Rutin solubility and dissolution rate improvement - by conversion into solid dispersions in hydroxyalkyl-theophylline or -theobromine derivs. e.g. hydroxyethyl-theophylline

摘要

Process for increasing the solubility and dissolution rate of rutin, with the objective of improving absorption from the gastrointestinal tract, comprises the prodn. of solid dispersions (solid solns.) from (a) rutin and (b) readily water-soluble hydroxyalkyl derivs. of theophy-line (1,3-dimethylxanthine) and the obromine (3,7-dimethyl(xanthine). The solid dispersions or solns. have better water solubility and dissolution rate than rutin or its physical mixtures with water-soluble hydroxyalkyl theophylline or theobromine derivs. Pref. hydroxyalkyl-theophlline and theobromine derivs are hydroxyethyltheophylline, duhydroxypropyltheophylline, hydroxypropyltheophylline, hydroxyethyltheobromine, dihydroxypropyltheobromine, hydroxypropyltheobromine, and their mixtures.