Bioequivalence between omeprazole MUPS 20 mg as tablet and omeprazole MUPS 20 mg as tablet encapsulated in a hard gelatine capsule.
OBJECTIVE
To investigate pharmacokinetic characteristics of omeprazole MUPS 20 mg tablets and its encapsulated form.


METHODS
Bioequivalence of omeprazole MUPS 20 mg tablet (Reference) and omeprazole MUPS 20 mg tablet in a hard gelatine capsule (Test) was evaluated in a randomized, 2-period crossover study in 38 healthy male Caucasian subjects who received a single oral dose of 20 mg omeprazole in each study period. Serum concentrations of omeprazole MUPS 20 mg were measured using an HPLC assay. In addition, in vitro dissolution profiles were studied.


RESULTS
Both formulations were bioequivalent as assessed by the primary pharmacokinetic characteristics AUC(0-infinity) and Cmax, the corresponding ratios (Test/Reference) being 0.97 and 0.98, respectively. Thus, the 90% CI of these ratios were within the equivalence range of 0.8 to 1.25 for AUC(0-infinity) (CI 0.90-1.04) and 0.67 to 1.50 for Cmax (Cl 0.86-1.10). The ratios of the secondary criteria, Cmax/AUC(0-infinity) and t 1/2, were also within the equivalence range. Median tmax of Reference and Test was identical. Both formulations revealed comparable dissolution profiles with high batch conformity and homogeneity releasing > 80% omeprazole within 1 hour. Both study formulations were well tolerated without relevant differences.


CONCLUSIONS
The encapsulation of omeprazole MUPS 20 mg tablets does not influence the extent and rate of absorption as indicated by the AUC and Cmax ratios. Thus, bioequivalence could be demonstrated.
Schaltenbrand
R
R
Institute for Research and Development, University of Witten/Herdecke, Germany. office@ife-europe.com
Huber
R
R
Cotoraci
C A
CA
Mascher
H
H
Potthast
H
H
Hole
U
U
D000328:Adult; D000897:Anti-Ulcer Agents / Q000097:blood / Q000493:pharmacokinetics*; D019540:Area Under Curve; D002626:Chemistry, Pharmaceutical; D018592:Cross-Over Studies; D006207:Half-Life; D006801:Humans; D007408:Intestinal Absorption; D008297:Male; D009853:Omeprazole / Q000097:blood / Q000493:pharmacokinetics*; D013608:Tablets, Enteric-Coated; D013810:Therapeutic Equivalency
D000897:Anti-Ulcer Agents; D013608:Tablets, Enteric-Coated; D009853:Omeprazole