title: In silico and in vitro methods to optimize the performance of experimental gastroretentive floating mini-tablets.
abstract: BACKGROUND
  Development of floating drug delivery systems (FDDS) is challenging. To facilitate this task, an evaluation method was proposed, which allows for a combined investigation of drug release and flotation.
  
  
  OBJECTIVE
  It was the aim of the study to use functionalized calcium carbonate (FCC)-based lipophilic mini-tablet formulations as a model system to design FDDS with a floating behavior characterized by no floating lag time, prolonged flotation and loss of floating capability after complete drug release.
  
  
  METHODS
  Release of the model drug caffeine from the mini-tablets was assessed in vitro by a custom-built stomach model. A cellular automata-based model was used to simulate tablet dissolution. Based on the in silico data, floating forces were calculated and analyzed as a function of caffeine release.
  
  
  CONCLUSIONS
  Two floating behaviors were identified for mini-tablets: linear decrease of the floating force and maintaining of the floating capability until complete caffeine release. An optimal mini-tablet formulation with desired drug release time and floating behavior was developed and tested.
  
  
  CONCLUSIONS
  A classification system for a range of varied floating behavior of FDDS was proposed. The FCC-based mini-tablets had an ideal floating behavior: duration of flotation is defined and floating capability decreases after completion of drug release.
authors: a Department of Pharmaceutical Sciences, Division of Pharmaceutical Technology , University of Basel , Klingelbergstrasse , Basel , Switzerland .
authors: Veronika A
authors: VA
authors: Eberle
authors: a Department of Pharmaceutical Sciences, Division of Pharmaceutical Technology , University of Basel , Klingelbergstrasse , Basel , Switzerland .
authors: Armella
authors: A
authors: Häring
authors: b Omya International AG , Oftringen , Switzerland , and.
authors: Joachim
authors: J
authors: Schoelkopf
authors: c School of Chemical Technology, Aalto University , Aalto , Helsinki , Finland.
authors: Patrick A C
authors: PA
authors: Gane
authors: a Department of Pharmaceutical Sciences, Division of Pharmaceutical Technology , University of Basel , Klingelbergstrasse , Basel , Switzerland .
authors: Jörg
authors: J
authors: Huwyler
authors: a Department of Pharmaceutical Sciences, Division of Pharmaceutical Technology , University of Basel , Klingelbergstrasse , Basel , Switzerland .
authors: Maxim
authors: M
authors: Puchkov
mesh_terms: D002110:Caffeine / Q000737:chemistry; D002119:Calcium Carbonate / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003198:Computer Simulation; D003692:Delayed-Action Preparations / Q000737:chemistry*; D016503:Drug Delivery Systems / Q000379:methods; D065546:Drug Liberation; D005079:Excipients / Q000737:chemistry; D005753:Gastric Mucosa / Q000378:metabolism*; D066298:In Vitro Techniques / Q000379:methods*; D012995:Solubility; D013607:Tablets / Q000737:chemistry*; D013678:Technology, Pharmaceutical / Q000379:methods*
chemical_list: D003692:Delayed-Action Preparations; D005079:Excipients; D013607:Tablets; D002110:Caffeine; D002119:Calcium Carbonate
keywords: Drug release; floating force; flotation; functionalized calcium carbonate; mini-tablet formulations