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制备高乌甲素(1)磷脂酰胆碱复合物并考察复合物的基本性质。对制备的1复合物进行X射线衍射(XRD)、差示扫描量热法(DSC)、核磁共振(NMR)等分析,并考察复合物的溶解性能。结果表明,磷脂酰胆碱复合物中1以无定形状态存在,推测1与磷脂酰胆碱发生氢键或分子间作用力,但未形成新的化合物。1磷脂酰胆碱复合物显著改善了1在水和正辛醇中的表观溶解度,在一定程度上提高了溶出速率及累积释放率,有利于提高其生物利用度。
Preparation of lappaconitine (1) phosphatidylcholine complexes and investigate the basic properties of the complex. The prepared composite 1 was analyzed by X-ray diffraction (XRD), differential scanning calorimetry (DSC) and nuclear magnetic resonance (NMR). The solubility of the complex was also investigated. The results showed that phosphatidylcholine complex 1 in the presence of an amorphous state, presumably a hydrogen bond with the phosphatidylcholine or intermolecular force, but did not form a new compound. 1 phosphatidyl choline complex significantly improves the apparent solubility of 1 in water and n-octanol, to a certain extent, improve the dissolution rate and cumulative release rate, is conducive to improving its bioavailability.