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Structured Development Approach for Amorphous Systems

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Formulating Poorly Water Soluble Drugs

Part of the book series: AAPS Advances in the Pharmaceutical Sciences Series ((AAPS,volume 3))

Abstract

A structured development approach is presented to guide the development of stable and commercially viable amorphous formulations. The proposed approach should not only enable the delivery of poorly soluble drugs but also help reduce the API needs, reduce in vivo screening, minimize risks for late-stage development, and ensure consistent quality. During initial assessment, a guided evaluation of the physicochemical properties of the API helps to assess the degree of difficulty for the development. A range of tests including in silico evaluation, high-throughput screening assays, and miniaturized screening tools provide a road map for selecting the appropriate polymer, drug loading, and suitable manufacturing process. A dedicated section provides a review of the characterization tools to assess and quantify the crystallinity, understanding the phase behavior of amorphous solid dispersion, and designing the in vitro dissolution methods. Finally, a reference chart is provided that summarizes the key concepts proposed as part of the structured development approach that can serve as a blueprint for the development of amorphous formulations.

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Authors and Affiliations

  1. Pharmaceutical and Analytical Research and Development, Hoffman-La Roche, Inc., 340 Kingsland Street, Nutley, NJ, 07110-1199, USA

    Navnit Shah, Harpreet Sandhu & Duk Soon Choi

  2. F. Hoffmann-La Roche AG, Grenzacherstrasse 124, 4070, Basle, Switzerland

    Oskar Kalb, Susanne Page & Nicole Wyttenbach

Authors
  1. Navnit Shah
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  2. Harpreet Sandhu
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  3. Duk Soon Choi
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  4. Oskar Kalb
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  5. Susanne Page
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  6. Nicole Wyttenbach
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Correspondence to Navnit Shah .

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Editors and Affiliations

  1. , Division of Pharmacy, University of Texas at Austin, Mailstop A1920, Austin, 78712, USA

    Robert O. Williams III

  2. College of Pharmacy, Drug Dynamics Institute, University of Texas, Austin, 78712, Texas, USA

    Alan B. Watts

  3. , Pharmaceutical and Analytical R&D, Hoffmann-La Roche, Inc., Kingsland St 340, Nutley, 07110, USA

    Dave A. Miller

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© 2012 American Association of Pharmaceutical Scientists

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Shah, N., Sandhu, H., Choi, D.S., Kalb, O., Page, S., Wyttenbach, N. (2012). Structured Development Approach for Amorphous Systems. In: Williams III, R., Watts, A., Miller, D. (eds) Formulating Poorly Water Soluble Drugs. AAPS Advances in the Pharmaceutical Sciences Series, vol 3. Springer, New York, NY. https://doi.org/10.1007/978-1-4614-1144-4_8

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