Simulation of pharmacokinetic behaviour of drug-cyclodextrin complexes

Pharmazie. 1984 Dec;39(12):830-4.

Abstract

Complexation with cyclodextrin decreases the hydrophobicity of poorly soluble drugs and results in enhanced dissolution rates and higher solubility. In vivo experiments showed that this "molecular encapsulation" of drugs leads to enhanced bioavailability, which is controlled by the solubilities, stability constants of the complexes, the molar ratio of drug: cyclodextrin, etc. This modification of the pharmacokinetic processes has been simulated by computing the theoretical blood level curves. These computer-simulated curves seem to be appropriate models of the experimental observations. Knowing the numerical values of the parameters utilized in these computer simulations, the modification of the pharmacokinetics can be predicted when using cyclodextrin complexes in oral dosage forms.

MeSH terms

  • Adsorption
  • Biological Availability
  • Body Fluids / metabolism
  • Cellulose / metabolism*
  • Chemical Phenomena
  • Chemistry, Pharmaceutical
  • Chemistry, Physical
  • Cyclodextrins / metabolism*
  • Dextrins / metabolism*
  • Half-Life
  • Humans
  • In Vitro Techniques
  • Kinetics
  • Models, Chemical
  • Pharmaceutical Preparations / metabolism
  • Solubility
  • Starch / metabolism*

Substances

  • Cyclodextrins
  • Dextrins
  • Pharmaceutical Preparations
  • cyclodextrin polymer
  • Cellulose
  • Starch