[Experiences with the rectal use of a chemotherapeutic agent. 1. In vitro biopharmaceutical examinations; selection of the optimal vehicle].

The factors influencing in vitro liberation (Part 1) and in vivo absorption (Part 2) from trimethoprim-containing rectal suppositories and the authors' results related to them are reported in this two-part publication. Special emphasis was laid on selecting the optimal suppository base which is harmless physiologically yet not indifferent pharmacologically. From among the 24 compositions studied, a lipophilic mixture containing a surface active additive (Witepsol W 35) and a hydrophilic (Macrogolum) mixture were found to be the best in all respects. Liberation from the trimethoprim-containing rectal suppositories was measured with in vitro dynamic diffusion and spectrophotometrically. A power relation was found to exist between the quantity of the released pharmacon and the diffusion time, and a significant negative exponential relation was observed between the doses and their respective in vitro availability values.