Powder Dissolution Method for Estimating Rotating Disk Intrinsic Dissolution Rates of Low Solubility Drugs

Abstract

The results demonstrate that using potentially 10,000-fold less drug material does not sacrifice the quality of the measurement, and lends support to an earlier study that the disk IDR measurement may possibly serve as a surrogate for the BCS solubility classification.

Suggested Improvements for Measurement of Equilibrium Solubility-pH of Ionizable Drugs

“…However, the miniaturized-volume dissolution apparatus, µDISS Profiler (Pion Inc.), uses 1.0 mL working volumes and makes it practical to determine solubility (Avdeef et al [69]; Avdeef and Tsinman [70]; Tsinman et al [71]; Avdeef et al [72]; Fagerberg et al [73]). Since the instrument uses in situ fiber optic UV (diode array) detection, the progression of dissolution may be followed in real time, making it possible to characterize the (transient) solubility of different polymorphs/solvates, over periods of days, if necessary.…”

Physicochemical Profiling in Drug Research and Development

“…This apparatus is also suitable for the measurement of equilibrium solubility of sparingly soluble compounds, provided enough material is used to maintain the saturation [41,88,89]. In this procedure, 5 mg of drug are compressed into pellets and inserted into a rotating disk carrier containing an embedded magnetic stir bar at its bottom.…”

Intrinsic Dissolution as a Tool for Evaluating Drug Solubility in Accordance with the Biopharmaceutics Classification System

“…A good correlation of results is observed compared with the fixed-disk system and even other systems not detailed in pharmacopeias but tested in several studies to determine the intrinsic dissolution rate. The latter include the flowcell system and a miniature apparatus (Mini-IDR) similar to the rotating disk (32,33,36,42,43).…”