[The increase in the liberation rate of propyphenazone from preoral solid dosage forms]

The authors report on the influence of the granulation and tabletting applying macromolecular agents (polyvinylpolypyrrolidone Heweten 40, polyethylenglycol 6000, polyvinylpyrrolidone K25, polyvinylpyrrolidone K90 and potato starch) on the liberation rate of propyphenazone which exhibits by its hydrophobicity unfavourable dissolution parameters. A significant increase of the liberation rate of propyphenazone (re-crystallized from various media) has been realized by direct pressing of polyvinylpolypyrrolidone and Heweten 40 as well as by gelatine solution granulation, with which the last method exhibits the advantage of an increased accuracy of dosage and a decreased friability. The gelatine granulation of the drug itself as well as the starch granulate addition resulted in an increased dissolution rate. The addition of other agents (polyvinylpyrrolidone K25, K90 and polyethylenglycol 6000) as well as the pressing of a propyphenazone produced by re-crystallization of an aqueous tenside solution, which distinguishes by an extreme dissolution rate, were not at all suitable for the tabletting. The tablet disintegration caused by hydrophile disintegration media, is the condition granting the liberation of the hydrophobic drug. The wettability and thus the dissolution rate of the drug are increased by the liberation.