EVALUATION OF LIPID-CONTAINING ORAL DOSAGE FORMS IN RATS

概要

論文の詳細を見る
A novel method for evaluation of oral lipid formulation in rats, which enabled us to reduce the dose level to 2 mcl/rat with satisfactory acuracy, was presented. The dose level was fairly comparable to that of clinical unit dose such as a soft capsule on mcl/kg (lipid dose/body weight) basis. By using this method, lipid-containing oral dosage forms were evaluated. A new antiinflammatory agent 1-cyclopropyl-4-phenyl-6-chlor-2(1H)-quinazolinone (SL-512) was selected as a model of poorly water soluble drug. A medium chain triglyceride was mostly used as a lipid vehicle. It was demonstrated that the characteristics of the lipid formulation could be estimated by measuring the gastric emptying rate of the drug or sometime combined with the intestinal remaining of the drug in rats. These results basically consisted of those obtained from 20 mcl/rat dosing experiments previously reported. It was newly found that by reducing the dose level to 2 mcl/rat, the drug absorption was less affected by the dosage form factors such as the drug concentration in the preparation or the digestibility of lipid vehicle. It was also shown by this method that compared with an aqueous suspension, the drug absorption of the lipid formulation was less variable and less affected by the concomitant food intake.
公益社団法人日本薬学会の論文