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International Journal of Pharmacology
  Year: 2020 | Volume: 16 | Issue: 4 | Page No.: 375-381
DOI: 10.3923/ijp.2020.375.381
 
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Pharmacokinetics Effect of Diclofenac or Ketorolac-methyl Eugenol and Their Implication in the Gastroprotection

Leticia Cruz-Antonio, María Elena Sánchez-Mendoza, Yaraset López-Lorenzo, Héctor Isaac Rocha-González, Aida Robles-Sánchez and Jesús Arrieta

Abstract:
Background and Objective: Gastric ulcers are a global health problem, in part caused by the frequent administration of NSAIDs. To reduce gastrointestinal damage, these drugs are often co-administered with gastroprotective agents, which also have severe adverse effects. The objective of this study was to evaluate the protective activity of methyl eugenol against diclofenac- and ketorolac-induced gastric damage and explore the pharmacokinetics of a possible drug interaction of the combined treatments. Materials and Methods: Rats were orally administered methyl eugenol at different doses and 1 h later given diclofenac (80 mg kg1) or ketorolac (35 mg kg1). The control groups were treated with diclofenac or ketorolac only. After 4 or 6 h, respectively, the animals were sacrificed and the stomachs removed. Gastric damage was quantified to calculate the percentage of gastroprotection. Additionally, a pylorus ligation was performed to test for an anti-secretory effect of methyl eugenol. Other animals received 10 mg kg1 of diclofenac or ketorolac with or without methyl eugenol co-administration (100 mg kg1) to analyze possible drug interactions. The plasma concentrations of diclofenac and ketorolac were determined by HPLC and pharmacokinetics parameters were assessed. Results: Methyl eugenol decreased gastric lesions induced by diclofenac and ketorolac, achieving the maximum protection of 74.4 and 49.0%, respectively, at 100 mg kg1. No anti-secretory activity was detected. With the co-administration of methyl eugenol, the bioavailability of diclofenac was unchanged but that of ketorolac declined. Conclusion: Methyl eugenol provided greater protection against diclofenac- than ketorolac-induced gastric lesions. It affected the bioavailability of ketorolac (due to alterations in absorption) but not that of diclofenac.
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How to cite this article:

Leticia Cruz-Antonio, María Elena Sánchez-Mendoza, Yaraset López-Lorenzo, Héctor Isaac Rocha-González, Aida Robles-Sánchez and Jesús Arrieta, 2020. Pharmacokinetics Effect of Diclofenac or Ketorolac-methyl Eugenol and Their Implication in the Gastroprotection. International Journal of Pharmacology, 16: 375-381.

DOI: 10.3923/ijp.2020.375.381

URL: https://scialert.net/abstract/?doi=ijp.2020.375.381

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