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Bioavailability of acetaminophen containing suppositories in rats.

An attempt was made to optimize the rectal delivery of acetaminophen (paracetamol). One of the aims was to determine which of the various lipophilic and hydrophilic suppository bases proved to be the best with respect to in vitro drug liberation. Among several experimental vehicles the Witepsol H 15 base with 10 of Miglyol 812 and the Macrogolum 1540 with 5% of Span 20 proved to be excellent. Furthermore, a well-known pharmacological effect of the paracetamol containing suppositories was evaluated in vivo in rats. The antipyretic response to the drug depends on the vehicle administered, showing an excellent correlation between in vitro and in vivo results.