The disposition of the hypolipidemic agent, o-(N-phthalimido)acetophenone, in Sprague-Dawley rats.
Disposition studies of the potent experimental hypolipidemic agent, o-(N-phthalimido)acetophenone, were conducted in the laboratory rat. Intravenous administration of the drug demonstrated a declining biphasic plasma concentration-time curve suggesting a rapid distribution into tissues. Less than 5% of the intravenous dose was recovered in urine and feces after 5 days. Oral administration of the drug showed that the maximum blood levels were attained within 15 min. After 48 hr, 92% of the orally administered 14C dose was eliminated either via urine (60%) or feces (40%). 14C in a 0-24-hr urine collection after oral administration showed that urinary radioactivity was composed of 22% of the parent compound o-(N-phthalimido) acetophenone, a benzoic acid metabolite (22%) o-(N-phthalimido)benzoic acid, and an amic acid metabolite (56%) N-(o-acetophenone)phthalamic acid. The two metabolites were unconjugated and possessed less hypolipidemic activity than the parent drug.
D000098:Acetophenones / Q000378:metabolism / Q000493:pharmacokinetics*; D000818:Animals; D001711:Biotransformation; D005243:Feces / Q000032:analysis; D005753:Gastric Mucosa / Q000378:metabolism; D006207:Half-Life; D000960:Hypolipidemic Agents / Q000378:metabolism / Q000493:pharmacokinetics*; D066298:In Vitro Techniques; D007275:Injections, Intravenous; D007408:Intestinal Absorption; D008297:Male; D010797:Phthalimides / Q000378:metabolism / Q000493:pharmacokinetics*; D051381:Rats; D011919:Rats, Inbred Strains
D000098:Acetophenones; D000960:Hypolipidemic Agents; D010797:Phthalimides; C056304:O-(N-phthalimido)acetophenone