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Gastroprotection and effect of the simultaneous administration of Cuachalalate ( Amphipterygium adstringens ) on the pharmacokinetics and anti-inflammatory activity of diclofenac in rats

2005; Oxford University Press; Volume: 57; Issue: 12 Linguagem: Inglês

10.1211/jpp.57.12.0013

2042-7158

Andrés Navarrete, María Elena Sánchez‐Mendoza, Jesús Arrieta, Leticia Cruz‐Antonio, Iván Oliva, Gilberto Castañeda‐Hernández,

Ginger and Zingiberaceae research

Abstract This work aimed to study the effect of Cuachalalate methanol extract (CME) on the anti-inflammatory activity and pharmacokinetics of diclofenac sodium, a frequently prescribed non-steroidal antiinflammatory drug (NSAID). The gastroprotective effect of CME on the gastric injury induced by diclofenac was studied in rats. CME showed a gastroprotective effect of 15.7% at 1 mg kg−1 and 72.5% at dose of 300 mg kg−1. Omeprazole, used as anti-ulcer reference drug, showed gastroprotective effects of 50–89.7% at doses tested (1–30 mg kg−1). The value of the 50% effective dose for the anti-inflammatory effect of diclofenac sodium (ED50 = 1.14 ± 0.23 mg kg−1) using carrageenaninduced rat paw oedema model, was not modified by the concomitant administration of 30 or 100 mg kg−1 of CME. The effect of CME (30, 100 and 300 mg kg−1, p.o.) on the pharmacokinetics of diclofenac sodium was studied. It was observed that the simultaneous administration of diclofenac sodium and 300 mg kg−1 of CME decreased significantly the values of Cmax (7.08 ± 1.42 μg mL−1) and AUC (12.67 ± 2.97 μg h mL−1), but not the value of tmax (0.13 (0.1–0.25) h) obtained with the administration of diclofenac alone. The simultaneous administration of 30 or 100 mg kg−1 of CME did not modify the pharmacokinetic parameters of diclofenac. The experimental findings in rats suggest that CME at doses lower than 100 mg kg−1 protects the gastric mucosa from the damage induced by diclofenac sodium without altering either the anti-inflammatory activity or the pharmacokinetics of this NSAID.