Preformulation in Drug Product Design

  • Ashlee D. Brunaugh
  • Hugh D. C. Smyth
  • Robert O. Williams III
Part of the AAPS Introductions in the Pharmaceutical Sciences book series (AAPSINSTR)


This chapter provides an overview of the factors that are considered in dosage form design, including physicochemical properties of drugs, drug solubility and dissolution, drug bioavailability, membrane permeability, and solid-state characteristics. Commonly performed preformulation studies including dissolution testing, X-ray diffraction, thermogravimetric analysis, differential scanning calorimetry, particle size analysis and drug degradation testing are discussed.


Preformulation studies Physicochemical properties Dosage-form design Bioavailability Biopharmaceutics Classification System Solid-state characterization Drug stability 

Further Reading

  1. Suggested readings for the student include the following texts:Google Scholar
  2. 1.
    Arnott JA, Planey SL. The influence of lipophilicity in drug discovery and design. Expert Opin Drug Discovery. 2012;7(10):863–75.CrossRefGoogle Scholar
  3. 2.
    Huang S, Mao C, Williams RO III, Yang CY. Solubility advantage (and disadvantage) of pharmaceutical amorphous solid dispersions. J Pharm Sci. 2016;105(12):3549–61.CrossRefGoogle Scholar
  4. 3.
    Jermain SV, Brough C, Williams RO III. Amorphous solid dispersions and nanocrystal technologies for poorly water-soluble drug delivery–an update. Int J Pharm. 2018;535(1–2):379–92.CrossRefGoogle Scholar
  5. 4.
    Leleux J, Williams R. Recent advancements in mechanical reduction methods: particulate systems. Drug Dev Ind Pharm. 2014;40(3):289–300.CrossRefGoogle Scholar
  6. 5.
    Liu X, Feng X, Williams RO, Zhang F. Characterization of amorphous solid dispersions. J Pharm Investig. 2018;48(1):19–41.CrossRefGoogle Scholar
  7. 6.
    Ma X, Williams RO III. Characterization of amorphous solid dispersions: an update. J Drug Deliv Sci Technol. 2019;50:113–24.CrossRefGoogle Scholar
  8. 7.
    Murikipudi V, Gupta P, Sihorkar V. Efficient throughput method for hygroscopicity classification of active and inactive pharmaceutical ingredients by water vapor sorption analysis. Pharm Dev Technol. 2013;18(2):348–58.CrossRefGoogle Scholar
  9. 8.
    Newman AW, Reutzel-Edens SM, Zografi G. Characterization of the “hygroscopic” properties of active pharmaceutical ingredients. J Pharm Sci. 2008;97(3):1047–59.CrossRefGoogle Scholar
  10. 9.
    Rautio J, Kumpulainen H, Heimbach T, Oliyai R, Oh D, Järvinen T, Savolainen J. Prodrugs: design and clinical applications. Nat Rev Drug Discov. 2008;7(3):255.CrossRefGoogle Scholar
  11. 10.
    Varum FJ, Hatton GB, Basit AW. Food, physiology and drug delivery. Int J Pharm. 2013;457(2):446–60.CrossRefGoogle Scholar
  12. 11.
    Huang S, Mao C, Williams RO III, Yang C-Y. Solubility advantage (and disadvantage) of pharmaceutical amorphous solid dispersions. J Pharm Sci. 2016;105:3549–61.CrossRefGoogle Scholar

Copyright information

© American Association of Pharmaceutical Scientists 2019

Authors and Affiliations

  • Ashlee D. Brunaugh
    • 1
  • Hugh D. C. Smyth
    • 1
  • Robert O. Williams III
    • 1
  1. 1.College of PharmacyThe University of Texas at AustinAustinUSA

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