Pharmacokinetics of a New Immediate-release Compound Omeprazole Capsule and its Comparison with the Enteric-coated Formulation under Fasting and Fed Conditions

Abstract

Background and Aims:

The present study was conducted to describe the pharmacokinetic profile of immediate-release compound omeprazole capsule and compare it with the enteric-coated formulation under fasting and fed condition.

Methods:

This study was designed to phase I, open-label, randomized, 3-part clinical trial. 12 subjects in part one received single doses (20 mg and 40 mg) and repeated doses (20 mg). Different 30 subjects in part 2 (fasting condition) and part 3 (fed condition) received either compound omeprazole capsule (40 mg) or delayed-release omeprazole (40 mg) separated by 7 days.

Results:

Compound omeprazole capsule showed dose non-proportionality in the range from 20 mg to 40 mg. The AUC_0–t of 20 mg omeprazole is 78% higher after repeated doses. The C _max was higher and T _max was lower for compound omeprazole capsule than delayed-release omeprazole. 90% CIs for AUC_0–t of the 2 periods (test/reference) under fasting and fed conditions were 106.3% (102.2%~109.2%) and 104.1% (93.4%~109.6%), respectively. Presence of food reduced the rate (C _max) and extent (AUC_0–t) of systemic exposure of the test and reference formulations from 1 462 to 777 ng · mL⁻¹, 1 055 to 602 ng · mL⁻¹, 2 597 to 1 852 ng · h · mL⁻¹ and 2 454 to 1 873 ng · h · mL⁻¹, respectively.

Conclusions:

Exposed dose of omeprazole in subjects with compound omeprazole capsule was time- and dose-dependent. Compared with delayed-release omeprazole, compound omeprazole capsule had rapid but similar degree of absorption of omeprazole.

Key words

pharmacokinetics - omeprazole - non-proportionality - CYP2C19 - food

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