AU2025220825A1 — Tablet formulation for CGRP-active compounds

USPTO Abstract

#$%^&*AU2025220825A120250911.pdf##### ABSTRACT The present invention is directed to compositions comprising an extmdate or solid solution of a compound, or a salt thereof, of Formula I (API): Formula I, wherein "Ra" 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. ABSTRACT Colloidal Silica (Cab-O-Sil) Cosieve Microcrystalline Cellulose (Avicel) Milled dispersion Screen (optional) Mannitol NaCl Powder Crocarmellose Sodium Blend/Lubricate Coseived Cab-O-Sil/Avicel Sodium Stearyl Fumarate Compress to Tablet FIG.3 0 N o NH NFgC N N 0H3C Rº Rª (I) R* RRª The present invention is directed to compositions comprising an extmdate or solid solution of a compound, or a salt thereof, of Formula I (API): Formula I, wherein "Ra" 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. 20 25 22 08 25 22 A ug 2 02 5 A B S T R A C T 2 0 2 5 2 2 0 8 2 5 2 2 A u g 2 0 2 5 C o l l o i d a l S i l i c a ( C a b - O - S i l ) C o s i e v e M i c r o c r y s t a l l i n e C e l l u l o s e ( A v i c e l ) M i l l e d d i s p e r s i o n S c r e e n ( o p t i o n a l ) M a n n i t o l N a C l P o w d e r C r o c a r m e l l o s e S o d i u m B l e n d / L u b r i c a t e C o s e i v e d C a b - O - S i l / A v i c e l S o d i u m S t e a r y l F u m a r a t e C o m p r e s s t o T a b l e t F I G . 3 0 N o N H I N F g C N N 0 H 3 C Rº R ª ( I ) R * R R ª T h e p r e s e n t i n v e n t i o n i s d i r e c t e d t o c o m p o s i t i o n s c o m p r i s i n g a n e x t m d a t e o r s o l i d s o l u t i o n o f a c o m p o u n d , o r a s a l t t h e r e o f , o f F o r m u l a I ( A P I ) : F o r m u l a I , w h e r e i n " R a " i s i n d e p e n d e n t l y H o r - F , i n a w a t e r - s o l u b l e p o l y m e r m a t r i x w h i c h f u r t h e r c o m p r i s e s a d i s i n t e g r a t i o n s y s t e m a l l o w i n g a t a b l e t m a d e t h e r e f r o m t o r a p i d l y d i s i n t e g r a t e i n t h e e n v i r o n m e n t i n w h i c h t h e A P I i s t o b e r e l e a s e d .