New dextran deriv. - are bile acid adsorption agents for treating hyperlipidaemia in low doses

摘要

Dextran derivs. of formula (I) are new. In the formula R = OH; carboxy-bound 6-30C satd. or unsatd. natural or synthetic fatty acid; residue of 4-20C alcohol; carboxy-bound natural or synthetic amino acid; bile acid (bonded via 2-12C alkyl or alkoxy at 3 position) and/or -X-A-NR1R2 (II); X = NR3, O, NR3CO, OCO, pref. O or OCO; with the CO gp. not adjacent to the dextran residue; A = 2-15 (pref. 2-8)C linear (pref.) or branched alkylene, alkenylene or alkynylene; R1,R2 and R3 = H or 1-6 (pref. 1-3)C alkyl; best R3 is H; n = 30-80 (pref. 35-70). Also new are conjugates (A) of (I) with at least one bile acid. Pref. only one type of substit. is present, i.e. only amino acid (including (II)) or fatty acid and/or alcohol. In partic. amino acid and (II) residues are not present together. USE/ADVANTAGE - (I) bind bile acids in a concn.-dependent manner; are not themselves resorbable and have a high binding rate at neutral pH. By binding bile acids they reduce serum cholesterol levels so are useful as hypolipidaemic agents for use in foods and fruit juices. Unlike known resins they do not cause avitaminosis, constipation or steatorrhoea; only relatively small doses (0.5-10 g/kg) are needed and they do not have to be formulated with taste improvers, emulsifiers, sweeteners, etc. (I) can also be used for group-selective enrichment of bile acids from biological fluids.