Some properties and the inclusion behavior of branched cyclodextrins.
Some properties and the inclusion behavior of branched cyclodextrins.
复制标题
支链环糊精的一些性质和包合行为。
DOI：
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发表时间：
1988
影响因子：
1.7
通讯作者：
K. Ogata
中科院分区：
文献类型：
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作者：
Y. Okada;Y. Kubota;K. Koizumi;S. Hizukuri;T. Ohfuji;K. Ogata
以麦芽糖或麦芽三糖为原料，分别与α-、β-或γ-环糊精（CD）通过假单胞菌异淀粉酶或产气克雷伯氏菌普鲁兰酶合成麦芽糖基（G2）-和麦芽三糖基（G3）-环糊精（CD），用高效液相色谱法对其进行纯化，并研究了它们在水和不同浓度甲醇水溶液中的溶解度、比旋光度和溶血活性。在水和甲醇水溶液中，G2-和G3-CD以及葡糖基（G1）-CD比每个母体CD更易溶。分支CD的溶血活性随侧链长度的增加而降低; CD>G1-CD>G2-CD>G3-CD。用溶解度法和差示扫描量热法研究了支化环糊精与难溶性药物在水溶液和固体中的包合作用。G_1-、G_2-、G_3-CD与它们的母体CD在一系列中的络合能力几乎相同，并且络合物在水中的稳定性几乎不受侧链长度的影响。然而，支化CD对水溶性差的药物的溶解度的增强比母体CD显著得多。
Maltosyl (G2)- and maltotriosyl (G3)-cyclodextrins (CDs), synthesized from maltose or maltotriose and α-, β- or γ-CD with Pseudomonas isoamylase or Klebsiella aerogenes pullulanase were purified by high-performance liquid chromatography, and their solubilities in water and in various concentrations of methanol in water, specific rotations, and hemolytic activities were studied. G2-and G3-CDs, as well as glucosyl (G1)-CDs, were much more soluble than each parent CD in water and methanol aqueous solutions. The hemolytic activities of the branched CDs decreased with increasing side chain length; CD>G1-CD>G2-CD>G3-CD. The inclusion behavior of the branched CDs with slightly soluble or insoluble drugs in aqueous solution and in the solid state was examined by the solubility method and the differential scanning calorimetry. The complexation abilities of G1-, G2-, G3-CD and their parent CD in a series appeared to be almost the same and the stabilities of complexes in water practically unaffected by the length of the side chain. However, the enhancement of solubility of poorly water-soluble drugs by branched CDs was much more marked than that by the parent CD.