Abstract
Coarse oil-in-water (o/w) emulsions stabilized by glycerol monostoarate have been converted (by addition of polysorbate 20) to a flocculated structure consisting of a cluster of fine oil globules and narrow, tortuous aqueous channels. The mean apparent interglobular space in the glycerol monostearate emulsion (A) was 26 ± 11 μm, and in the glycerol monostearate-polysorbate emulsion (B) the mean space was 1 ± 0.8 μm. In vitro release rates of chloroquine phosphate from the emulsions at 37 °C were 1.5 mg h −1 (A) and 0.5 mg h −1 (B). Oral bioavailability in rats in 3 h was 10.3 ± 2 and 7.5 ± 1.1 μg/ml, respectivey. The retard release effect observed in B relates to the greater tortuosity of aqueous diffusion channels in its structure, and its low rate of diffusive mixing with aqueous fluids.
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