The present application relates to solid state forms of Betrixaban and its Maleate salt, and processes for preparation thereof.

Polymorphs of betrixaban & its maleate salt

The invention provides a hydrate amorphous form of betrixaban maleate and a preparation method of the hydrate amorphous form. The hydrate amorphous form adopts pale yellow powder, and has the molecular formula of C23H22ClN5O3.C4H4O4.H2O. The invention further discloses the preparation method of the hydrate amorphous form of the betrixaban maleate. The preparation method comprises the following steps: feeding a betrixaban maleate raw material in an isopropanol solvent to form a suspension, cooling to the room temperature after dissolved clarification, gradually adding a proper amount of deionized water, and performing freeze drying to obtain a target product. The hydrate amorphous form product is high in solubility and fluidity, and the requirement of the hydrate amorphous form as a preparation API (Active Pharmaceutical Ingredient) is met.

Hydrate amorphous form of betrixaban maleate and preparation method of hydrate amorphous form

An amorphous form of betrixaban maleate and process for the preparation of the same are disclosed. A solid dispersion of amorphous betrixaban maleate with pharmaceutically acceptable excipients and processes for the preparation of the same are also disclosed. Betrixaban base polymorphic forms and processes for preparing the same are also disclosed.

Chaitanya Muggu

Papers

Polymorphs and solid dispersion of betrixaban and methods for the preparation thereof