张学农, 阎雪莹, 唐丽华, 龚金红, 张强. 马蔺子素-羟丙基-β-环糊精包合物的制备、鉴定及包合作用J. 药学学报, 2005, 40(4): 369-372.
引用本文: 张学农, 阎雪莹, 唐丽华, 龚金红, 张强. 马蔺子素-羟丙基-β-环糊精包合物的制备、鉴定及包合作用J. 药学学报, 2005, 40(4): 369-372.
ZHANG Xue-nong, YAN Xue-ying, TANG Li-hua, GONG Jin-hong, ZHANG Qiang. Preparation, identification and inclusion actions of irisquinone hydroxypropyl-β-cyclodextrin inclusion complexJ. Acta Pharmaceutica Sinica, 2005, 40(4): 369-372.
Citation: ZHANG Xue-nong, YAN Xue-ying, TANG Li-hua, GONG Jin-hong, ZHANG Qiang. Preparation, identification and inclusion actions of irisquinone hydroxypropyl-β-cyclodextrin inclusion complexJ. Acta Pharmaceutica Sinica, 2005, 40(4): 369-372.

马蔺子素-羟丙基-β-环糊精包合物的制备、鉴定及包合作用

Preparation, identification and inclusion actions of irisquinone hydroxypropyl-β-cyclodextrin inclusion complex

  • 摘要: 目的制备和鉴定马蔺子素-羟丙基-β-环糊精包合物,并考察马蔺子素与HP-β-CD之间的包合作用及构成摩尔质量比。方法通过冷冻干燥法制备马蔺子素-羟丙基-β-环糊精包合物,采用摩尔梯度法和连续递变法考察了包合物中主客分子之间的包合摩尔比;采用X射线衍射(XRD)和差示扫描量热法(DSC)对包合物进行了鉴定。结果主客分子摩尔梯度和反应热力学结果显示,25 ℃,35 ℃和45 ℃下HP-β-CD与马蔺子素包合摩尔质量比为2∶1,此时具有最大的增溶特性和较大的结合常数,其冻干粉经鉴别已形成包合物。结论马蔺子素包合物能显著增大药物的溶解度和稳定性。

     

    Abstract: AimTo perpare and identify irisquinone hydroxypropyl-β-cyclodextrin inclusion complex (irisquinone-HP-β-CD), as well as to study the inclusion mechanism and molecule stoichiometry between irisquinone and hydroxypropyl-β-cyclodextrin. MethodsIrisquinone-HP-β-CD was prepared by freeze-drying technique. The ratio of host and guest was also studied in inclusion process by mol gradient and continuing variational methods. At the same time, the inclusion complex was identified by X-ray diffraction (XRD) and differential scanning calorimetry (DSC). ResultsIt was demonstrated that the solubility of irisquinone was enhanced markedly by inclusion with HP-β-CD when stoichiometry was 2∶1 of host and guest at 25 ℃, 35 ℃ and 45 ℃. ConclusionThe solubility and stability of irisquinone could be increased by preparing the inclusion complex with hydroxypropyl-β-cyclodextrin.

     

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