Pharmacokinetics of meloxicam administered as regular and fast dissolving formulations to the rat: influence of gastrointestinal dysfunction on the relative bioavailability of two formulations

European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V
Ali Aghazadeh-Habashi, Fakhreddin Jamali

Abstract

It is believed that acute pain suppresses nervus vagus, thereby, influencing gastrointestinal secretion and motility, which are the two factors that are necessary for disintegration and dissolution of solid dosage forms. We studied the pharmacokinetics of meloxicam and the effect of vagal suppression on the oral bioavailability and bioequivalence using a marketed (Brand) and a fast dissolving (FD) formulation. In simulated gastric juice, FD was disintegrated in 30s and released 30% of its meloxicam in 15 min and 60% in 2h. Brand was disintegrated in 4.5 min with a dissolution rate of 5.6% in 30 min that stayed plateau for the 2h experiment time. To suppress the vagus nerve, intraperitoneal injection of 20mg/kg propantheline 1 and 2h before meloxicam administration was used. Meloxicam (0.9 mg/kg) was administered to both control and vagally suppressed rats i.v. (n=4-6/group) as well as orally in a paired random fashion as broken pieces of Brand or FD tablets (n=7/ group). Serial (0-48h) blood samples were collected for pharmacokinetic and bioavailability studies. Relative bioavailability was measured according to a method in use for bioequivalence assessments. Systemic pharmacokinetics of meloxicam was not affected by vagal supp...Continue Reading

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Citations

Dec 25, 2012·Archives of Pharmacal Research·Dixit Anil Satyanarayana, Kulkarni Parthasarathi Keshavarao
Jan 12, 2016·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·May AlmukainziRaimar Löbenberg
Sep 1, 2011·International Journal of Pharmaceutics·Jianjun ZhangYuan Gao
Jan 8, 2020·Nature Reviews. Disease Primers·Asbjørn M DrewesSøren S Olesen

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