FIELD: pharmaceutical industry.
SUBSTANCE: invention relates to a pharmaceutical anti-tumor lyophilised composition, comprising a pH adjusting agent and a copolymer block of formula (1), containing a glutamic acid link bound with a camptothecin derivative:
,
where R1, R4, R5 is H or (C1-C6) alkyl group; A is (C1-C6) alkylene group; R2 is H, (C1-C6) acyl group or (C1-C6) alkoxycarbonyl group; R3 is -OH and/or -N(R6)CONH(R7); R6 and R7 are (C1-C8) alkyl group; each of t, d, e is an integer; t=45-450; (d+e)=6-60; share of d and e relative to (d+e) respectively 1–100 % and 0–99 %; fraction of glutamic acid links when R3 -OH and when R3 -N(R6)CONH(R7) is 15–60 % and 0–50 % relative to (d+e), respectively. PH of the aqueous solution of the disclosed composition with concentration of the copolymer block of formula (1) 1 mg/ml in terms of the camptothecin derivative ranges from 3.0 to 6.5.
EFFECT: invention improves stability of the composition during storage, while preserving the properties of the copolymer block to form associates in the aqueous solution.
1 cl, 24 ex, 10 tbl
