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Drug Res (Stuttg) 2013; 63(07): 370-375
DOI: 10.1055/s-0033-1341477
Original Article
© Georg Thieme Verlag KG Stuttgart · New York

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

Z. Liu
1   Department of pharmaceutical analysis, China Pharmaceutical University, Tongjiaxiang, Nanjing, China
,
L. Ding
1   Department of pharmaceutical analysis, China Pharmaceutical University, Tongjiaxiang, Nanjing, China
,
S. Zhong
1   Department of pharmaceutical analysis, China Pharmaceutical University, Tongjiaxiang, Nanjing, China
,
X. Cao
2   Department of pharmacology, Jinling Hospital, Nanjing University, East Zhongshan Road, Nanjing, China
,
L. Jiang
1   Department of pharmaceutical analysis, China Pharmaceutical University, Tongjiaxiang, Nanjing, China
,
H. Duan
1   Department of pharmaceutical analysis, China Pharmaceutical University, Tongjiaxiang, Nanjing, China
› Author Affiliations
Further Information

Publication History

received 19 November 2012

accepted 11 March 2013

Publication Date:
04 April 2013 (online)

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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 AUC0–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 AUC0–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 (AUC0–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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