Werkhoven (NL)
Assigned to Oblita Therapeutics BVBA, Zoersel (BE)
Appl. No. 17/603,024
Filed by Oblita Therapeutics BVBA, Zoersel (BE)
PCT Filed Apr. 10, 2020, PCT No. PCT/EP2020/060324
§ 371(c)(1), (2) Date Oct. 12, 2021,
PCT Pub. No. WO2020/208230, PCT Pub. Date Oct. 15, 2020.
Claims priority of application No. 19168885 (EP), filed on Apr. 12, 2019.
Prior Publication US 2022/0183975 A1, Jun. 16, 2022
Int. Cl. A61K 9/16 (2006.01); A61K 9/20 (2006.01); A61K 9/28 (2006.01); A61K 31/685 (2006.01)
CPC A61K 9/1641 (2013.01) [A61K 9/1652 (2013.01); A61K 9/1694 (2013.01); A61K 9/2013 (2013.01); A61K 9/2018 (2013.01); A61K 9/205 (2013.01); A61K 9/2054 (2013.01); A61K 9/2095 (2013.01); A61K 9/2813 (2013.01); A61K 9/2826 (2013.01); A61K 9/288 (2013.01); A61K 9/2893 (2013.01); A61K 31/685 (2013.01)] 14 Claims
 
1. A process for making an olelyl phosphocholine (OlPC) containing granulate, said process comprising a blending step, a hot melt extrusion step and a milling step,
wherein the blending step comprises preparing a granulation mixture of olelyl phosphocholine and granulation excipients, wherein said granulation excipients comprise at least a spacer, an antioxidant and a disintegrant, and optionally a binder and/or a lubricant;
wherein the hot melt extrusion step comprises preparing an extrudate by heating said granulation mixture at a temperature of at least 50° C. and below 90° C. and extrudating said heated granulation mixture;
wherein the milling step comprises cooling said extrudate and milling said cooled extrudate to obtain a milled extrudate;
wherein no solvent is added during the process for granulation,
wherein the concentration of oleyl phosphocholine in the milled extrudate is between 10 and 50 weight percent,
wherein, if a binder is added as a granulation excipient, the concentration of the binder in the milled extrudate is between 10 and 50 weight percent,
wherein, if a lubricant is added as a granulation excipient, the concentration of the lubricant in the milled extrudate is between 1 and 20 weight percent,
wherein the concentration of the antioxidant in the milled extrudate is between 0.05 and 5 weight percent,
wherein the concentration of the disintegrant in the milled extrudate is between 1 and 20 weight percent,
wherein the concentration of the spacer in the milled extrudate is between 10 and 50 weight percent, and
wherein the concentrations are relative to the milled extrudate.