COMPOSITION WITH ARIMOCLOMOL Russian patent published in 2021 - IPC A61K31/4545 A61K47/38 A61K47/00 A61K9/16 A61K9/22 A61K9/50 A61P25/28 A61P3/10 

FIELD: pharmaceutical industry.

SUBSTANCE: invention relates to the pharmaceutical industry and namely to a composition based on N-[2-hydroxy-3-(1-piperidinyl)-propoxy]-pyridine-1-oxide-3-carboximidoyl-chloride, its stereoisomers and their acid addition salts. A sustained release oral pharmaceutical formulation includes: a. an active pharmaceutical ingredient selected from N-[2-hydroxy-3- (1-piperidinyl)-propoxy]-pyridine-1-oxide-3-carboxyimidoyl-chloride, its stereoisomers and their acid addition salts, and b. an excipient that controls release. The excipient that controls release provides sustained release of the active pharmaceutical ingredient, and the composition reduces OCT2 inhibition relative to an equivalent amount of N-[2-hydroxy-3-(1-piperidinyl)-propoxy]-pyridine-1-oxide-3-carboximidoyl-chloride, its stereoisomers and their acid addition salts administered by an immediate release oral dosage form and/or by IV bolus injection, and where the active pharmaceutical ingredient is present in a single dosage form or a composition unit in a total amount of 5-1000 mg per dose. The composition provides C_max that is less than or equal to 10 mcM.

EFFECT: composition effectively reduces OCT2 inhibition relative to an equivalent amount of N-[2-hydroxy-3-(1-piperidinyl)-propoxy]-pyridine-1-oxide-3-carboximidoyl-chloride, its stereoisomers and their acid addition salts administered via an immediate release oral dosage form and/or by IV bolus injection.

46 cl, 27 tbl, 4 ex, 17 dwg