鼠李素磷脂复合物的处方工艺优化、表征及体外溶出度考察  

Optimization and characterization of isorhamnetin-phospholipids complex and evaluation of dissolution in vitro

作　　者：陈晓敏 曹伶俐 崔伟峰[2] CHEN Xiao-min;CAO Ling-li;CUI Wei-feng(Zhengzhou Health Vocational College,Henan Zhengzhou450199,China;Henan Academy of Chinese Medicine,Henan Zhengzhou 450004,China)

机构地区：[1]郑州卫生健康职业学院,河南郑州450199 [2]河南中医药研究院,河南郑州450004

出　　处：《中国医院药学杂志》2022年第4期399-403,共5页Chinese Journal of Hospital Pharmacy

基　　金：河南省高等学校重点科研项目计划(编号:21B360011)。

摘　　要：目的:制备异鼠李素磷脂复合物,考察其基本性质。方法:采用复合率为指标,单因素试验和正交试验优化异鼠李素磷脂复合物处方工艺,并对磷脂复合物进行紫外分光光度法、X射线衍射法、差示扫描量热、扫描电镜分析;比较异鼠李素及其磷脂复合物在不同pH值的油水分配系数,转篮法比较异鼠李素及其磷脂复合物的溶出度。结果:按照正交试验得出的最佳处方工艺,异鼠李素磷脂复合物的复合率达到99.29%。异鼠李素在磷脂复合物中转变为无定形态,且物相发生了改变,但异鼠李素磷脂复合物不是新的化合物。异鼠李素磷脂复合物在不同pH值的油水分配系数对数值(lgP)为1.14~1.56。磷脂复合物大大提高了异鼠李素的累积溶出度。结论:成功制备了异鼠李素磷脂复合物,为下一步研究工作奠定了基础。OBJECTIVE To prepare isorhamnetin-phospholipids complex and investigate its physicochemical properties.METHODS Taking recombination rate as evaluation index, single factor and orthogonal test were employed to optimize the preparations of isorhamnetin-phospholipids complex.The complex was analyzed by ultraviolet and visible spectrophotometry(UV),X-ray powder diffraction(XRPD),differential scaning calarmeutry(DSC)and scanning electronic microscopy(SEM).The oil/water partition coefficient of isorhamnetin and its phospholipids complex in different pH values were compared.Dissolution rates of isorhamnetin and its phospholipids complex were compared by rotating basket method.RESULTS According to the optimum preparations obtained by orthogonal test, the recombination rate of isorhamnetin-phospholipids complex could achieve 99.29%.Isorhamnetin was an amorphous form in the phospholipids complex, and its phase has changed, but not a new compound.The logarithm of oil/water partition coefficient of isorhamnetin-phospholipids complex was 1.14-1.56 in different pH values.Cumulative dissolution of isorhamnetin was improved greatly by phospholipids complex.CONCLUSION Isorhamnetin-phospholipids complex was prepared successfully, which lays a foundation for the further research work.

关 键 词：异鼠李素 磷脂复合物 无定形态 溶出 

分 类 号：R943[医药卫生—药剂学]