title: Esomeprazole immediate release tablets: Gastric mucosa ex vivo permeation, absorption and antisecretory activity in conscious rats.
abstract: The aim of this work was to study the esomeprazole activity on the control of gastric secretion after administration of a novel immediate release tablet. The ex vivo permeation of esomeprazole across porcine gastric mucosa from immediate release tablets, containing sodium carbonate or magnesium oxide as alkalinizing agents, was firstly assessed. Pharmacokinetics and pharmacodynamics studies in conscious rats following the administration of immediate release tablets with sodium carbonate, in comparison with delayed-release tablets having the same formula, were also conducted. The results showed an important effect of sodium carbonate and magnesium oxide on the drug release, on the ex vivo trans-mucosal transport and the stability in acid environment. In particular, the presence of sodium carbonate in esomeprazole tablet formulation provided the maximum increase of the drug in vitro transport across the mucosa. Then, the absorption and the antisecretory activity of this proton pump inhibitor orally administered in rats as immediate release tablets containing Na2CO3, was superior but not significantly different compared to delayed-release tablets having the same formula. In the adopted animal model, an activity of esomeprazole from immediate release alkaline formulation was seen also in presence of partial gastric absorption allowing inhibition of proton pumps reached via systemic circulation. This esomeprazole immediate release formulation could be used for the on-demand treatment of acid-related disorders such as gastro-esophageal reflux disease.
authors: Department of Pharmacy, University of Parma, Parco Area delle Scienze 27/A, 43124 Parma, Italy.
authors: Camillo
authors: C
authors: Benetti
authors: Department of Pharmacy, University of Parma, Parco Area delle Scienze 27/A, 43124 Parma, Italy.
authors: Lisa
authors: L
authors: Flammini
authors: Department of Pharmacy, University of Parma, Parco Area delle Scienze 27/A, 43124 Parma, Italy.
authors: Valentina
authors: V
authors: Vivo
authors: Department of Pharmacy, University of Parma, Parco Area delle Scienze 27/A, 43124 Parma, Italy.
authors: Paolo
authors: P
authors: Colombo
authors: Department of Life Sciences and Biotechnology, University of Ferrara, Via Fossato di Mortara 17/19, 44121 Ferrara, Italy.
authors: Gaia
authors: G
authors: Colombo
authors: Department of Pharmacy, University of Parma, Parco Area delle Scienze 27/A, 43124 Parma, Italy.
authors: Lisa
authors: L
authors: Elviri
authors: Department of Clinical & Experimental Medicine, University of Parma, Via Gramsci 14, 43126 Parma, Italy.
authors: Carmelo
authors: C
authors: Scarpignato
authors: Department of Pharmacy, University of Parma, Parco Area delle Scienze 27/A, 43124 Parma, Italy.
authors: Francesca
authors: F
authors: Buttini
authors: Department of Pharmacy, University of Parma, Parco Area delle Scienze 27/A, 43124 Parma, Italy.
authors: Ruggero
authors: R
authors: Bettini
authors: Department of Pharmacy, University of Parma, Parco Area delle Scienze 27/A, 43124 Parma, Italy.
authors: Elisabetta
authors: E
authors: Barocelli
authors: Department of Pharmacy, University of Parma, Parco Area delle Scienze 27/A, 43124 Parma, Italy. Electronic address: alessandra.rossi@unipr.it.
authors: Alessandra
authors: A
authors: Rossi
mesh_terms: D000818:Animals; D064098:Esomeprazole / Q000378:metabolism / Q000494:pharmacology*; D005260:Female; D065570:Gastric Absorption / Q000187:drug effects* / Q000502:physiology*; D005753:Gastric Mucosa / Q000187:drug effects* / Q000378:metabolism*; D008297:Male; D009924:Organ Culture Techniques; D054328:Proton Pump Inhibitors / Q000378:metabolism / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D013552:Swine; D013607:Tablets
chemical_list: D054328:Proton Pump Inhibitors; D013607:Tablets; D064098:Esomeprazole
keywords: Esomeprazole; Ex vivo permeability; Immediate release; Pharmacodynamics; Pharmacokinetics; Rats