环糊精对氨苄西林水溶液聚合的抑制作用。

Drug design and delivery Pub Date : 1990-12-01
H Aki, K Yamamoto, N Sawai, M Yamamoto
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引用次数: 0

摘要

氨苄西林在水溶液中聚合产生抗原聚合物;用阴离子交换色谱法对聚合物进行了分离,并通过快速原子轰击质谱的质量发现,聚合物由氨苄西林的二聚体、三聚体、四聚体和五聚体组成。在其圆二色光谱中,在230 nm附近的特征正棉花效应揭示了每个聚合物中存在完整的β -内酰胺环。β -环糊精被发现抑制这种聚合通过复杂的形成涉及等摩尔量的成分。该络合物在10%的水溶液中,在24℃下6小时内完全形成。随着聚合程度的增加,β -内酰胺环产生的正棉效应降低,但与β -环糊精形成的正棉效应不变。
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Inhibitory effect of beta-cyclodextrin on ampicillin polymerization in aqueous solution.

Ampicillin polymerizes in aqueous solution to produce antigenic polymers; the polymers were separated by anion-exchange chromatography and shown to consist of a dimer, trimer, tetramer and pentamer of ampicillin by the masses found in fast atom bombardment mass spectroscopy. The presence of an intact beta-lactam ring in each of the polymers was revealed by the characteristic positive Cotton effect near 230 nm in their circular dichroism spectra. beta-Cyclodextrin was found to inhibit this polymerization by complex formation involving equimolar quantities of the constituents. Formation of this complex was complete in 10% aqueous solution within 6 hr at 24 degrees C. The positive Cotton effect arising from the beta-lactam ring decreased as the degree of polymerization increased, but was unchanged by the complex formation with beta-cyclodextrin.

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