Comparison of total oral bioavailability and the lymphatic transport of halofantrine from three different unsaturated triglycerides in lymph-cannulated conscious rats

The lymphatic transport and the portal absorption of the lipophilic drug ha lofantrine were investigated in a conscious rat model. The rats were dosed with 0.1 g with triolein, trilinolein or trilinolenin containing 2 mg halof antrine. Following oral administration of the triglycerides, the mesenteric lymph and plasma samples were collected. The lymphatic transport for halof antrine was 11.1 +/-1.2 after administration of trilinolein, 9.0 +/-3.5 for trilinolenin and 8.6 +/-2.2 for triolein and the total amount of halofantr ine transported in the lymph was linear proportional with the amount of tri glyceride in the lymph. The absorption of halofantrine directly into the bl ood showed a trend towards a higher AUC for trilinolien and trilinolenin co mpared to triolein, but no statistical difference could be found. The stati stically analysis of the mean total bioavailability therefore shows that th e absorption of halofantrine was largely independent on triglyceride unsatu ration. (C) 2001 Elsevier Science B.V. All rights reserved.