TRIALS OF IN-SITU GELLING AND MUCOADHESIVE ACETAMINOPHEN LIQUID SUPPOSITORY IN HUMAN-SUBJECTS

For the development of in-situ gelling and mucoadhesive acetaminophen liquid suppository prepared with poloxamers (P 407, P 188) and sodium alginate, the physicochemical characteristics of liquid suppositories [acetaminophen/P 407/P 188/sodium alginate (5/15/19/0-1.0%)] were eval uated. Furthermore, a pharmacokinetic study of acetaminophen from liqu id and conventional solid suppositories in human subjects was carried out. The results showed that acetaminophen liquid suppository [acetami nophen/P 407/P 188/sodium alginate (5/15/19/0.6%)] with optimal gelati on temperature, gel strength and bioadhesive force had a similar relea se pattern to conventional suppository, The area under the drug concen tration-time curve (AUC), mean residence time (MRT), biological half-l ife (t(1/2)) and apparent elimination rate constant (K-el) of acetamin ophen from liquid suppository were not significantly different from th ose from conventional suppository. However, liquid suppository gave si gnificantly faster the time to reach the maximum plasma concentration (T-max) and higher the maximum plasma concentration of drug (C-max) of acetaminophen than conventional suppository (p < 0.05). It is conclud ed that in situ gelling and mucoadhesive acetaminophen liquid supposit ory, which was easy to administer to the anus and showed faster absorp tion of acetaminophen in human subjects than conventional suppository, was more comfortable for the patients and therefore, is thought to be a favorable anti-pyretic and analgesic dosage form for infants and ch ildren. (C) 1998 Elsevier Science B.V. All rights reserved.