| 摘要 |
A novel crystalline form of sitagliptin hydrochloride having inhibitory effects on DP-IV(dipeptidyl peptidase-IV) is provided to improve water stability by reducing water-absorption over the time, thereby inhibiting decomposition and purity lowering of the compound and storing it for a long period. A novel crystalline form of sitagliptin hydrochloride having a powder X-ray diffraction pattern showing peaks at 2-theta of 13.7, 18.0, 22.6, 25.7 and 27.0±0.2 degrees is prepared by reacting (a) amine hydrochloride or a mixture of amine compounds and hydrochloric acid having smaller pKa than maximum pKa of sitagliptin with (b) sitagliptin in at least one organic solvent selected from hydroxy, nitroalkane, acetonitrile, acetate, ether, alkane chloride and ketone, and optionally stirring the reaction product to promote crystallization of sitagliptin.
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