In silico and in vitro methods to optimize the performance of experimental gastroretentive floating mini-tablets

Veronika A. Eberle, Armella Häring, Joachim Schoelkopf, Patrick A. C. Gane, Jörg Huwyler, Maxim Puchkov

    Research output: Contribution to journalArticleScientificpeer-review

    8 Citations (Scopus)

    Abstract

    Context: 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.

    Materials and 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.

    Results and discussion: 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.

    Conclusion: 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.

    Original languageEnglish
    Pages (from-to)808-817
    Number of pages10
    JournalDRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
    Volume42
    Issue number5
    DOIs
    Publication statusPublished - 3 May 2016
    MoE publication typeA1 Journal article-refereed

    Keywords

    • mini-tablet formulations
    • flotation
    • floating force
    • Drug release
    • functionalized calcium carbonate
    • DRUG-DELIVERY SYSTEMS
    • DOSAGE FORMS
    • GASTRIC RETENTION
    • RELEASE CHARACTERISTICS
    • CALCIUM-CARBONATE
    • MICROSPHERES
    • BEHAVIOR
    • POLYMER
    • INVIVO
    • VIVO

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