Guidance in the setting of drug particle size specifications to minimize variability in absorption

Pharm Res. 1996 Dec;13(12):1795-8. doi: 10.1023/a:1016068705255.

Abstract

Purpose: To provide guidance in setting particle size specifications for poorly soluble drugs to minimize variability in absorption.

Methods: A previously reported computer method was used to simulate the percent of dose absorbed as a function of solubility, absorption rate constant, dose, and particle size.

Results: The simulated percent of dose absorbed was tabulated over a realistic range of solubilities, absorption rate constants, and doses using drug particle sizes that might be typically found in a dosage form.

Conclusions: The greatest effect of particle size on absorption was simulated for low dose- low solubility drugs. In general, the sensitivity of absorption to particle size decreased with increasing dose or solubility. At a solubility of 1 mg/mL, particle size had practically no effect on the percent of dose absorbed over the range of doses simulated (1-250 mg).

MeSH terms

  • Computer Simulation
  • Intestinal Absorption*
  • Models, Theoretical
  • Particle Size*
  • Pharmaceutical Preparations / metabolism*
  • Solubility

Substances

  • Pharmaceutical Preparations