Influence of Surfactants, Polymers, and Concentration of the Water Phase on in Vitro Drug Release from Emulsion-Type Suppositories

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Generally, drug release from the base is considered to be one of the most important parameters in evaluating the pharmaceutical usefulness of suppositories in vivo and in vitro. In spite of the therapeutic importance and wide applications of suppositories, the absorption mechanisms and the factors determining their absorption characteristics have not been established. The present study was undertaken to investigate the effects of surfactants, polymers, and concentration of the water phase on in vitro drug release emulsion-type suppositories. N_1-(2'-furanidyl)-5-fluorouracil (FT-207), theophylline and indomethacin were chosen as model compounds. In order to clarify the behavior of the rectal membrane, the following three different methods for studying drug release (in vitro) were selected : (1) the filter membrane technique, (2) the use of membranes of animal origin, (3) in situ rectal recirculation technique. The following results were obtained. (1) In the case of readily water-soluble compounds such as FT-207,the amount of drug released increased with increase of the water content in the suppository base. (2) On the other hand, no significant effect of concentration of the water phase in the suppository base was found for fatty drugs such as indomethacin. (3) By the addition of aqueous polymer, the amount of drug released could be controlled and the release prolonged in the emulsion-type suppository base.
公益社団法人日本薬学会の論文
1982-08-25

Influence of Surfactants, Polymers, and Concentration of the Water Phase on in Vitro Drug Release from Emulsion-Type Suppositories

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