Abstract
The effect of oral administration of the anion exchange resins colestipol hydrochloride (10 g) or cholestyramine (8 g) on the systemic clearance and other pharmacokinetic parameters of intramuscularly administered ketoprofen (50 mg) has been studied in six healthy male subjects. The study was performed according to a randomized three-way crossover design with a 1 week washout period between each treatment phase. After dosing, serial blood samples were collected for a period of 8 h. Plasma harvested from blood was analyzed for ketoprofen by a sensitive high-performance liquid Chromatographie assay. Cholestyramine administration resulted in a significant reduction in ketoprofen plasma concentrations. No significant differences between colestipol-treated and control groups were observed in the calculated pharmacokinetic parameters (Cl, AUC,
K
el
, t
1
2
and MRT). Cholestyramine treatment resulted in a significant increase in the
K
el (55%,
p < 0.01), and Cl (32%,
p < 0.005) and a significant decrease in the AUC (24%,
p < 0.001),
t
1
2
(33%, p < 0.01)
and MRT (30%,
p < 0.001). These results indicate an enhancement of ketoprofen elimination following cholestyramine administration and a lack of interaction between colestipol and ketoprofen.