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Investigation of inclusion complex of honokiol with sulfobutyl ether-β-cyclodextrin

机译:厚朴酚与磺基丁基醚-β-环糊精的包合物研究

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摘要

This study aimed to prepare and characterize an inclusion complex of honokiol (HNK) with sulfobutyl ether-3-cyclodextrin (SB-β-CD). The inclusion complex (HNK/CD COMP) was prepared utilizing a freeze-drying method. Phase-solubility curves were employed to obtain stability constants and thermodynamic parameters. The phase-solubility diagram showed a typical A_L-type, indicating that the 1:1 (HNK:SB-β-CD) inclusion complex was formed. The solid inclusion complex was then characterized by differential scanning calorimetry and Fourier transform infrared spectroscopy. Results showed that HNK/CD COMP exhibited a higher drug release rate than free HNK in vitro. A comparative study of the pharmacokinetics between HNK/CD COMP and free HNK was also performed in rats. In vivo results indicated that AUCo-t and C_(max) of HNK/CD COMP increased by approximately 158% and 123% compared with those of the free HNK, respectively. These results suggest that SB-β-CD will be potentially useful in the delivery of poorly soluble drugs, such as HNK.
机译:这项研究旨在制备和表征厚朴酚(HNK)与磺基丁基醚-3-环糊精(SB-β-CD)的包合物。使用冷冻干燥法制备包合物(HNK / CD COMP)。相溶解度曲线用于获得稳定性常数和热力学参数。相溶解度图显示了典型的A_L型,表明形成了1:1(HNK:SB-β-CD)包合物。然后通过差示扫描量热法和傅里叶变换红外光谱对固体包合物进行表征。结果表明,HNK / CD COMP的体外药物释放速率高于游离的HNK。还对大鼠的HNK / CD COMP和游离HNK的药代动力学进行了比较研究。体内结果表明,与游离HNK相比,HNK / CD COMP的AUCo-t和C_(max)分别增加了约158%和123%。这些结果表明,SB-β-CD可能在难溶性药物(如HNK)的递送中有用。

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