论文部分内容阅读
目的:制备吴茱萸碱超分子复合物(EVO-PLC),并考察其体外溶出。方法:以吴茱萸碱(EVO)和磷脂的复合率为评价指标,通过单因素试验优化磷脂复合物的制备工艺。采用薄层色谱法,紫外光谱法验证磷脂复合物的形成,并测定其粒径和Zeta电位。用Weibull模型拟合法和相似因子(f2)法考察磷脂复合物的体外溶出动力学。结果:超分子磷脂复合物的最佳制备工艺为:以四氢呋喃为反应溶剂,磷脂与吴茱萸碱的物质的量的比为2∶1,吴茱萸碱的反应浓度为1.5 mg·mL-1,反应温度为60℃,反应时间为3 h;最优工艺的复合率为(92.01±0.11)%,粒径为(248.03±9.15)nm,Zeta电位为(-24.68±3.97)mV;薄层色谱法提示吴茱萸碱与磷脂复合过程中没有生成新物质;紫外光谱法提示吴茱萸碱与磷脂之间存在相互作用,而非简单的物理混合,溶出动力学结果表明吴茱萸碱磷脂复合物的溶出符合Weibull模型,相似因子(f2)法结果表明EVO通过与磷脂复合促进了EVO的体外溶出。结论:本文制备得到了工艺简单、复合率较高的吴茱萸碱超分子磷脂复合物,通过制备磷脂复合物大大增加了吴茱萸碱的体外溶出。
Objective: To prepare evodiamine (EVO-PLC) and study its dissolution in vitro. Methods: The composite ratio of evodiamine (EVO) and phospholipid was used as evaluation index to optimize the preparation process of phospholipid complex by single factor experiment. The formation of phospholipid complex was confirmed by TLC and UV spectroscopy, and its particle size and Zeta potential were measured. In vitro dissolution kinetics of phospholipid complexes was investigated by Weibull model fitting and similarity factor (f2). Results: The optimum preparation conditions for the supramolecular phospholipid complex were as follows: the amount of phospholipid and evodiamine was 2:1, the evusate concentration of evodiamine was 1.5 mg · mL-1, the reaction temperature Was 60 ℃ and the reaction time was 3 h.The recombination rate in the optimal process was (92.01 ± 0.11)%, the particle size was (248.03 ± 9.15) nm and the zeta potential was (-24.68 ± 3.97) mV. The thin layer chromatography Evodiamine and phospholipids did not produce new substances during the complexing process. Ultraviolet spectroscopy indicated that there was interaction between evodiamine and phospholipids, rather than simple physical mixing. The dissolution kinetics indicated that the dissolution of evodiamine phospholipid complex was in accordance with Weibull model The factor (f2) results show that EVO promotes the in vitro dissolution of EVO by complexing with phospholipids. CONCLUSION: The evodiamine phospholipid complex with simple process and high recombination rate was prepared in this paper. The evodiamine phospholipid complex greatly increased the evusate of evodiamine in vitro.