ANTI-CANCER DRUG TOPOISOMERASE I INHIBITOR Russian patent published in 2022 - IPC A61K31/7056 A61K47/26 A61K47/58 A61P35/00 

Abstract RU 2786727 C1

FIELD: medicine.

SUBSTANCE: present invention relates to the field of medicine, namely to an antitumor drug of a topoisomerase I inhibitor based on indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7-diones-n-{12-(β-d-xylopyranosyl)-5,7-dioxo-indolo[2,3-a]pyrrolo[3,4-c]carbazol-6-yl}pyridine-2-carboxamide, characterized in that it additionally contains as part of the medicinal unit forms Polysorbate 80, Polyvinylpyrrolidone (PVP) with the following ratio of components (mg) in the dosage form unit - vial:

indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7-diones-n-{12-(β-d-xylopyranosyl)-5,7-dioxo-indolo[2,3-a]pyrrolo[3,4-c]carbazol-6-yl}pyridine-2-carboxamide 22,5-27,5 mg Polysorbate 80 PVP

EFFECT: invention provides for the development of an antitumor agent whose excipients, such as Polysorbate 80 and Polyvinylpyrrolidone, promote rehydration of the lyophilisate with water for injection and obtain a true solution, which provides a bolus intravenous administration of it to animals, and the resulting composition of the agent is a drug for parenteral use, with good solubility and stability due to the possibility of its lyophilization, also the antitumor agent is convenient to use - the required dose of the active substance in the dosage form unit (a vial with 25 mg lyophilisate), and the biological activity of the agent is equivalent to the prototype, but toxic manifestations are less pronounced, due to the absence organic solvents in the composition.

1 cl, 1 tbl, 3 ex

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Authors

Lantsova Anna Vladimirovna

Nikolaeva Lyudmila Leonidovna

Orlova Olga Lvovna

Smirnova Galina Borisovna

Pokrovskij Vadim Sergeevich

Sanarova Ekaterina Viktorovna

Polozkova Alevtina Pavlovna

Shprakh Zoya Sergeevna

Ignateva Elena Vladimirovna

Borisova Larisa Mikhajlovna

Kiseleva Marina Petrovna

Dmitrieva Mariya Vyacheslavovna

Golubeva Irina Sergeevna

Kulbachevskaya Nataliya Yurevna

Konyaeva Olga Ivanovna

Ermakova Nadezhda Pavlovna

Prosalkova Irina Robertovna

Gusev Dmitrij Vasilevich

Eremina Vera Aleksandrovna

Pugacheva Ruzhena Borisovna

Dates

2022-12-26Published

2022-09-01Filed