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首页> 外文期刊>Crystal growth & design >Application of Intermolecular Spaces between Polyethylene Glycol/ γ-Cyclodextrin-Polypseudorotaxanes as a Host for Various Guest Drugs
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Application of Intermolecular Spaces between Polyethylene Glycol/ γ-Cyclodextrin-Polypseudorotaxanes as a Host for Various Guest Drugs

机译：聚乙二醇/γ-环糊精-聚伪轮烷之间的分子间空间在多种客用药物中的应用

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Eleven guest drugs with planar structures were incorporated into the intermolecular spaces between polyethylene glycol/γ-cyclodextrin (γ-CD)-polypseudorotaxanes by a sealed-heating method. Drug incorporation changed the crystal packing of γ-CD from hexagonal- to monoclinic-columnar forms, without dependence on the guest species. The incorporation of guest drugs was size dependent and stoichiometric. Guest drugs with one benzene ring and maximum cross sectional areas of ca. 40?55 ?~2 exhibited a drug to γ-CD stoichiometry of 2:1. Meanwhile, the stoichiometry was 1:1 for drugs with 2?3 benzene rings and maximum cross sectional areas of ca. 60?75 ?~2. More sterically bulky drugs (four and five benzene rings) did form complexes, though the complexation efficiency was insufficient to form stoichiometric complexes, due to steric hindrance. The volume of intermolecular space of the host was estimated to be larger than that of a β-CD cavity and as large as that of a γ-CD cavity. Hydrophobic and van der Waals interactions worked as driving forces for the complexation because polycyclic aromatic hydrocarbons with high log P values formed the complex. The dissolution property of the hydrophobic pharmaceutical drug naproxen was clearly improved by the complexation because naproxen existed in a monomolecular state in the complex.
机译：通过密封加热方法将11种具有平面结构的客用药物掺入到聚乙二醇/γ-环糊精（γ-CD）-聚假轮烷之间的分子间空间中。药物掺入将γ-CD的晶体堆积从六方柱状变为单斜柱状，而不必依赖客体。客用药物的掺入是尺寸依赖性的和化学计量的。带有一个苯环且最大横截面积约为ca的客用药物。 40？55？〜2对γ-CD化学计量比为2：1的药物。同时，对于具有2？3苯环且最大横截面积约为ca的药物，化学计量比为1：1。 60？75？〜2。尽管由于空间位阻，络合效率不足以形成化学计量的络合物，但空间更大的药物（四个和五个苯环）确实形成了络合物。据估计，宿主的分子间空间的体积大于β-CD腔的体积，而与γ-CD腔的体积相同。疏水和范德华相互作用是络合的驱动力，因为具有高log P值的多环芳烃形成了络合物。由于萘普生在复合物中以单分子状态存在，因此疏水化药物萘普生的溶解性质明显地通过络合得到改善。

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