Gastro-Intestinal Absorption of Ethyl 2-Chloro-3-[4-(2-methyl-2-phenylpropyloxy)phenyl]propionate from Different Dosage Forms in Rats and Dogs

概要

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To obtain information as to a suitable formulation of ethyl 2-chloro-3-[4-(2-methyl-2-phenylpropyloxy)-phenyl]propionate (AL-294), an antihyperlipidemic drug of low water solubility, the bioavailability after its oral administration in various dosage forms was evaluated in rats and dogs. After AL-294 was administered orally, AL-294 acid (2-chloro-3-[4-(2-methyl-2-phenylpropyloxy)phenyl]propionic acid), which is a metabolite of AL-294,was detected in the plasma. Therefore, absorbability of AL-294 was evaluated using plasma AL-294 acid levels. AL-294 in an oil solution or in a gelatin capsule showed poor absorption, whereas it's absorption was greatly enhanced in the form of an emulsion. The postprandial administration also showed batter absorption. The elimination rate of AL-294 acid from the plasma after oral administration of the emulsion was similar to that after intravenous administration of a sodium salt of AL-294 acid.
社団法人日本薬学会の論文
1990-10-25