Patent Evaluation: Polyamide bile acid sequestrants are more potent than cholestyramine

Summary

Novelty: Amide polymers, potentially useful in the treatment of hypercholesterolaemia, are claimed. The polymers form ionic and hydrogen bonds with bile acids, preventing reabsorption and facilitating their excretion. The compositions have greater efficacy than the known therapeutic agents, cholestyramine and cholestipol, which have a similar mode of action.

Biology: A six month in vivo canine study evaluating the ability of the compounds to lower plasma cholesterol levels is described (animals were fed on a semi-synthetic, low cholesterol diet with and without a bile acid sequestrant). The results indicate that the compounds are effective for the control of blood cholesterol levels and show superior activity to cholestyramine.

Chemistry: Dimethylaminopropylmethacrylamide (DMAPMA) is one of thirty-four polymers specifically claimed. Preparative details using standard techniques are presented.