EP4045048A1 — Oral formulations comprising sitagliptin hci monohydrate with improved pharmaceutical characteristics

USPTO Abstract

An oral pharmaceutical formulation in the form of an immediate release tablet comprising sitagliptin hydrochloride, preferably monohydrate manufactured by using wet granulation method wherein croscarmellose sodium and dibasic calcium phosphate are used both in intragranular and extragranular phases. The total amount ratio of croscarmellose sodium used in intragranular and extragranular phases to the total amount of composition is between 1:5 and 5:1, preferably between 1:2 and 2:1, more preferably 1:2.5 and, the amount of ratio of dibasic calcium phosphate in intragranular to the amount of ratio of dibasic calcium phosphate in extragranular phases is 1:5, preferably 1:2, more preferably 1:1.