STUDY ON THE BIOLOGICAL FATE OF PARABEN AT THE DOSE OF PRACTICAL USAGE IN RAT .1. METABOLISM AND EXCRETION OF ETHYL PARA-HYDROXYBENZOATE (ETHYL PARABEN) AND PARA-HYDROXYBENZOIC ACID
STUDY ON THE BIOLOGICAL FATE OF PARABEN AT THE DOSE OF PRACTICAL USAGE IN RAT .1. METABOLISM AND EXCRETION OF ETHYL PARA-HYDROXYBENZOATE (ETHYL PARABEN) AND PARA-HYDROXYBENZOIC ACID
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DOI：
10.1248/bpb1978.2.356
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发表时间：
1979-01-01
期刊：
影响因子：
--
通讯作者：
HANANO, M
中科院分区：
文献类型：
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作者：
KIWADA, H;AWAZU, S;HANANO, M
在大鼠中研究了用作药物制剂和食品防腐剂的尼泊金乙酯 (EP) 和 EP 母体化合物对羟基苯甲酸 (HB) 在实际使用剂量 (2 mg/kg) 下的生物归宿。 EP和HB均代谢为HB的甘氨酸缀合物(M1)、酯型葡萄糖醛酸苷(M3)和硫酸盐(M4)并在尿液和胆汁中排泄，排泄比例与较高剂量实验的结果相比有所不同，并且在胆汁中的排泄率存在路径依赖性。在静脉注射中。 EP给药后，每剂尿中排泄总活性为91.3%，胆汁中为5.97%，每剂尿中主要代谢物排泄百分比为HB的8.14%、M1的39.6%、M3的29.5%和M4的6.48%。十二指肠内给予EP时，与静脉注射相比，其排泄总活性（83.5%）和以HB形式排泄的活性（3.51%）均降低。行政。在HB给药中，未发现总活性的途径依赖性，但发现十二指肠内给药中HB的排泄减少。总放射性的排泄在5小时时几乎停止，并且从尿液中排泄的代谢物的西格玛-负图的β-相获得的生物半衰期是40-70分钟。本研究获得的结果与高剂量实验的结果不同。
The biological fates of ethylparaben (EP) which was used as a preservative for the pharmaceutical preparations and foods, and p-hydroxybenzoic acid (HB), which is the parent compound of EP, were studied at the dose of practical usage (2 mg/kg) in rats. 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 and a route dependency was found in the rate of excretion in the bile. In i.v. 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 i.v. 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 h and the biological half-lives obtained from the .beta.-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 at the high dose experiments.