Scaled-up preparation of drug-loaded electrospun polymer fibres and investigation of their continuous processing to tablet form

EXPRESS POLYMER LETTERS(2018)

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摘要
Polymer-based electrospun amorphous solid dispersions (ASDs) were prepared and investigated from pharmaceutical application point of view. Spironolactone (SPIR) was used as model drug mixed in various concentrations with polymers suitable for fibre formation, such as vinylpyrrolidone-vinyl acetate copolymer, polyvinylpyrrolidone K30 and hydroxypropyl methylcellulose. Single needle electrospinning was applied at first for screening the composition of the prepared ASDs. Scaling-up the selected polymer-drug combination was accomplished by high speed electrospinning, the productivity of which enabled investigation of downstream processing to generate tablet formulation. The steps of a potential continuous production line (fibre collection, grinding, feeding and tableting) proved to be feasible with the electrospun ASD without any sign of crystallization. If crystalline drug was added into the ASD containing tablets as impurity strictly monotonous decrease of drug dissolution was observed in the function of the crystalline drug content. The capabilities of the non-destructive Raman and near-infrared spectroscopies, as fast quality assurance tools, were compared to each other in quantifying of crystalline SPIR content in the prepared tablets.
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关键词
industrial applications,high speed electrospinning,amorphous solid dispersions,tableting,continuous processing technologies
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