Tablet formulation for CGRP active compounds
The present invention is directed to compositions comprising an extrudate or solid solution of a compound, or a salt thereof, of Formula I (API): wherein “R a ” is independently —H or —F, in a water-soluble polymer matrix which further comprises a disintegration system allowing a tablet made therefrom to rapidly disintegrate in the environment in which the API is to be released.
1. A tablet comprising:
an extrudate comprising:
a water-soluble polymer matrix;
a dispersing agent; and
a compound of Formula Ia, or a pharmaceutically acceptable salt thereof:
wherein each of R b is —H,
wherein the compound of Formula Ia is dispersed within the polymer matrix; and
a disintegration system.
2. The tablet according to claim 1 , wherein the water-soluble polymer matrix is a water-soluble polyvinylpyrrolidone/vinyl acetate (PVP-VA) copolymer.
3. The tablet according to claim 1 , wherein the disintegration system comprises a disintegrant selected from the group consisting of croscarmellose sodium and crospovidone.
4. The tablet according to claim 3 , wherein the disintegrant is croscarmellose sodium.
5. The tablet according to claim 1 , wherein the dispersing agent is selected from the group consisting of d-alpha tocopherol polyethyleneglycol succinate (TPGS) and polyethoxylated castor oil.
6. The tablet according to claim 5 , wherein the dispersing agent is d-alpha tocopherol polyethyleneglycol succinate (TPGS).
7. The tablet according to claim 1 , wherein the compound of Formula Ia is present in an amount from about 20 wt % to about 22 wt % of the extrudate.
8. The tablet according to claim 7 , wherein the extrudate comprises about 50 wt % of the tablet.
9. The tablet according to claim 1 , wherein the tablet has a hardness of from about 12 kP to about 18 kP.
10. The tablet of claim 1 , wherein the disintegration system comprises powdered sodium chloride.