Pharmacokinetic Strategies in the Development of Prodrugs

  • L. P. Balant
  • E. Doelker
  • P. Buri
Part of the NATO ASI Series book series (NSSA, volume 221)


The term prodrug was first introduced by Albert in 1958 to describe compounds which undergo biotransformation prior to exhibiting their pharmacological effects. Since then, many papers have been published on this subject [Higuchi & Stella, 1975; Roche, 1977; Higuchi et al, 1983; Stella et al, 1985; Waller & George, 1989; Balant et al, 1990a]. Usually, the use of the term prodrug implies a covalent link between an “active moiety” and a “carrier moiety”, but some authors also use this term to characterize some form of salts of the active principle. In this review, only covalently bound moieties will be considered.


Active Moiety Acetyl Ester Pivalic Acid Hydroxypropyl Cellulose Phosphoramide Mustard 


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Copyright information

© Plenum Press, New York 1991

Authors and Affiliations

  • L. P. Balant
    • 1
    • 2
  • E. Doelker
    • 2
  • P. Buri
    • 2
  1. 1.Clinical Research and Clinimetrics UnitPsychiatric University Institutions of GenevaSwitzerland
  2. 2.School of PharmacyUniversity of GenevaSwitzerland

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