Claims for Patent: 11,969,409

Summary for Patent: 11,969,409

Title:	Formulations of apremilast
Abstract:	Provided herein are oral dosage forms comprising a) a core tablet comprising (i) a drug layer comprising apremilast and hypromellose acetate succinate (HPMCAS) in an amorphous solid dispersion; and (ii) a swellable layer comprising one or more swellable polymers; and b) a coating layer disposed on the core tablet, wherein the oral dosage form surface comprises at least one drug release orifice. The disclosed oral dosage forms provide once-a-day dosing of apremilast and are suitable for treating diseases or disorders ameliorated by inhibiting phosphodiesterase subtype IV (PDE4).
Inventor(s):	Nathan Bennette, William Brett Caldwell, Christi Hostetler, Kazden Ingram, Dory King, Kyle Kyburz, Alison Viles
Assignee:	Amgen Inc
Application Number:	US18/196,718
Patent Claims:	1. An oral dosage form comprising: a. a core tablet comprising (i) a drug layer comprising a) amorphous apremilast and hypromellose acetate succinate (HPMCAS) in a solid dispersion and b) a water soluble polymer; and (ii) a swellable layer comprising one or more swellable polymers; and b. a coating layer disposed on the core tablet, wherein the amorphous apremilast and HPMCAS are present in a weight ratio of 45:55 to 55:45 in the core tablet and the oral dosage form surface comprises at least one drug release orifice. 2. The oral dosage form of claim 1, wherein the apremilast is present in an amount of 6-15 wt % of the core tablet. 3. The oral dosage form of claim 1, wherein the HPMCAS is present in an amount of 6-15 wt % of the core tablet. 4. The oral dosage form of claim 1, wherein apremilast and HPMCAS are present in a weight ratio of 48:52 to 52:48 in the core tablet. 5. The oral dosage form of claim 1, wherein the water soluble polymer comprises polyethylene oxide having an average molecular weight of 200 kDa or higher. 6. The oral dosage form of claim 5, wherein the polyethylene oxide has an average molecular weight of 200-600 kDa. 7. The oral dosage form of claim 1, wherein the water soluble polymer is present in an amount of 30-55 wt % of the core tablet. 8. The oral dosage form of claim 1, wherein the water soluble polymer and apremilast are present in a weight ratio of 2 to 6:1, in the drug layer. 9. The oral dosage form of claim 1, wherein the drug layer further comprises one or more of an osmotic agent, a diluent, and a lubricant. 10. The oral dosage form of claim 9, wherein the drug layer comprises an osmotic agent. 11. The oral dosage form of claim 10, wherein the osmotic agent comprises sodium chloride. 12. The oral dosage form of claim 11, wherein the osmotic agent is present in the drug layer in an amount of 3-8 wt % of the core tablet. 13. The oral dosage form of claim 5, wherein the swellable polymer comprises polyethylene oxide. 14. The oral dosage form of claim 13, wherein the polyethylene oxide of the swellable layer has a higher average molecular weight of the polyethylene oxide in the drug layer. 15. The oral dosage form of claim 13, wherein the polyethylene oxide of the swellable layer has an average molecular weight of 5,000 kDa. 16. The oral dosage form of claim 1, wherein the swellable layer further comprises one or more of an osmotic agent, a diluent, and a lubricant. 17. The oral dosage form of claim 16, wherein the swellable layer comprises an osmotic agent. 18. The oral dosage form of claim 17, wherein the osmotic agent comprises sodium chloride. 19. The oral dosage form of claim 1, wherein the drug layer and swellable layer are present in a weight ratio of 2:1 in the core tablet.