Abstract
Four xanthene derivatives, namely, 8-chlorotheophylline, caffeine, theophylline and 1-methyl-3-sisobutylxanthene (SC-2964) were studied to ascertain their in vitro intestinal absorbability and partitioning property in an octyl alcohol/pH 7.4 buffer system. Absorbability in vitro was estimated as the cumulative transfer rate (μglmin.) of the test compounds transfering across everted rat intestine sacs. The results demonstrated a dependency of the cumulative transfer rates on the partition coefficients. A logarithmic correlation between cumulative transfer rates and partition coefficients of the test compounds was observed. It is concluded that this predictive methodology could be adopted to screen potentially active compounds and optimize the selection of compounds to be developed into orally bioavailable dosage forms.
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