POLYMERIC WATER-SOLUBLE ANALOG OF ACETYL-SALICYLIC ACID AND METHOD OF ITS SYNTHESIS Russian patent published in 2003 - IPC

FIELD: organic chemistry, chemical-pharmaceutical industry, pharmacy. SUBSTANCE: invention relates to preparing water-soluble preparations of acetylsalicylic acid. Invention proposes novel water-soluble analog of acetylsalicylic acid of the formula: where n : m = (5:1)-(1:5). Analog is synthesized by chemical immobilization of acetylsalicylic acid on copolymer of N-vinylpyrrolidone with N-(glycidyl)-vinyl-γ-amino-butyric acid. This polymer is prepared by treatment of polyvinyl-pyrrolidone with chloromethyloxirane in the presence of catalyst that results to opening part of pyrrolidone cycles to form structure of N-vinyl-γ-aminobutyric acid and formation of by-side chains carrying reactive glycidyl groups. New analog shows the enhanced analgetic, anti-inflammatory, antipyretic and thrombolytic activity and reduced gastrotoxicity and nephrotoxicity. New analog of acetylsalicylic acid in the dose containing 75 mg of substance does not exhibit the damage effect on stomach mucosa that is typical for equal dose of acetyl- -salicylic acid. EFFECT: improved properties of analog. 3 cl, 2 tbl, 5 ex