PHARMACEUTICAL COMPOSITION CONTAINING A CAMPTOTHECIN POLYMER DERIVATIVE Russian patent published in 2020 - IPC A61K9/08 A61K9/19 A61K31/4745 A61K31/787 A61K47/26 A61K47/50 A61K47/60 A61K47/64 A61P35/00 

FIELD: pharmaceutical industry.

SUBSTANCE: invention relates to a pharmaceutical anti-tumor lyophilized preparation, comprising a block copolymer and 2–100 parts by weight of a saccharide or sugar alcohol relative to 1 part by weight of said block copolymer, where the block copolymer contains a glutamic acid link associated with a camptothecin derivative, and is represented by general formula (1)

in which R₁, R₄ , R₅ is H or (C₁-C₆) alkyl group; A—(C₁-C₆) alkylene group; R₂—H, (C₁-C₆) acyl group or (C₁-C₆) alkoxycarbonyl group; R₃ is -OH or -N(R₆)CONH(R₇); R₆, R₇ is a (C₁-C₈) alkyl group; each of t, d, e, (d+e) is an integer; t=45–450; (d+e)=6–60; ratio d and e to (d+e) is 1–100 % and 0–99 %, respectively; relative content of glutamic acid links, in which R₃ -OH and in which R₃ -N(R₆)CONH(R₇), relative to (d+e) is 15–60 % and 0–50 % respectively.

EFFECT: invention provides improved stability of the preparation during storage, which is determined by preserving the property of forming nanoparticles from block copolymer associates, and the ability to suppress the dissociation of the camptothecin derivative in the lyophilized preparation.

5 cl, 18 ex, 2 tbl