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Solid-State Techniques for Improving Solubility

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Formulating Poorly Water Soluble Drugs

Part of the book series: AAPS Advances in the Pharmaceutical Sciences Series ((AAPS,volume 50))

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Abstract

Poor aqueous solubility of a drug substance can often be attributed to strong intermolecular forces within its crystal lattice, which, in turn, prevent molecules from esca** in solution. Through the use of solid-state chemistry, it is possible to modify the crystal structure in such a way that mitigates intermolecular forces, thus improving aqueous solubility and increasing rates of dissolution. Solid-state techniques utilized for solubility enhancement include the formation of salts, polymorphic or amorphous forms, and cocrystals. Each technique has specific advantages and, in some cases, disadvantages that may prevent its successful use. The purpose of this chapter is to describe each of the methods, allowing the reader to gain an understanding of solid-state modifications available for solubility enhancement.

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Author information

Authors and Affiliations

  1. Molecular Pharmaceutics and Drug Delivery Division, College of Pharmacy, The University of Texas at Austin, Austin, TX, USA

    Miguel O. Jara & Robert O. Williams III

  2. ThermoFisher Scientific, High Point, NC, USA

    Justin R. Hughey

  3. Syntheic Molecule Design and Development, Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN, USA

    Siyuan Huang

Authors
  1. Miguel O. Jara
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  2. Justin R. Hughey
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  3. Siyuan Huang
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  4. Robert O. Williams III
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Corresponding author

Correspondence to Robert O. Williams III .

Editor information

Editors and Affiliations

  1. Division of Pharmaceutics, The University of Texas at Austin, Austin, TX, USA

    Robert O. Williams III

  2. Division of Pharmaceutics, College of Pharmacy, The University of Texas at Austin, Austin, TX, USA

    Daniel A. Davis Jr.

  3. DisperSol Technologies, LLC, Georgetown, TX, USA

    Dave A. Miller

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Jara, M.O., Hughey, J.R., Huang, S., Williams, R.O. (2022). Solid-State Techniques for Improving Solubility. In: Williams III, R.O., Davis Jr., D.A., Miller, D.A. (eds) Formulating Poorly Water Soluble Drugs. AAPS Advances in the Pharmaceutical Sciences Series, vol 50. Springer, Cham. https://doi.org/10.1007/978-3-030-88719-3_3

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