Biotransformation of diclofenac sodium (Voltaren) in animals and in man. II. Quantitative determination of the unchanged drug and principal phenolic metabolites, in urine and bile.
Biotransformation of diclofenac sodium (Voltaren) in animals and in man. II. Quantitative determination of the unchanged drug and principal phenolic metabolites, in urine and bile.
复制标题
双氯芬酸钠（扶他林）在动物和人体中的生物转化。
DOI：
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发表时间：
1979
期刊：
影响因子：
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通讯作者：
J. Faigle
中科院分区：
文献类型：
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作者：
H. Stierlin;J. Faigle
1.通过对大鼠、犬、恒河猴、狒狒和人的尿液以及大鼠、犬和人的胆汁进行反向同位素稀释分析，对原型双氯芬酸及其两种主要酚类代谢产物进行定量测定。在各种酶和化学水解方法之前和之后进行同位素稀释分析。2.同样的样品也通过二维t.l.c.分析。以及随后的放射自显影，以估计剩余的酚类代谢物。3.与大鼠、恒河猴、狒狒和人（主要排泄羟基化代谢物）相反，犬不会氧化双氯芬酸。犬尿液中含有相对稳定的双氯芬酸牛磺酸结合物，胆汁中排泄出酯葡糖苷酸，即使在弱碱性溶液中也能分解。4.在犬胆汁中发现的不稳定酯葡糖苷酸在大鼠胆汁中也可证实。推测其在十二指肠中水解，释放双氯芬酸，双氯芬酸经历肝肠循环。
1. Quantitative determinations of unchanged diclofenac and two of its major phenolic metabolites were made by reverse isotope dilution analysis on urine of rat, dog, rhesus monkey, baboon and man and on bile of rat, dog and man. Isotope dilution analysis was performed before and after various methods of enzymic and chemical hydrolysis. 2. The same samples were also analysed by two-dimensional t.l.c. and subsequent autoradiography, to estimate the remaining phenolic metabolites. 3. In contrast to rat, rhesus monkey, baboon and man, which excrete mainly hydroxylated metabolites, the dog does not oxidize diclofenac. Dog urine contained a relatively stable taurine conjugate of diclofenac, and in the bile an ester glucuronide was excreted, which decomposed even in weakly alkaline soln. 4. The unstable ester glucuronide found in dog bile was also demonstrable in rat bile. It presumably hydrolyses in the duodenum, releasing diclofenac which undergoes enterohepatic circulation.