GB929391A — Therapeutic compositions comprising polymeric amines

USPTO Abstract

Orally administrable pharmaceutical compositions for binding bile-acids in the gastro-intestinal tract and having blood cholesterol lowering activity comprise a carrier and a synthetic, non-toxic polymer having a skeleton inert to digestive enzymes and a molecular weight in excess of about 3000 and containing ionizable amino groups, the polymer if water-insoluble having the property of binding at least 30% by weight of the available glycocholic acid into a form incapable of dialysis through a cellulose membrane within 5 minutes when exposed to an equal weight of the acid, and having a moisture content of at least 65% after equilibration with air at 100% humidity at 25 DEG C., and, if water-soluble, having an equivalent weight, based on the ionizable amino groups of at least 500 and the property of binding at least 80% of its weight of glycocholic acid in vitro into a form incapable of dialysis through a cellulose membrane. Suitable polymers are divinyl benzene cross-linked polystyrene quaternary ammonium salt resins, e.g. those sold under the Trade Mark "Dowex 1," linear acrylic type quaternary ammonium salt polymers having a molecular weight of the order of 2,000,000, e.g. those sold under the Trade Marks "Acryloid CQ," and "Acrysol CQ," and its tertiary amine salt "Acrysol CA," polyethyleneimine having an average molecular weight of about 30,000 and a co-polymer of acrylamide and vinyl benzene trimethylammonium chloride in a weight ratio of about 30 : 70 having an equivalent weight of about 302 and an average molecular weight of above 100,000. The compositions may be in conventional forms, e.g. a tablet, elixir, syrup or flavoured aqueous solution.