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局部用糖皮质激素布地奈德和倍氯米松 17α,21 - 二丙酸酯在人肝和肺匀浆中的生物转化。

Biotransformation of the topical glucocorticoids budesonide and beclomethasone 17 alpha,21-dipropionate in human liver and lung homogenate.

作者信息

Andersson P, Ryrfeldt A

出版信息

J Pharm Pharmacol. 1984 Nov;36(11):763-5. doi: 10.1111/j.2042-7158.1984.tb04868.x.

Abstract

Tritiated budesonide and beclomethasone 17 alpha,21-dipropionate (BDP) were incubated with the 9000g supernatant of human liver homogenate. BDP was immediately hydrolysed to beclomethasone 17 alpha-propionate (BMP). BMP was then further biotransformed to polar metabolites. Budesonide was rapidly biotransformed (2-4 times more rapidly than BMP) to metabolites of low glucocorticoid potency. The compounds were also incubated with the 1000g supernatant of human lung homogenate. BDP was rapidly hydrolysed to BMP and then more slowly to beclomethasone. Budesonide was not biotransformed in the lung.

摘要

将氚标记的布地奈德和倍氯米松17α,21 - 二丙酸酯(BDP)与人肝匀浆的9000g上清液一起孵育。BDP立即水解为倍氯米松17α - 丙酸酯(BMP)。然后BMP进一步生物转化为极性代谢产物。布地奈德迅速生物转化(比BMP快2 - 4倍)为低糖皮质激素活性的代谢产物。这些化合物也与人肺匀浆的1000g上清液一起孵育。BDP迅速水解为BMP,然后更缓慢地水解为倍氯米松。布地奈德在肺中未发生生物转化。

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