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

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 anti-inflammatory 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 carrageenan-induced 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 microg mL(-1)) and AUC (12.67 +/- 2.97 microg 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.

Anti-ulcer activity of Cyrtocarpa procera analogous to that of Amphipterygium adstringens, both assayed on the experimental gastric injury in rats

“…A previous study corroborates the anti-ulcer activity of Amphipterygium adstringens in experimental models such as ethanol-induced gastric lesions in rats (Navarrete et al, 2005). It has also been described that Amphipterygium adstringens possesses anti-Helicobacter pylori (H. pylori) activity (Castillo-Juárez et al, 2007), an etiologic agent that plays an important role in the pathogenesis of peptic ulcer disease.…”

Contrasting effects of cord injury on intravenous and oral pharmacokinetics of diclofenac: a drug with intermediate hepatic extraction

“…14 Diclofenac concentration was determined in whole blood by an high-performance liquid chromatography method described previously. 18 For each animal, a diclofenac blood concentration curve against time was constructed. Pharmacokinetic parameters were estimated by non-compartmental analysis, as describe previously.…”

Acute toxicity and mutagenic activity of Mexican plants used in traditional medicine

“…Table 1 includes scientific names, common uses as well as pertinent references of previous chemical, pharmacological and/or clinical investigations, if any, on these plants. Anacardic acids, anacardic aldehydes, alkyl naphtalenes, triterpenoids and sterols Mata et al (1991), Mata (1993), Makino et al (2004), Oviedo-Chávez et al (2004), Rivero-Cruz et al (2005a) and Navarrete et al (2005) Brickellia veronicaefolia (Asteraceae)…”