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标题：THE STUDY ON THE BIOLOGICAL FATE OF PARABEN AT THE DOSE OF PRACTICAL USAGE IN RAT. I. THE METABOLISM AND EXCRETION OF ETHYL p-HYDROXYBENZOATE (ETHYLPARABEN) AND p-HYDROXYBENZOIC ACID
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作者：HIROSHI KIWADA ; SHOJI AWAZU ; MANABU HANANO 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：6
页码：356-364
DOI：10.1248/bpb1978.2.356
出版社：The Pharmaceutical Society of Japan
摘要：The biological fates of ethylparaben (EP) which has been widely used as a preservatives for the pharmaceutical preparations and foods, and p-hydroxybenzoic acid (HB) which is the parent compound of EP, were investigated at the dose of practical usage (2 mg/kg) in rats. Although both EP and HB were metabolized to glycine conjugate (M1), ester type glucuronide (M3) and sulfate (M4) of HB and excreted in the urine and bile, the excretion ratios were different as compared with the results of higher dose experiments carried out by other authors, and a route dependency was also found in the rate of excretion in the bile. The excretion data obtained in this study are shown as follows : In intravenous administration of EP, the excreted total activity was 91.3% per dose in the urine and 5.97% in the bile, and percentages per dose of the major metabolites excreted in the urine were 8.14% of HB, 39.6% of M1, 29.5% of M3 and 6.48% of M4. In intraduodenal administration of EP, the excreted total activity (83.5%) and the activity excreted as HB (3.51%) decreased compared with the intravenous administration. In the HB administration, the route dependency of the total activity was not found, but a decrease in the excretion of HB in the intraduodenal administration was found. The excretion of total radioactivity almost ceased by 5 hr and the biological halflives obtained from the β-phase of the sigma-minus plots of the metabolites excreted in the urine were 40-70 min. The result obtained in this study differ from those of other authors at the high dose experiments.
关键词：p-hydroxybenzoic acid