Excipient-drug interactions in parenteral formulations

J Pharm Sci. 2002 Nov;91(11):2283-300. doi: 10.1002/jps.10154.

Abstract

Excipients are added to parenteral formulations to enhance or maintain active ingredient solubility (solubilizers) and/or stability (buffers, antioxidants, chelating agents, cryo- and lyoprotectants). Excipients also are important in parenteral formulations to assure safety (antimicrobial preservatives), minimize pain and irritation upon injection (tonicity agents), and control or prolong drug delivery (polymers). These are all examples of positive or synergistic interactions between excipients and drugs. However, excipients may also produce negative effects such as loss of drug solubility, activity, and/or stability. This review article will highlight documented interactions, both synergistic and antagonistic, between excipients and drugs in parenteral formulations. The reader will gain better understanding and appreciation of the implications of adding formulation ingredients to parenteral drug products.

Publication types

  • Review

MeSH terms

  • Animals
  • Chemistry, Pharmaceutical
  • Drug Interactions*
  • Excipients / metabolism*
  • Humans
  • Infusions, Parenteral
  • Pharmaceutical Preparations / metabolism*

Substances

  • Excipients
  • Pharmaceutical Preparations