Abstract

The surface of the skin supports a range of microorganisms capable of metabolizing some topically applied drugs. In order to ascertain the significance of this degradation we have established a mathematical model to predict the influence of this biotransformation on the plasma levels of the drug. The model is a linear kinetic representation of the process of skin absorption and the rate constants are predicted from a physicochemical consideration of the properties of the drug. The results of the simulations show that microbial degradation of the drug can be significant, particularly if the topical formulation is a thin film. If a transdermal device is used the theoretical calculations show that enzymatic degradation of the active substance is likely to be clinically less significant.

Original languageEnglish
Pages (from-to)89-97
Number of pages9
JournalInternational Journal of Pharmaceutics
Volume26
Issue number1-2
DOIs
Publication statusPublished - Sept 1985

Bibliographical note

Funding Information:
We thank Vick International, Alza and NIH (GM-33395) for financial support. RHG is the recipient of a Special Emphasis Research Career Award (l-KOl-OH-00017) from the U.S. National Institute of Occupational Safety and Health.

Keywords

  • linear kinetic model
  • microbial degradation of drugs
  • skin absorption
  • topical drugs
  • transdermal drug device

ASJC Scopus subject areas

  • Pharmaceutical Science

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