title: Relative bioavailability of rafoxanide following intraruminal and intra-abomasal administration in sheep.
abstract: The bioavailability of rafoxanide was compared after intraruminal and intra-abomasal administration in healthy adult sheep (n = 6) in a single dose, 2 parallel group study at 7.5 mg/kg. Rafoxanide concentrations in plasma were measured by means of HPLC analysis. Primary pharmacokinetic parameters for bioavailability and disposition of rafoxanide in plasma for both routes of administration were determined by non-compartmental and non-linear, 1-compartmental pharmacokinetic analysis, respectively. Significantly (P < or = 0.05) higher peak plasma concentrations (c(max)) of rafoxanide and a more rapid rate of absorption (c. 3.5 times) was observed in sheep after intra-abomasal (i-a) administration compared to intraruminal (i.r.) administration. A significantly (P < or = 0.05) longer lag period (t(lag)) before absorption (6.8 +/- 2.9 h) occurred after i.r. than after i-a treatment (1.9 +/- 0.6 h). There was no significant difference (P > 0.05) in AUC, MRT and in the rates of elimination (k10-HL and t(1/2beta)) between the i.r. and i-a routes of administration. The results of the study demonstrated the important influence of the rumino-reticulum on absorption of rafoxanide in sheep.
authors.affiliation: Department of Pharmacology and Toxicology, Faculty of Veterinary Science, University of Pretoria, Onderstepoort, South Africa.
authors.forename: G E
authors.initials: GE
authors.lastname: Swan
authors.forename: H A
authors.initials: HA
authors.lastname: Koeleman
authors.forename: H S
authors.initials: HS
authors.lastname: Steyn
authors.forename: M S
authors.initials: MS
authors.lastname: Mülders
mesh_terms: D000018:Abomasum; D000042:Absorption; D000818:Animals; D000871:Anthelmintics / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D019540:Area Under Curve; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid; D004333:Drug Administration Routes / Q000662:veterinary; D005260:Female; D008297:Male; D011888:Rafoxanide / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D011897:Random Allocation; D012417:Rumen; D012756:Sheep / Q000378:metabolism*; D013997:Time Factors
chemical_list: D000871:Anthelmintics; D011888:Rafoxanide