DDS COMPOUND AND PROCESS FOR THE PREPARATION THEREOF

摘要

A DDS compound in which amino group at 1-position of (1S,9S)-1-amino-9-ethyl-5-fluoro-2,3-dihydro-9-hydroxy-4-methyl-1H,12H -benzoÄdeÜpyranoÄ3',4':6,7Ü-indolizinoÄ1,2-bÜquinoline-10,13(9 H,15H)-dione as a drug compound is bound to a carboxyl group of a carboxymethyldextran polyalcohol with a spacer containing one amino acid or two to eight amino acids linked by peptide bond(s); characterized in that an introduced amount of residue of the drug compound is in a range of from 3.2% to 8.4% by weight; a weight-average molecular weight of the carboxymethyldextran polyalcohol is in a range of from 240,000 to 480,000; and degree of carboxymethylation is in a range of from 0.14 to 0.47; and a method for preparing said DDS compound, which comprises the steps of, for example, adding an aqueous solution containing sodium periodate to an aqueous solution containing dextran at a temperature of 4 DEG C +/- 2 DEG C to oxidize the dextran, and then adding the resulting reaction mixture to an aqueous solution containing sodium borohydride at a temperature not higher than 15 DEG C to obtain a dextran polyalcohol.