STABLE CRYSTALLINE MONOHYDRATE OF HYDROCHLORIDE EPIRUBICIN AND METHOD FOR ITS PRODUCTION Russian patent published in 2017 - IPC C07C29/78 C07H15/252 C07H1/00 

FIELD: pharmacology.

SUBSTANCE: invention relates to a process for preparation of stable crystalline epirubicin hydrochloride monohydrate with a water content in the range of 2.7% to 3.5% (w/w), free of residual solvents. The method comprises addition of at least the first solvent and at least the second solvent for the epirubicin hydrochloride. The first solvent is selected from the group consisting of 1-butanol, 2-butanol, isobutanol, t-butanol and mixtures thereof; the second solvent is selected from the group consisting of 1-propanol, isopropanol, ethanol and mixtures thereof; and the volume ratio of the first solvent to the second solvent is in the range of 1:1 to 2:1 (v/v); adjustment of the water content of the solution obtained in step (a) to an amount in the range of 8% to 11% (w/w); (c) heating of the solution obtained in step (b) to a temperature of 70°C to 90°C to ensure crystallization; and (d) purification of the crystals obtained in the step (c). The resulting crystalline monohydrate has a water content in the range of 2.7% to 3.5% (w/w) and does not contain residual solvents. And the resulting crystalline monohydrate is characterized by a powder X-ray diffraction pattern comprising peaks at medium diffraction angles (2Θ) 5.1°, 9.1°, 13.6°, 22.1°, 22.5° and 24.0° (each ±0.2°).

EFFECT: new efficient method to obtain a valuable substance used in medicine.

7 cl, 13 dwg, 5 tbl, 8 ex