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Preparation and Characterization of Highly Porous Direct Compression Carrier Particles with Improved Drug Loading During an Interactive Mixing Process

  • Research Article
  • Theme: Advanced Technologies for Oral Controlled Release
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Abstract

The aim of this study was to prepare highly porous carrier particles by emulsion solvent evaporation and compare the loading capacity of these beads with two traditional carriers, sugar beads, and microcrystalline cellulose granules during an interactive mixing process. The porous carrier particles were prepared by an emulsion solvent evaporation process using cellulose propionate as a binder, anhydrous dibasic calcium phosphate, and ion exchange resins as a fillers, and polyethylene glycol as a pore inducer. Micronized furosemide or griseofulvin powder was mixed with the same volume of each carrier in an interactive mixing process. The tableting properties, drug loading per unit volume of carrier, content uniformity of the mixtures, and dissolution of the drugs from the mixtures were measured. The results showed that highly porous microcapsules with desirable hardness equivalent to that of sugar beads and MCC granules were successfully prepared. On average the loading capacity of the new carrier was 310% that of sugar beads and 320% that of MCC granules during an interactive mixing process with very good content uniformity. The tableting properties of the microcapsules were equivalent to that of microcrystalline cellulose granules, and the dissolution of the drugs from interactive mixtures prepared with the new carrier was equivalent to that of drug suspensions. This showed that the prepared microcapsule carrier could be used to improve the loading capacity during an interactive mixing and to prepare tablets by direct compression.

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Acknowledgment

We are grateful to the University of Wisconsin (USA) and the North-West University (RSA) for research support.

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Authors and Affiliations

  1. School of Pharmacy, University of Wisconsin-Madison, 777 Highland Avenue, Madison, Wisconsin, 53705-2222, USA

    Mingna Song, Ning Li & Melgardt M. de Villiers

  2. College of Pharmacy, University of Louisiana at Monroe, Monroe, Louisiana, 71209, USA

    Mingna Song & Michael D. Degennaro

  3. Laboratory for Electron Microscopy, Faculty of Natural Sciences, North-West University, Potchefstroom, 2520, South Africa

    Louwrens R. Tiedt

Authors
  1. Mingna Song
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  2. Ning Li
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  3. Louwrens R. Tiedt
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  4. Michael D. Degennaro
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  5. Melgardt M. de Villiers
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Correspondence to Melgardt M. de Villiers.

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Guest Editors: Michael Repka, Joseph Reo, Linda Felton, and Stephen Howard

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Song, M., Li, N., Tiedt, L.R. et al. Preparation and Characterization of Highly Porous Direct Compression Carrier Particles with Improved Drug Loading During an Interactive Mixing Process. AAPS PharmSciTech 11, 698–707 (2010). https://doi.org/10.1208/s12249-010-9426-8

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  • DOI: https://doi.org/10.1208/s12249-010-9426-8

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