BIOAVAILABILITY OF IBUPROFEN FROM HARD GELATIN CAPSULES CONTAINING SUCRALFATE OR SODIUM ALGINATE AS DILUENT

The bioavailability of ibuprofen from two experimental hard gelatin ca psule formulations was evaluated in a single-dose (400 mg) study. The formulations contained sucralfate or sodium alginate as an additive in the capsule. Mean peak plasma levels of 30.3 +/- 9.5 mg . l-1 (mean /- S.D.) for the sucralfate-based capsules and 37.2 +/- 5.0 mg . l-1 f or the sodium alginate-based capsules were reached at 3.2 +/- 1.0 and 2.6 +/- 1.0 h, respectively. The individual plasma concentration profi les suggested a sustained-release action for the sucralfate-based caps ules, but a less pronounced sustained-release action for sodium algina te-based capsules, because of interindividual variation. The effect of concomitant administration of sucralfate and ibuprofen in separate do sage forms on the absorption of ibuprofen was also studied. The effect was dose-dependent. A dose of 1000 mg of sucralfate resulted in a sig nificant (p < 0.001) decrease in C(max) (26.6 +/- 7.9 mg . l-1) and in crease (p < 0.05 in t(max) (3.6 +/- 1.0 h) values as compared with val ues obtained with a smaller dose of 355 mg of sucralfate (C(max) 37.8 +/- 8.2 mg . l-1, t(max) 2.5 +/- 0.6 h). The smaller dose was, however , able as an additive in capsules to produce a sustained-release effec t, although one less pronounced than with concomitantly administered 1 000 mg of sucralfate. No differences were found in the amounts of ibup rofen absorbed between any of the dosage regimes studied.