New pectin deriv. bile acid adsorption agents - useful for treating hyperlipidaemia and can be administered at lower doses than colestyramine or colestipol resins

摘要

Pectin derivs. of formula (I) are new. In formula, R = OH, 6-30C opt. unsatd. natural or synthetic fatty acid bonded via carboxy, 6-30C alcohol function bonded via the alcohol gp., a natural or synthetic aminoacid bonded via carboxy, a bile acid bonded through a 2-12C alkyl or alkoxy gp. in position 3 and/or -XANR3R4; X = O or -OC(=O)-; A = 2-15C (pref. 2-8C and pref. branched) alkylene, alkenylene or alkynylene; R3, R4 = H or 1-6C alkyl pref. 1-3C alkyl; R2 = CO2H or -C(=O)Y-A-B; Y = O or NH; B = H, NH2 or a bile acid bonded through a mono or di(1-6C)alkyl gp. in position 3; and n = 10-500, pref. 30-200, esp. 40-100. Also claimed is a conjugate comprising (I) and at least one bile acid. USE/ADVANTAGE - (I) inhibit bile acid resorption and are useful as hypolipidaemic agents or for concentating bile acids in biological fluids used in food or fruit juice. (I) are prepd. in high yields under mild conditions. Dosage is 0.5-10g/Kg/day which is lower than that of known colestyramine and colestipol.