US 11,654,113 B2
Modified release formulations and uses thereof
Takumi Asada, Hyogo (JP); Gerald R. Galluppi, Marlborough, MA (US); Seth Cabot Hopkins, Northborough, MA (US); Megumi Maruyama, Okayama (JP); Siriporn Toongsuwan, Berlin, MA (US); and Yuki Tsushima, Osaka (JP)
Assigned to Sunovion Pharmaceuticals Inc., Marlborough, MA (US)
Filed by Sunovion Pharmaceuticals Inc., Marlborough, MA (US)
Filed on Sep. 30, 2021, as Appl. No. 17/490,616.
Application 17/490,616 is a continuation of application No. 16/892,641, filed on Jun. 4, 2020, granted, now 11,160,758.
Claims priority of provisional application 62/944,023, filed on Dec. 5, 2019.
Claims priority of provisional application 62/872,623, filed on Jul. 10, 2019.
Claims priority of provisional application 62/856,952, filed on Jun. 4, 2019.
Prior Publication US 2022/0117899 A1, Apr. 21, 2022
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 9/20 (2006.01); A61K 31/40 (2006.01); A61K 47/38 (2006.01); A61P 25/18 (2006.01); A61P 25/24 (2006.01)
CPC A61K 9/2054 (2013.01) [A61K 31/40 (2013.01); A61K 47/38 (2013.01); A61P 25/18 (2018.01); A61P 25/24 (2018.01)] 24 Claims
OG exemplary drawing
 
1. A solid oral dosage pharmaceutical composition comprising:
between about 100 mg to about 600 mg of amisulpride by weight of free base,
an unequal mixture of (R)-(+)-amisulpride and (S)-(−)-amisulpride, or pharmaceutically acceptable salts thereof, wherein the enantiomeric ratio of (R)-(+)-amisulpride to (S)-(−)-amisulpride is 85:15 by weight of free base, and
an extended release agent in an amount between about 10% to about 50% by total solid oral dosage composition weight to provide a modified-release form;
wherein:
after administration of the composition to a subject results in a population geometric mean AUC from 0 to 24 hours after administration (AUC0-24) of amisulpride that is less than about 80% of the population geometric mean AUC0-24 achieved by an immediate release composition having the same enantiomeric ratio and same total daily amount of amisulpride as the solid oral dosage composition;
over the period of 12 hours after administration of the composition to a subject results in a subject population average maximum QTcF interval prolongation relative to baseline that is less than 12 milliseconds (ms); and
about 27 hours after administration of the composition to a subject results in a population average occupancy of dopamine D2 receptors between about 20% and about 60%.