STABILIZED PHARMACEUTICAL COMPOSITIONS OF CAMPTOTHECIN Russian patent published in 2020 - IPC A61K31/4745 A61K47/18 A61K47/24 A61K47/26 A61K47/28 A61K9/127 A61P35/00 

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a liposomal pharmaceutical composition of irinotecan for treating cancer containing irinotecan sucrose octasulfate (SOS), encapsulated in liposomes, consisting of cholesterol and phospholipids with ratio of 500±10 g of irinotecan lactone per mole of total amount of phospholipids, where the composition is obtained by a method involving: (a) formation of liposomes, containing 1,2-distearoyl-sn-glycero-3-phosphocholine (DSPC), cholesterol and methoxy-terminated polyethylene glycol-distearoylphosphatidylethanolamine, encapsulating a substituted ammonium salt of SOS with a sulphate concentration of 0.4–0.5 M; (b) bringing the liposomes into contact with a solution containing irinotecan, at a temperature higher than the transition temperature of phospholipid components to obtain encapsulated irinotecan sucrose octasulfate in liposomes; (c) adjusting the pH of the liposome preparation to pH from 7.25 to 7.50.

EFFECT: invention provides stability of the composition consisting of less than 20 mol % of lysophosphatidylcholine of the total amount of phospholipids for 6 months of storage at temperature of 2 to 8 °C.

31 cl, 13 dwg, 15 tbl, 9 ex