The Analysis of Drug Release from Diluted Water/oil/water Emulsions by a Model of the Rupture of Oil Membrane

Abstract

Abstract The release behaviour of theophylline encapsulated in the inner aqueous phase of a water/oil/water emulsion was investigated by two methods. A cellulose tube containing a sample of the emulsion was placed in a rotary basket and was stirred in a dissolution medium (Method A), or the w/o/w emulsion was dispersed in a dissolution medium and the system was stirred by a paddle, allowing the drug to permeate into a cellulose tube placed in the dispersing medium (Method B). In Method A, the drug release rate from the emulsion decreased with increase in the concentration of sodium chloride co-formulated with the drug in the inner aqueous phase. The drug release rate in the dissolution test medium No. 1 or No. 2 of the JP XII was greater than that in purified water and was increased with the ionic strength of the dissolution medium. The drug was released more rapidly in Method B than in Method A, because the emulsion was destroyed more easily using the former method. As this destruction of emulsion structure occurred immediately after dilution with dissolution medium, the influence of the dissolution medium on the release profile could not be detected using Method B. The experimental data of drug release were satisfactorily explained by the destruction model of the oil membranes of the water/oil/water emulsions.