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Pharmaceutics 2018, 10(3), 152; https://doi.org/10.3390/pharmaceutics10030152

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

1
College of Pharmacy, Catholic University of Daegu, Gyeongsan, Gyeongbuk 38430, Korea
2
College of Pharmacy, Wonkwang University, Iksan, Jeonbuk 54538, Korea
3
School of Pharmacy, Sungkyunkwan University, Suwon, Gyeonggi 16419, Korea
4
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)
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Abstract

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
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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).
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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.

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