METHOD FOR SOLUBILIZATION OF 5-AMINO-2,3-DIHYDRO-1,4-PHTHALAZINEDIONE Russian patent published in 2023 - IPC C07D237/32 A61K31/502 A61K45/00 A61K47/10 A61K47/12 A61K47/14 A61K47/22 A61K47/24 A61K9/08 A61P29/00 A61P37/02 A61P37/06 A61P43/00 

FIELD: medicine.

SUBSTANCE: present invention relates to a method for solubilization of 5-amino-2,3-dihydro-1,4-phthalazinedione. The method includes following stages: a) provision of 5-amino-2,3-dihydro-1,4-phthalazinedione in the total range from 0.1% to 25% by wt., at a room temperature and pressure from 0.2 bar to 1 bar; b) addition, in any order, of solubilizing agents: at least one phosphatidylcholine in the total range from 20% to 80% by wt., at least one triglyceride with an average chain length in the total range from 10% to 70% by wt., at least one lysophosphatidylcholine in the total range from 1% to 15% by wt., at least one C2-C4 alcohol in the total range from 1% to 20% by wt., and at least one glyceryl stearate and/or saturated or unsaturated C14-C20 fatty acid in the total range from 0.5% to 10% by wt., respectively, while relative weight percentages of all ingredients amount to no more than 100%, and all solubilizing agents are independently of each other a food additive and/or pharmaceutically acceptable auxiliary substance; c) gentle heating of the resulting mixture by continuous increasing a temperature with continuous increment of the temperature of 0.5°C/min - 3°C/min for a period from 20 to 60 minutes; d) termination of temperature increasing in the temperature range from 30°C to 125°C as soon as a transparent solution is obtained; and e) cooling of solubilizate to a room temperature. The invention also discloses solubilizate of 5-amino-2,3-dihydro-1,4-phthalazinedione; solubilizate of sodium, potassium, or lithium salt of 5-amino-2,3-dihydro-1,4-phthalazinedione, or a mixture thereof; preventive or therapeutic use of solubilizate as an immunomodulator for the treatment of conditions with an excessive immune reaction or conditions with immunodeficiency background, as well as a pharmaceutical composition containing 5-amino-2,3-dihydro-1,4-phthalazinedione and at least one pharmaceutically acceptable auxiliary substance.

EFFECT: ease of handling, absence of long time for development of a suitable composition, absence of the need for use of expensive equipment, cheap materials and production costs, absence of the need for addition of polysorbate solubilizers.

14 cl, 10 ex