MANUFACTURE OF DEGARELIX Russian patent published in 2018 - IPC A61K38/09 A61K47/12 A61K9/19 

FIELD: medicine.

SUBSTANCE: group of inventions relates to degarelix and methods for the manufacture of a medicinal product containing degarelix substance. Substance includes degarelix, acetic acid in an amount of 4.5 to 10.0% (w/w), water in an amount of 10% (w/w). After dissolution in water of 20 mg of degarelix as a free base and mannitol in an amount of 2.5 wt. %, the substance exhibits a viscosity of up to 3.2 mPa⋅C. Viscosity is measured with a viscometer with a cone-plane measuring system with D=60 mm and 1°. Shear rate is increased from 0 to 500 s^-1 for 20 steps at a constant temperature of 20±0.2°C. Methods for the preparation of a medicament substance of degarelix and the manufacture of a lyophilized drug product of degarelix are also provided.

EFFECT: inventions make it possible to manufacture medical products with a viscosity and bioavailability that provides a sustained release of the active substance for several months depending on the dosage.

12 cl, 3 dwg, 2 tbl, 8 ex