Formulations of AG10
The present disclosure provides high-load tablet formulations of AG10 or a pharmaceutically acceptable salt thereof. In some aspects, provided herein are table formulations of AG10 or a pharmaceutically acceptable salt thereof that include at least 40% or more AG10 by weight and at least one pharmaceutical excipient selected from one or more fillers, one or more binders, one or more disintegrants, and one or more lubricants.
1. A tablet formulation comprising AG10, or a pharmaceutically acceptable salt thereof, and one or more fillers, wherein
(a) said tablet formulation comprises at least 40% or more by weight of AG10 or a pharmaceutically acceptable salt thereof; and
(b) said one or more fillers comprise a high-grade microcrystalline cellulose characterized by cellulose polymers with (i) spherical morphology and porous structure or (ii) needle-like particle shape.
2. The tablet formulation of claim 1 , comprising about 40-85% by weight of AG10 or a pharmaceutically acceptable salt thereof.
3. The tablet formulation of claim 2 , comprising about 50-75% by weight of AG10 or a pharmaceutically acceptable salt thereof.
4. The tablet formulation of claim 1 , comprising about 50% by weight of AG10 or a pharmaceutically acceptable salt thereof.
5. The tablet formulation of claim 1 , comprising about 66.7% by weight of AG10 or a pharmaceutically acceptable salt thereof.
6. The tablet formulation of claim 1 , comprising about 75% by weight of AG10 or a pharmaceutically acceptable salt thereof.
7. The tablet formulation of claim 1 , wherein said one or more fillers comprise about 1-60% by weight of said tablet formulation.
8. The tablet formulation of claim 7 , wherein said one or more fillers comprise about 5-55% by weight of said tablet formulation.
9. The tablet formulation of claim 7 , wherein said one or more fillers comprise about 10-50% by weight of said tablet formulation.
10. The tablet formulation of claim 7 , wherein said one or more fillers comprise about 15-45% by weight of said tablet formulation.
11. The tablet formulation of claim 1 , wherein said one or more fillers further comprise a cellulose derivative or an inorganic salt.
12. The tablet formulation of claim 1 , wherein said one or more fillers further comprise silicon dioxide.
13. The tablet formulation of claim 1 , further comprising one or more disintegrants, said one or more disintegrants comprise about 1-15% by weight of said tablet formulation.
14. The tablet formulation of claim 13 , wherein said one or more disintegrants comprise about 3-8% by weight of said tablet formulation.
15. The tablet formulation of claim 13 , wherein said one or more disintegrants comprise about 6% by weight of said tablet formulation.
16. The tablet formulation of claim 13 , wherein said one or more disintegrants comprise croscarmellose sodium.
17. The tablet formulation of claim 1 , further comprising one or more lubricants, said one or more lubricants comprise about 0.1-8% by weight of said tablet formulation.
18. The tablet formulation of claim 17 , wherein said one or more lubricants comprise about 1.5% by weight of said tablet formulation.
19. The tablet formulation of claim 17 , wherein said one or more lubricants comprise magnesium stearate.
20. The tablet formulation of claim 1 , wherein said tablet formulation is at least 75% dissolved after performance of a dissolution test in a solution of 0.1N HCl at 37±0.5° C. in an Apparatus-II (Paddles) with a paddle speed of about 50 rpm for 10 minutes.
21. The tablet formulation of claim 20 , wherein said tablet formulation is at least 85% dissolved after performance of said dissolution test.
22. The tablet formulation of claim 21 , wherein said tablet formulation is at least 95% dissolved after performance of said dissolution test.
23. The tablet formulation of claim 20 , wherein said dissolution test is performed at least three months after preparation of said tablet formulation.
24. The tablet formulation of claim 1 , further comprising a coating agent.
25. The tablet formulation of claim 1 , wherein AG10 is the pharmaceutically acceptable salt form of Formula Ia
26. A tablet formulation comprising at least 40% or more by weight of AG10, or a pharmaceutically acceptable salt thereof; a high-grade microcrystalline cellulose filler; an inorganic salt filler; a disintegrant; and a lubricant, wherein
said high-grade microcrystalline cellulose is characterized by cellulose polymers (i) with spherical morphology and porous structure or (ii) needle-like particle shape.