Effects of Micronization on Digestive Absorption of Diosmin

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Abstract
Objective: To investigate the effect of diosmin particle size on the rate and extent of absorption and excretion of total radioactivity, following oral administration of micronized and non-micronized [14C]-diosmin to New Zealand White rabbits. Design: This study was conducted in a 2 x 12 cross-over design at a uniform target dose level of 10 mg/kg, and was conducted according to Good Laboratory Practice. The micronized formulation was prepared using a Microdismembrator II, and all prepared doses were suspended in 0.5% w/v aqueous methylcellulose at a target concentration of 5 mg/ml. Particle size analysis indicated that in the micronized formulation, 90% of particles were ≤2 14C]-diosmin when administered orally as a suspension to rabbits resulted in a marked increase in the proportion of the dose excreted in urine. This increase was considered to reflect an increased absorption of radiolabelled components from the micronized dose.

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