Abstract:

Herein, esomeprazole magnesium trihydrate was prepared and its crystal form was controlled. Moreover, the properties of the product, such as the particle size distribution, were optimized. X-ray powder diffraction was used to characterize the crystal shape of the product. A two-dimensional online imaging system was employed to monitor changes in the crystal morphology during the reactive crystallization of esomeprazole magnesium trihydrate. A Marvin laser particle size analyzer was used to monitor changes in the particle size distribution. The effects of the crystallization temperature, reactant concentration, on the crystal form and mophorology of esomeprazole trihydrate magnesium were investigated. Results show that the crystallization mode of esomeprazole magnesium trihydrate is spherical and the crystallization temperature is the key factor affecting the crystal shape. The optimized reaction temperature was 25 ℃. Using the optimized process, drug particles of esomeprazole magnesium trihydrate with a fixed crystal shape, uniform particle size distribution, and large average particle size can be synthesized.

Key words: :esomeprazole magnesium trihydrate, crystal shape control, reactive crystallization, particle size