An attempt was made to optimize the rectal delivery of acetaminophen (parac
etamol). One of the aims was to determine which of the various lipophilic a
nd hydrophilic suppository bases proved to be the best with respect to in v
itro 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 pro
ved to be excellent. Furthermore, a well-known pharmacological effect of th
e paracetamol containing suppositories was evaluated in vivo in rats. The a
ntipyretic response to the drug depends on the vehicle administered, showin
g an excellent correlation between in vitro and in vivo results.