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).
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Johnson, K.C., Swindell, A.C. Guidance in the Setting of Drug Particle Size Specifications to Minimize Variability in Absorption. Pharm Res 13, 1795–1798 (1996). https://doi.org/10.1023/A:1016068705255
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DOI: https://doi.org/10.1023/A:1016068705255