US 12,390,474 B2
Immediate release multilayer tablet
Renato A. Chiarella, Dublin (IE); Hector Guzman, Dublin (IE); Paul Hurley, Dublin (IE); David Manser, Dublin (IE); and Kristopher Perkin, Dublin (IE)
Assigned to Alkermes Pharma Ireland Limited, Dublin (IE)
Filed by Alkermes Pharma Ireland Limited, Dublin (IE)
Filed on Nov. 15, 2023, as Appl. No. 18/510,585.
Application 18/510,585 is a continuation of application No. 18/327,229, filed on Jun. 1, 2023, granted, now 11,951,111.
Application 18/327,229 is a continuation of application No. 17/855,242, filed on Jun. 30, 2022, granted, now 11,707,466, issued on Jul. 25, 2023.
Application 17/855,242 is a continuation of application No. PCT/EP2021/081585, filed on Nov. 12, 2021.
Claims priority of provisional application 63/113,067, filed on Nov. 12, 2020.
Prior Publication US 2024/0082257 A1, Mar. 14, 2024
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 9/20 (2006.01); A61K 9/24 (2006.01); A61K 31/485 (2006.01); A61K 31/5513 (2006.01)
CPC A61K 31/5513 (2013.01) [A61K 9/2013 (2013.01); A61K 9/2018 (2013.01); A61K 9/2027 (2013.01); A61K 9/2054 (2013.01); A61K 9/209 (2013.01); A61K 9/2095 (2013.01); A61K 31/485 (2013.01)] 16 Claims
 
1. A pharmaceutically acceptable tablet for orally delivering a fixed dose of olanzapine and 10 mg of samidorphan, wherein the tablet comprises:
a first tablet layer comprising:
10 mg samidorphan or a pharmaceutically acceptable salt of samidorphan in an amount to deliver 10 mg samidorphan;
about 75-90 wt % of a first diluent selected from the group consisting of lactose or a hydrate thereof, microcrystalline cellulose, mannitol, sorbitol, xylitol, dicalcium phosphate, starch and combinations thereof; based on the weight of the first tablet layer; and
about 1.5 to about 2 wt % of magnesium stearate;
a second tablet layer comprising:
a dose of olanzapine selected from the group consisting of 5 mg, 10 mg, 15 mg and 20 mg of the olanzapine;
about 75-90 wt % of a second diluent selected from the group consisting of lactose or a hydrate thereof, microcrystalline cellulose, mannitol, sorbitol, xylitol, dicalcium phosphate, starch and combinations thereof; based on the weight of the first tablet layer; and
about 1.0 wt % magnesium stearate;
wherein the tablet releases at least 97% of olanzapine and at least 97% of the samidorphan after 30 minutes when the tablet is tested in 500 mL USP acetate buffer at pH 1.0 using a USP Apparatus II (Paddle Method) at 37° C., with a paddle speed of 75 rpm and using a three-prong sinker.