Comparative bioavailability of a cisapride suppository and tablet formulation in healthy volunteers.
The comparative bioavailability of cisapride as a 30 mg suppository and three 5 mg oral tablets was investigated in 12 non-smoking, healthy male volunteers. The two formulations were administered on two separate occasions following an overnight fast, according to a randomized cross-over design. The plasma concentration of cisapride was measured over 48 h after drug administration. The 30 mg suppository exhibited a mean time to the peak plasma concentration of 3.8 h, while the tablets showed a significantly earlier peak time of 1.5 h. The maximum plasma concentration of cisapride after the 30 mg suppository (50.3 ng.ml-1) was significantly lower than after the tablets (74.3 ng.ml-1). The AUCs following the two treatments did not differ significantly from each other. The comparative bioavailability of the 30 mg cisapride suppository in relation to the three 5 mg oral tablets was 85%, with a 95%-confidence interval of 67% to 102% (not adjusted for dose). Normalizing the mean AUC by dose, the relative bioavailability of the suppository was 43% of that of the tablet. The elimination half-life of cisapride was not significantly different following the administration of the two formulations (9.3 h for the suppository and 9.8 h for the tablet).
Hedner
T
T
Department of Clinical Pharmacology, Sahlgren's University Hospital, Göteborg, Sweden.
Hedner
J
J
Gelin-Friberg
A
A
Huang
M L
ML
Van de Poel
S
S
Woestenborghs
R
R
Van Peer
A
A
Heykants
J
J
D000328:Adult; D001682:Biological Availability; D020117:Cisapride; D006207:Half-Life; D006801:Humans; D008297:Male; D010880:Piperidines / Q000008:administration & dosage / Q000493:pharmacokinetics*; D011897:Random Allocation; D013488:Suppositories; D013607:Tablets
D010880:Piperidines; D013488:Suppositories; D013607:Tablets; D020117:Cisapride