METHOD OF PRODUCING AMORPHOUS SOLID DISPERSION OF N-BUTYL-N-METHYL-1-PHENYLPYRROLO[1,2-A]PYRAZINE-3-CARBOXAMIDE Russian patent published in 2024 - IPC C07D487/04 A61K31/4985 A61P25/00 

Abstract RU 2823423 C1

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing an amorphous solid dispersion containing a pharmaceutical substance as an active substance N-butyl-N-methyl-1-phenylpyrrolo[1,2-a]pyrazine-3-carboxamide, and as a polymer, additives are acceptable in pharmaceutical technology, according to which mixture containing 1 g of N-butyl-N-methyl-1-phenylpyrrolo[1,2-a]pyrazine-3-carboxamide, polyvinylpyrrolidone polymer (15–20 g) or PEG 6000/vinylcaprolactam/vinyl acetate (15–20 g), at a weight ratio of 1:15–20, is dissolved in 34–96% ethanol (30–35 g), the obtained solution is dried at 40–65°C in a drying cabinet for 8–12 hours.

EFFECT: novel method of producing an amorphous solid dispersion containing a pharmaceutical substance as an active substance N-butyl-N-methyl-1-phenylpyrrolo[1,2-a]pyrazine-3-carboxamide, which enables to obtain N-butyl-N-methyl-1-phenylpyrrolo[1,2-a]pyrazine-3-carboxamide from a crystalline into an amorphous state and improve the solubility and pharmaceutical bioavailability of tablets based thereon.

1 cl, 6 dwg, 2 tbl, 9 ex

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RU 2 823 423 C1

Authors

Mokrov Grigorij Vladimirovich

Yarkova Milada Arnoldovna

Vakhitova Yuliya Venerovna

Seredenin Sergej Borisovich

Alekseev Konstantin Viktorovich

Blynskaya Evgeniya Viktorovna

Tishkov Sergej Valerevich

Minaev Sergej Viktorovich

Markeev Vladimir Borisovich

Dates

2024-07-23Published

2023-04-11Filed