	US 12,478,587 B1
	Formulation for lacosamide
Shoufeng Li, Piscataway, NJ (US); Ye Huang, Piscataway, NJ (US); Fen Ren, Shanghai (CN); and Bolun Zhang, Shanghai (CN)
Assigned to SHANGHAI AUCTA PHARMACEUTICALS CO., LTD., Shanghai (CN)
Filed by Shanghai Aucta Pharmaceuticals Co., Ltd., Shanghai (CN)
Filed on Feb. 6, 2025, as Appl. No. 19/047,536.
Int. Cl. A61K 9/00 (2006.01); A61K 9/16 (2006.01); A61K 9/50 (2006.01); A61K 31/165 (2006.01)

CPC A61K 9/5084 (2013.01) [A61K 9/0053 (2013.01); A61K 9/1611 (2013.01); A61K 9/1617 (2013.01); A61K 9/1635 (2013.01); A61K 9/1652 (2013.01); A61K 31/165 (2013.01)]

19 Claims

1. A capsule enclosing lacosamide, comprising: (a) a first dosage form comprising a first portion of lacosamide, which comprises an immediate release (IR) portion of lacosamide and an extended release (ER) portion of lacosamide, wherein the first portion is substantially released at a pH ranging from 1.0 to 8.0 after the capsule is administered to a subject; and

(b) a second dosage form comprising a second portion of lacosamide configured for extended release, wherein the second portion of lacosamide is coated with an enteric layer comprising one or more pH dependent polymers and accounts for at least 10% of the total amount of lacosamide in the capsule, wherein the second portion of lacosamide is substantially released at a pH ranging from 5.5 to 8.0 after the capsule is administered to the subject;

wherein, when administered once a day, the capsule provides at steady state a ratio between C_min,ssand C_max,ssranging from about 1:1.2 to about 1:3.0 and a peak-trough fluctuation (PTF) ranging from about 35% to about 65%, and

wherein the first portion of lacosamide ranges from about 65% to about 90% of the total amount of lacosamide in the capsule.