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Effects of the Preparation Process on the Properties of Amorphous Solid Dispersions

  • Review Article
  • Theme: Applications of KinetiSol® for Advanced Amorphous Solid Dispersions
  • Published:
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Abstract

The use of amorphous solid dispersions to improve the bioavailability of active ingredients from the BCS II and IV classifications continues to gain interest in the pharmaceutical industry. Over the last decade, methods for generating amorphous solid dispersions have been well established in commercially available products and in the literature. However, the amorphous solid dispersions manufactured by different technologies differ in many aspects, primarily chemical stability, physical stability, and performance, both in vitro and in vivo. This review analyzes the impact of manufacturing methods on those properties of amorphous solid dispersions. For example, the chemical stability of drugs and polymers can be influenced by differences in the level of thermal exposure during fusion-based and solvent-based processes. The physical stability of amorphous content varies according to the thermal history, particle morphology, and nucleation process of amorphous solid dispersions produced by different methods. The in vitro and in vivo performance of amorphous formulations are also affected by differences in particle morphology and in the molecular interactions caused by the manufacturing method. Additionally, we describe the mechanism of manufacturing methods and the thermodynamic theories that relate to amorphous formulations.

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Authors and Affiliations

  1. Division of Pharmaceutics, College of Pharmacy, The University of Texas at Austin, 2409 University Avenue, Mail Stop A1920, Austin, Texas, USA

    Siyuan Huang & Robert O. Williams III

  2. Small Molecule Design and Development, Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana, USA

    Siyuan Huang

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  1. Siyuan Huang
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Correspondence to Siyuan Huang.

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Huang, S., Williams, R.O. Effects of the Preparation Process on the Properties of Amorphous Solid Dispersions. AAPS PharmSciTech 19, 1971–1984 (2018). https://doi.org/10.1208/s12249-017-0861-7

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