METHODS FOR INCREASING SOLUBILITY OF MEDICINAL AGENT BASED ON PYRIMIDINE DERIVATIVE OF BENZOPHENONE Russian patent published in 2020 - IPC A61K31/513 A61K47/26 A61K31/30 A61P31/18 

Abstract RU 2729792 C1

FIELD: medicine; pharmaceuticals.

SUBSTANCE: invention refers to pharmaceutics and represents a method for increasing solubility of the active pharmaceutical ingredient 1-[2-(2-benzoylphenoxy)ethyl]-6-methyluracil by creating a composition for HIV-1 therapy containing the active ingredient in amount of 1–33 wt. % and auxiliary substance in amount of 67–99 wt. %, and including the stages: preparation of solution of 1-[2-(2-benzoylphenoxy)ethyl]-6-methyluracil in a solvent selected from ethanol, methanol, acetone, with addition of an auxiliary substance selected from the group: synthetic copolymer of polyethylene glycol 6000, vinylcaprolactam and vinyl acetate, polyvinylpyrrolidone in concentration of 2–7 g/l (solution A1) or preparation of solution of 1-[2-(2-benzoylphenoxy)ethyl]-6-methyluracil in one of said solvents (solution A2); preparation of solution of auxiliary substances in water in concentration of 50–100 g/l (solution B); mixing solution A1 with an equivalent amount of water and stripping solvent or mixing solution A1 or A2 with water, stripping solvent, mixing solution B and distilling solvent; drying suspension.

EFFECT: obtained composition has improved pharmacokinetic characteristics, in particular solubility and bioavailability.

1 cl, 4 dwg, 2 tbl, 7 ex

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RU 2 729 792 C1

Authors

Makarov Valerij Gennadevich

Makarova Marina Nikolaevna

Demchenko Dmitrij Valentinovich

Dates

2020-08-12Published

2019-07-29Filed