Comparative pharmacokinetic analysis with two omeprazole formulations “Proceptin®” and “Losec®” in healthy subjects

Abstract

The pharmacokinetics of omeprazole pharmaceutical products Proceptin® 20mg capsule and Losec® 20mg MUPS tablet were compared in healthy subjects. The study was an open-­‐label, randomized, two-­‐treatment, two-sequence, two-way crossover, single-dose bioavailability study conducted under fasting conditions with a wash out period of seven days between the two administrations. Blood samples were collected pre-­‐dosing and at 0.5–24.0 h post administration of a single oral dose of either of the formulation followed by HPLC analysis. Twenty-eight healthy male subjects (20-­‐28 years) participated in the study. Only four subjects dropped from the study and the other 24 completed the study and were included in the pharmacokinetic and statistical analysis. Evaluated mean (±SD) values of prime pharmacokinetic parameters for reference and test products were C_max - 345.28 (±42.38) and 316.23 (±26.12) ng/mL, t_max - 2.28 (±0.16) and 2.69 (±0.23) h, AUC_0-­‐24 - 710.01 (±92.51) and 771.13 (±102.35) h-­‐ng/ml and AUC_0-­‐∞ - 848.21 (±65.31) and 902.56 (±45.23) h.ng/mL, respectively with no significant (p>0.05) differences in paired t-­‐test. Moreover, 90% CI for the AUC_0-­‐24, and C_max values were 89.245-­‐ 103.154% and 81.634-­‐102.211% respectively were within the predetermined FDA bioequivalence range of 80–125%. On the basis of the pharmacokinetic parameters AUC_0-­‐24, the relative bioavailability of the test preparation Proceptin 20 capsule was 108.61% of that of the reference preparation Losec 20mg MUPS tablet. This study stipulated that, the test and reference formulations of omeprazole meet the regulatory criteria for bioequivalence. Thus the test product Proceptin^® 20mg may be supplanted for reference product Losec^® 20mg MUPS tablet in oral administration.

KEY WORDS: Omeprazole; Cross-­‐over design; HPLC; Comparative pharmacokinetics