Esomeprazole MUPS 40 mg tablets and esomeprazole MUPS 40 mg tablets encapsulated in hard gelatine are bioequivalent.
OBJECTIVE
To investigate the bioequivalence of esomeprazole MUPS 40 mg tablets administered with and without a hard gelatine capsule.


METHODS
Bioequivalence of the esomeprazole MUPS 40 mg tablet administered without (Reference) and with a hard gelatine capsule (Test) was evaluated using a randomized, two-period crossover study. In each study period 49 healthy male Caucasian subjects received a single oral dose of 40 mg esomeprazole. Blood samples were collected at specified time intervals, and serum was separated and analyzed for esomeprazole concentrations using a validated HPLC-MS method. The primary parameters were AUC (extent of absorption) and Cmax (rate of absorption). The time-to-peak plasma concentration, tmax, and the elimination half-life, t1/2, were determined as secondary characteristics. Point estimates and 90%-confidence intervals were obtained for the ratio of the population medians of Test and Reference, using a multiplicative model and a parametric analysis except in the case of tmax, where an additive model and a non-parametric analysis was used. Bioequivalence of Test and Reference was concluded if the 90%-confidence intervals were entirely within the predefined equivalence ranges.


RESULTS
The AUC(0-infinity) and Cmax-ratios (Test/Reference) were 1.00 and 1.01, respectively. The 90%-confidence intervals for AUC(0-infinity) (0.94-1.06) and Cmax (0.93-1.09) of these ratios were within the predefined equivalence range of 0.80-1.25 and 0.75-1.33, respectively. The ratios and 90%-confidence intervals of the secondary characteristics t1/2 and tmax were also within the respective predefined equivalence ranges. Both esomeprazole formulations were well tolerated and safe.


CONCLUSIONS
The encapsulation of esomeprazole MUPS 40 mg tablets does not influence the extent and rate of absorption assessed by using AUC(0-infinity) and Cmax. Thus, bioequivalence could be demonstrated.
Talpes
S
S
ALTANA Pharma AG, Konstanz, Germany.
Knoerzer
D
D
Huber
R
R
Pfaffenberger
B
B
D000042:Absorption; D000284:Administration, Oral; D000293:Adolescent; D000328:Adult; D000897:Anti-Ulcer Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D019540:Area Under Curve; D002214:Capsules; D002626:Chemistry, Pharmaceutical; D018592:Cross-Over Studies; D064098:Esomeprazole / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D005780:Gelatin; D006801:Humans; D008297:Male; D013607:Tablets; D013810:Therapeutic Equivalency
D000897:Anti-Ulcer Agents; D002214:Capsules; D013607:Tablets; D005780:Gelatin; D064098:Esomeprazole