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一种新型甾体抗炎药地夫可特在大鼠、狗和人体中的处置情况。

Disposition of a new steroidal anti-inflammatory agent, deflazacort, in rat, dog and man.

作者信息

Alessandro A, Antonio P, Giuseppe B, Valeria P

出版信息

Eur J Drug Metab Pharmacokinet. 1980;5(4):207-15. doi: 10.1007/BF03189466.

DOI:10.1007/BF03189466
PMID:7250144
Abstract

The physiological disposition of a new steroid anti-inflammatory agent, deflazacort, was examined in rat, dog and man following 5 mg/kg doses to the animals, and 50 mg to humans. The administered radiocarbon [2'-14C]-deflazacort), is rapidly and extensively absorbed into the general circulation in rat and man, whereas the bioavailability in the dog is low. The terminal plasma half-life for radioactivity elimination was, on the average, 11, 15 and 28 hr in rats, dogs and man, respectively. Urinary excretion was the predominant route of 14C elimination in the rat (-54% of the dose) and in man (-68% of the dose), whereas in the dog the majority of the dose was eliminated via the feces (82%). Tissue distribution studies in the rat did not show target organs, with the exception of the blood cells. Studies of binding to plasma proteins of the 21-desacetyl deflazacort, demonstrate in all the species a rather low level of binding of non-saturable type.

摘要

给大鼠、犬和人分别按5mg/kg(动物)和50mg(人)的剂量给予一种新型甾体抗炎药地夫可特后,对其生理处置情况进行了研究。所给予的放射性碳标记物[2'-14C]-地夫可特在大鼠和人体内迅速且广泛地被吸收进入体循环,而在犬体内的生物利用度较低。放射性消除的终末血浆半衰期在大鼠、犬和人中平均分别为11小时、15小时和28小时。尿排泄是大鼠(占剂量的-54%)和人(占剂量的-68%)体内14C消除的主要途径,而在犬体内,大部分剂量经粪便消除(82%)。大鼠的组织分布研究未显示出靶器官,但血细胞除外。对21-去乙酰地夫可特与血浆蛋白结合的研究表明,在所有物种中其结合水平均较低,且为非饱和型。

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Eur J Drug Metab Pharmacokinet. 1980;5(4):207-15. doi: 10.1007/BF03189466.
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