US 11,752,129 B2
Formulations of apremilast
Nathan Bennette, Thousand Oaks, CA (US); William Brett Caldwell, Thousand Oaks, CA (US); Christi Hostetler, Thousand Oaks, CA (US); Kazden Ingram, Thousand Oaks, CA (US); Dory King, Thousand Oaks, CA (US); Kyle Kyburz, Thousand Oaks, CA (US); and Alison Viles, Thousand Oaks, CA (US)
Assigned to AMGEN INC., Thousand Oaks, CA (US)
Filed by AMGEN INC., Thousand Oaks, CA (US)
Filed on Aug. 31, 2022, as Appl. No. 17/899,769.
Application 17/899,769 is a continuation of application No. PCT/US2022/031325, filed on May 27, 2022.
Claims priority of provisional application 63/194,247, filed on May 28, 2021.
Prior Publication US 2023/0000825 A1, Jan. 5, 2023
Int. Cl. A61K 9/20 (2006.01); A61K 31/4035 (2006.01); A61K 9/00 (2006.01); A61K 9/28 (2006.01)
CPC A61K 31/4035 (2013.01) [A61K 9/0065 (2013.01); A61K 9/2009 (2013.01); A61K 9/2054 (2013.01); A61K 9/2086 (2013.01); A61K 9/2853 (2013.01); A61K 9/2866 (2013.01)] 17 Claims
 
1. An oral dosage form comprising:
a core tablet comprising
(i) a drug layer comprising 8-11 wt % apremilast based upon total core tablet weight, 8-11 wt % hypromellose acetate succinate (HPMCAS) based upon total core tablet weight, 2-7 wt % mannitol based upon total core tablet weight, 40-45 wt % polyethylene oxide with molecular weight of 200,000 Da based upon total core tablet weight, 0.1-0.5 wt % magnesium stearate based upon total core tablet weight, and 0.1-0.5 wt % colloidal silicon dioxide based upon total core tablet weight, wherein the apremilast and HPMCAS are in a solid dispersion; and
(ii) a swellable layer comprising 18-25 wt % polyethylene oxide with molecular weight of 5,000,000 Da based upon total core tablet weight, 7-10 wt % microcrystalline cellulose based upon total core tablet weight, 1.5-3.5 wt. % sodium chloride based upon total core tablet weight, 0.01-0.2 wt % iron oxide based upon total core tablet weight, and 0.05-0.3 wt % magnesium stearate based upon total core tablet weight; and
a coating layer disposed on the core tablet and comprising cellulose acetate and polyethylene glycol; and
the oral dosage form surface comprises at least one drug release orifice.