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首页> 外文期刊>Biopharmaceutics and Drug Disposition >Mometasone furoate degradation and metabolism in human biological fluids and tissues.
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Mometasone furoate degradation and metabolism in human biological fluids and tissues.

机译：糠酸莫米松在人类生物体液和组织中的降解和代谢。

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The in vitro metabolic and non-metabolic degradation kinetics of mometasone furoate (MF) was investigated in selected human biological fluids and subcellular fractions of tissues. Qualitative and quantitative differences in transformation profiles of MF were observed among human biological media. Degradation was the major event in plasma and urine with four new degradation products identified; A: 21-chloro-17alpha-hydroxy-16alpha-methyl-9beta,11beta-oxidopregna-1,4-dien e-3,20-dione 17-(2-furoate), B: 9alpha,21beta-dichloro-11beta,21alpha-dihydroxy-16alpha-methylpregna-1,4,1 7,20-tetraen-3-one 21-(2-furoate), C: 21beta-chloro-21alpha-hydroxy-16alpha-methyl-9beta,11beta-oxidopregna-1,4, 17,20-tetraen-3-one 21-(2-furoate), and D: 21-chloro-17alpha-hydroxy-16alpha-methyl-9beta,11beta-oxidopregna-1,4-dien e-3,20-dione. A, B and C were predominant and D was minor in plasma while A and C were predominant in urine. Hydrolysis of the 17-ester bond of MF was not a major event in plasma. The turnover of MF in plasma was faster than that in phosphate buffers of pH 7.4.Metabolism of MF occurred primarily and rapidly in liver, appreciably in intestine, but negligibly in in vitro lung tissue. While 6beta-hydroxylation was a major metabolic pathway for MF in microsomes of both human liver and intestine, other parallel and subsequent metabolism pathways could also be involved. If these degradation and metabolic products are also formed and active in humans in vivo, both MF and its 'active' products need to be taken into account when determining the systemic bioavailability of MF and in establishing concentration-effect relationships with this drug.
机译：在选定的人类生物体液和组织的亚细胞部分中研究了糠酸莫米他松（MF）的体外代谢和非代谢降解动力学。在人类生物介质之间观察到MF的转化谱的定性和定量差异。降解是血浆和尿液中的主要事件，已鉴定出四种新的降解产物。 A：21-氯-17alpha-羟基-16alpha-甲基-9beta，11beta-oxidopregna-1,4-dien e-3,20-dione 17-（2-furoate），B：9alpha，21beta-dichloro-11beta， 21alpha-dihydroxy-16alpha-methylpregna-1,4,1 7,20-tetraen-3-one 21-（2-furoate），C：21beta-chloro-21alpha-hydroxy-16alpha-methyl-9beta，11beta-oxidopregna- 1,4，17,20-四烯-3-一21-（2-糠酸酯）和D：21-氯-17alpha-羟基-16alpha-甲基-9beta，11beta-oxidopregna-1,4-dien e-3 ，20-二酮。血浆中A，B和C占优势，D占少数，而尿中A和C占优势。 MF的17-酯键的水解不是血浆中的主要事件。血浆中MF的转换比pH 7.4的磷酸盐缓冲液中的转换更快.MF的代谢主要在肝脏中快速发生，在肠道中明显，但在体外肺组织中可以忽略不计。虽然6β-羟基化是人肝和肠微粒体中MF的主要代谢途径，但其他平行和后续代谢途径也可​​能参与。如果这些降解和代谢产物在人体中也能在人体中形成​​并具有活性，那么在确定MF的全身生物利用度并建立与该药物的浓度效应关系时，就必须考虑MF及其“活性”产物。

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