Next Article in Journal
Iontophoretic Transdermal Delivery of Human Growth Hormone (hGH) and the Combination Effect of a New Type Microneedle, Tappy Tok Tok®
Next Article in Special Issue
Pharmacokinetic Properties of Acetyl Tributyl Citrate, a Pharmaceutical Excipient
Previous Article in Journal
Development of Dual Drug Loaded Nanosized Liposomal Formulation by A Reengineered Ethanolic Injection Method and Its Pre-Clinical Pharmacokinetic Studies
Previous Article in Special Issue
Simultaneous Determination of Chlorogenic Acid Isomers and Metabolites in Rat Plasma Using LC-MS/MS and Its Application to A Pharmacokinetic Study Following Oral Administration of Stauntonia Hexaphylla Leaf Extract (YRA-1909) to Rats
Article Menu
Issue 3 (September) cover image

Export Article

Open AccessArticle
Pharmaceutics 2018, 10(3), 152;

Pharmacokinetics and Anti-Gastric Ulceration Activity of Oral Administration of Aceclofenac and Esomeprazole in Rats

College of Pharmacy, Catholic University of Daegu, Gyeongsan, Gyeongbuk 38430, Korea
College of Pharmacy, Wonkwang University, Iksan, Jeonbuk 54538, Korea
School of Pharmacy, Sungkyunkwan University, Suwon, Gyeonggi 16419, Korea
Korea United Pharm. Inc., Seoul 06116, Korea
Author to whom correspondence should be addressed.
Received: 13 August 2018 / Revised: 30 August 2018 / Accepted: 4 September 2018 / Published: 6 September 2018
(This article belongs to the Special Issue Drug Metabolism, Pharmacokinetics and Bioanalysis)
Full-Text   |   PDF [1231 KB, uploaded 6 September 2018]   |  


This study examined the effects of esomeprazole on aceclofenac pharmacokinetics and gastrointestinal complications in rats. Aceclofenac alone, or in combination with esomeprazole, was orally administered to male Sprague-Dawley rats. Plasma concentrations of aceclofenac, its major metabolite diclofenac, and esomeprazole were simultaneously determined by a novel liquid chromatography-tandem mass spectrometry method. Gastrointestinal damage was determined by measuring ulcer area and ulcer lesion index of the stomach. Oral administration of aceclofenac induced significant gastric ulceration, which was inhibited by esomeprazole administration. Following concurrent administration of aceclofenac and esomeprazole, overall pharmacokinetic profiles of aceclofenac and metabolic conversion to diclofenac were unaffected by esomeprazole. Aceclofenac metabolism and pharmacokinetics were not subject to significant food effects, whereas bioavailability of esomeprazole decreased in fed compared to fasting conditions. In contrast, the pharmacokinetics of aceclofenac and esomeprazole were significantly altered by different dosing vehicles. These results suggest that co-administration of esomeprazole with aceclofenac may reduce aceclofenac-induced gastrointestinal complications without significant pharmacokinetic interactions. The optimal combination and clinical significance of the benefits of the combination of aceclofenac and esomeprazole need to be further evaluated. View Full-Text
Keywords: aceclofenac; diclofenac; esomeprazole; pharmacokinetics; gastric ulcer aceclofenac; diclofenac; esomeprazole; pharmacokinetics; gastric ulcer

Graphical abstract

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

Share & Cite This Article

MDPI and ACS Style

Kim, T.H.; Thapa, S.K.; Lee, D.Y.; Chung, S.E.; Lim, J.Y.; Jeong, H.M.; Song, C.H.; Choi, Y.-W.; Cho, S.-M.; Nam, K.-Y.; Kang, W.-H.; Shin, S.; Shin, B.S. Pharmacokinetics and Anti-Gastric Ulceration Activity of Oral Administration of Aceclofenac and Esomeprazole in Rats. Pharmaceutics 2018, 10, 152.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Related Articles

Article Metrics

Article Access Statistics



[Return to top]
Pharmaceutics EISSN 1999-4923 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top