title: Evaluation of pantoprazole formulations in different dissolution apparatus using biorelevant medium.
abstract: OBJECTIVE
  The study was developed to compare the in vitro dissolution profiles of pantoprazole (CAS 102625-70-7) formulations in both The United States Pharmacopeia (USP) apparatus 2 and 3 by applying biorelevant medium. Moreover, an in vitro-in vivo relationship was proposed considering in vivo data from a previously published study.
  
  
  METHODS
  In vitro dissolution profiles were evaluated in biorelevant medium in USP apparatus 2 and 3 and the dissolution curves were either compared by the similarity factor (f2) or a model-independent approach. The fraction of drug dissolved in vitro in apparatus 2 was compared with the fraction of drug absorbed in vivo, which was obtained from a retrospective in vivo study. An in vitro-in vivo relationship analysis was then applied to elucidate the overall absorption characteristics of formulations.
  
  
  RESULTS
  The dissolution profiles of formulations demonstrated similar disposition in biorelevant medium in both USP apparatus 2 and 3. The dissolution profiles were described by f2 model in apparatus 2 and Weibull's function in apparatus 3. The vitro-in vivo relationship analysis showed that the formulations exhibited permeability rate-limiting absorption.
  
  
  CONCLUSIONS
  Biorelevant medium in both USP apparatus 2 and 3 may be used as a tool to predict in vivo disposition of formulations of pantoprazole. Furthermore, it can be argued that biowaiver can be granted for enteric coated formulations of pantoprazole on the basis of in vitro dissolution profile.
authors.affiliation: Clinical Pharmacology and Gastroenterology Unit, São Francisco University Medical School, Braganga Paulista, SP, Brazil. cinetica04@yahoo.com.br
authors.forename: Daniel Rossi
authors.initials: DR
authors.lastname: de Campos
authors.forename: Sandra
authors.initials: S
authors.lastname: Klein
authors.forename: Thomas
authors.initials: T
authors.lastname: Zoller
authors.forename: Nelson Rogério
authors.initials: NR
authors.lastname: Vieria
authors.forename: Fábio Alessandro Proença
authors.initials: FA
authors.lastname: Barros
authors.forename: Eduardo César
authors.initials: EC
authors.lastname: Meurer
authors.forename: Edvaldo Capobiango
authors.initials: EC
authors.lastname: Coelho
authors.forename: Marco Antônio
authors.initials: MA
authors.lastname: Marchioretto
authors.forename: José
authors.initials: J
authors.lastname: Pedrazzoli
mesh_terms: D053799:2-Pyridinylmethylsulfinylbenzimidazoles / Q000008:administration & dosage / Q000737:chemistry*; D019540:Area Under Curve; D002626:Chemistry, Pharmaceutical; D002851:Chromatography, High Pressure Liquid; D018592:Cross-Over Studies; D004311:Double-Blind Method; D005079:Excipients; D006207:Half-Life; D006801:Humans; D007700:Kinetics; D000077402:Pantoprazole; D054328:Proton Pump Inhibitors / Q000008:administration & dosage / Q000737:chemistry*; D012189:Retrospective Studies; D012995:Solubility; D013608:Tablets, Enteric-Coated
chemical_list: D053799:2-Pyridinylmethylsulfinylbenzimidazoles; D005079:Excipients; D054328:Proton Pump Inhibitors; D013608:Tablets, Enteric-Coated; D000077402:Pantoprazole