摘要
为改善三叶苷溶解度、油水分配系数和溶出度,制备了三叶苷-磷脂复合物,并对理化性质进行考察。以复合率为指标,单因素考察结合Box-Behnken设计-效应面法优化三叶苷-磷脂复合物处方工艺。测试三叶昔-磷脂复合物的溶解度、溶出度和油水分配系数,采用X射线衍射法、红外光谱法、差式扫描量热法进行分析。结果表明,三叶苷-磷脂复合物最佳处方工艺为三叶苷用量为60mg,磷脂用量为125mg,制备温度为50℃,制备时间为3.9h,三叶苷与磷脂的复合率达99.7%。与三叶苷相比,三叶苷-磷脂复合物溶解度及油水分配系数得到极显著性改善,12h累积释放度增加至75.1%。三叶苷在三叶苷-磷脂复合物中转变为无定型状态。三叶苷和磷脂之间可能以氢键结合在一起形成三叶苷-磷脂复合物。本研究成功制备了三叶苷-磷脂复合物,改善了自身理化性质的缺陷,为进一步应用奠定了基础。
In order to improve the solubility,oil-water partition coefficient and dissolution rate of tilobatin,tilobatin-phospholipids complex was prepared,and its physicochemical properties were also investigated.Recombination rate was employed as evaluation index,single factor analysis combined with Box-behnken design-response surface methodology was used to optimize the formulation of trilobin-phospholipids complex.Solubility,dissolution rate and oil-water partition coefficient were determined.X-ray diffraction,infrared spectroscopy and differential scanning calorimetry method were employed to analysis its physicochemical properties.Results showed that the optimized formulations of trilobin-phospholipids complex were as follows:trilobin dose was 60 mg,phospholipids dose was 125 mg,preparation temperature was 50℃and preparation time was 3.9 h.Recombination rate of trilobin-phospholipids complex was 99.7%.Compared to tilobatin,solubility and oil-water partition coefficient of tilobatin-phospholipids complex were significantly improved,and cumulative release rate in 12 h increased to 75.1%.The crystalline state of tilobatin changed to amorphous state in the complex.A hydrogen bond might be formed between trilobin and phospholipids to form the complex.In this study tilobatin-phospholipids complex were successfully prepared,defects of physicochemical properties of tilobatin were resolved,which laid a foundation for further application.
作者
尚慧杰
王颖慧
郝海军
SHANG Hui-jie;WANG Ying-hui;HAO Hai-jun(Department of Pharmacy,Zhengzhou Shuqing Medical College,Zhengzhou 450064,China;Department of Pharmacy,Shanghai Institute of Traditional Chinese Medicine,Shanghai 201401,China)
出处
《化学研究与应用》
CAS
北大核心
2024年第11期2724-2730,共7页
Chemical Research and Application
基金
河南省科技攻关项目(232102310384)资助
上海市科委项目(21S21903400)资助。
关键词
三叶苷
磷脂复合物
溶解度
溶出度
tilobatin
phospholipids complex
solubility
release rate
