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核心技术专利：CN118964589B侵权必究

核心技术专利：CN118964589B侵权必究

Lasker J, Rickert D E

Xenobiotica. 1978 Nov;8(11):665-72. doi: 10.3109/00498257809069578.

The absorption and glucuronylation of [14C]diethylstilbestrol (DES) were studied in situ in segments of rat small intestine. 2. DES glucuronide accounted for nearly 50% of the methanol-soluble radioactive material appearing in the intestinal venous blood. 3. There was no difference between DES glucuronide formation in intestinal segments near the pyloric sphincter and in segments located near the ileo-caecal junction. 4. The appearance of DES and its glucuronide in the venous blood of aborally-located segments was dose-dependent from 0.1 to 5 mM, but in orally-located segments, an increase in DES concn. from 2 to 5 mM produced no increase in DES or its glucuronide in the venous blood. In neither of these intestinal regions was the rate of appearance of DES or DES glucuronide dependent upon intestinal blood flow. 5. The results indicate that intestinal glucuronylation of certain compounds during absorption may be significant over a wide range of concn. in all regions of the intestine.

在大鼠小肠各段原位研究了[14C]己烯雌酚（DES）的吸收及葡糖醛酸化情况。2. DES葡糖醛酸酯占肠静脉血中出现的甲醇溶性放射性物质的近50%。3. 在靠近幽门括约肌的肠段和回盲部连接处附近的肠段中，DES葡糖醛酸酯的形成没有差异。4. 在口侧定位的肠段中，从0.1至5 mM，DES及其葡糖醛酸酯在向肛侧定位的肠段静脉血中的出现呈剂量依赖性，但在口侧定位的肠段中，DES浓度从2 mM增加至5 mM并未使静脉血中DES或其葡糖醛酸酯增加。在这两个肠区域中，DES或DES葡糖醛酸酯的出现速率均不依赖于肠血流量。5. 结果表明，在吸收过程中，某些化合物的肠葡糖醛酸化在肠道所有区域的广泛浓度范围内可能都很显著。

Lasker J, Rickert D E

Xenobiotica. 1978 Nov;8(11):665-72. doi: 10.3109/00498257809069578.

The absorption and glucuronylation of [14C]diethylstilbestrol (DES) were studied in situ in segments of rat small intestine. 2. DES glucuronide accounted for nearly 50% of the methanol-soluble radioactive material appearing in the intestinal venous blood. 3. There was no difference between DES glucuronide formation in intestinal segments near the pyloric sphincter and in segments located near the ileo-caecal junction. 4. The appearance of DES and its glucuronide in the venous blood of aborally-located segments was dose-dependent from 0.1 to 5 mM, but in orally-located segments, an increase in DES concn. from 2 to 5 mM produced no increase in DES or its glucuronide in the venous blood. In neither of these intestinal regions was the rate of appearance of DES or DES glucuronide dependent upon intestinal blood flow. 5. The results indicate that intestinal glucuronylation of certain compounds during absorption may be significant over a wide range of concn. in all regions of the intestine.

在大鼠小肠各段原位研究了[14C]己烯雌酚（DES）的吸收及葡糖醛酸化情况。2. DES葡糖醛酸酯占肠静脉血中出现的甲醇溶性放射性物质的近50%。3. 在靠近幽门括约肌的肠段和回盲部连接处附近的肠段中，DES葡糖醛酸酯的形成没有差异。4. 在口侧定位的肠段中，从0.1至5 mM，DES及其葡糖醛酸酯在向肛侧定位的肠段静脉血中的出现呈剂量依赖性，但在口侧定位的肠段中，DES浓度从2 mM增加至5 mM并未使静脉血中DES或其葡糖醛酸酯增加。在这两个肠区域中，DES或DES葡糖醛酸酯的出现速率均不依赖于肠血流量。5. 结果表明，在吸收过程中，某些化合物的肠葡糖醛酸化在肠道所有区域的广泛浓度范围内可能都很显著。