文章基本信息

标题：EVALUATION OF LIPID-CONTAINING ORAL DOSAGE FORMS IN RATS
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作者：YOSHIYA YAMAHIRA ; TETSUO NOGUCHI ; TAKESHI NOGUCHI 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：1979
卷号：2
期号：1
页码：52-59
DOI：10.1248/bpb1978.2.52
出版社：The Pharmaceutical Society of Japan
摘要：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.
关键词：variation of absorption rate