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地高辛与蒙脱石的相互作用:吸附与降解机制

Interaction of digoxin and montmorillonite: mechanism of adsorption and degradation.

作者信息

Porubcan L S, Born G S, White J L, Hem S L

出版信息

J Pharm Sci. 1979 Mar;68(3):358-61. doi: 10.1002/jps.2600680327.

Abstract

IR, X-ray diffraction, and absorption studies showed that digoxin is adsorbed onto montmorillonite by a reversible adsorption mechanism at pH 2 and 6. Degradation studies indicated abnormally high acid hydrolysis rates for digoxin interacted with montmorillonite. Accelerated digoxin degradation is attributed to the ability of the clay surface to concentrate both digoxin and protons. The effective pH at the clay surface appeared to be 1.5 pH unites lower than the bulk suspension pH. Bisdigoxigenin was the major adsorbed degradation product. A similar catalytic effect also may occur with other neutral drugs that degrade by acid hydrolysis and should be considered in the formulation of clay-containing drug products or their coadministration with other drugs.

摘要

红外光谱、X射线衍射和吸收研究表明,在pH值为2和6时,地高辛通过可逆吸附机制吸附在蒙脱石上。降解研究表明,与蒙脱石相互作用的地高辛酸水解速率异常高。地高辛加速降解归因于粘土表面浓缩地高辛和质子的能力。粘土表面的有效pH值似乎比整体悬浮液pH值低1.5个pH单位。双去氧地高辛是主要的吸附降解产物。对于其他通过酸水解降解的中性药物,也可能发生类似的催化作用,在含粘土药物产品的配方或其与其他药物的联合给药中应予以考虑。

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