title: Guidance in the setting of drug particle size specifications to minimize variability in absorption.
abstract: OBJECTIVE
  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).
authors.affiliation: Department of Pharmaceutical Research and Development, Pfizer Central Research, Groton, Connecticut 06340, USA.
authors.forename: K C
authors.initials: KC
authors.lastname: Johnson
authors.forename: A C
authors.initials: AC
authors.lastname: Swindell
mesh_terms: D003198:Computer Simulation; D007408:Intestinal Absorption; D008962:Models, Theoretical; D010316:Particle Size; D004364:Pharmaceutical Preparations / Q000378:metabolism*; D012995:Solubility
chemical_list: D004364:Pharmaceutical Preparations