INTERDEPENDENCE OF PHYSIOLOGICAL SURFACTANT AND DRUG PARTICLE SIZE ON DISSOLUTION BEHAVIOR OF WATER-INSOLUBLE DRUGS

A series of in vitro experiments was performed to demonstrate the interdependence of physiologic surfactant and drug particle size on the dissolution rate of glutethimide, griseofulvin, and a new diuretic Compound A. The presence of physiological concentrations of lysolecithin (a naturally occurring biosurfactant) is shown to exhibit micellar solubilizing properties on the drugs investigated. The data obtained from the dissolution rate studies showed that aqueous lysolecithin solution caused significant enhancement of the extent of solution of the drugs investigated. However, the reduction of particle size through micronization may not necessarily increase the in vitro dissolution rate. Data to support this statement are presented, and a plausible explanation for its occurrence is the electrostatic charge that develops on the solids after milling. This results in aggregates which can be larger in particle size than the unmilled drug. Copyright © 1968 Wiley‐Liss, Inc., A Wiley Company