The purpose of this study was to determine the pharmacokinetics and absolut
e bioavailability of cisapride after intravenous (i.v.) and intragastric (i
.g.) administration in healthy, adult horses. Five animals received single
doses of 0.1 mg/kg, 0.2 mg/kg and 0.4 mg/kg cisapride by the i.g, route in
an open, randomized fashion on different occasions separated by a washout p
eriod of at least 48 h. Four of these horses were also given a single i.v.
dose of 0.1 mg/kg cisapride. Jugular venous blood was collected periodicall
y up to 24 h after dosing. Plasma cisapride concentrations were measured by
high-performance liquid chromatography.
There was considerable inter individual variability in pharmacokinetic para
meters. The mean (SD) values for systemic clearance (Cl) and steady-state v
olume of distribution (Vss) were 494 (43.6) mL/h/kg and 1471 (578) mL/kg, r
espectively. Although the rate of cisapride absorption was quite rapid, onl
y about half the i.g, dose was absorbed systemically. The average terminal
half-life (t(1/2)) calculated over three i.g, doses was 2.06 h and that for
i.v. administration was 2.12 h. The pharmacokinetics of cisapride from 0.1
mg/kg to 0.4 mg/kg were independent of the i.g. dose.