不同固化液对相分离微球体外性质的影响

Effect of Different Solidified Liquid on in vitro Properties of Phase Separation Microspheres

本研究的目的是对比油酸乙酯和正庚烷两种体系的固化液对相分离法所制备的醋酸奥曲肽微球体外性质的影响.固定相分离阶段处方工艺,改变2种固化液体系中乙醇含量,以形貌、粒径、载药量、溶剂残留及体外累计释放为指标,对比2种体系形成的微球体外性质差别.结果表明,增加乙醇的用量,微球载药量、药物突释量降低,且能够减少二氯甲烷在微球内的残留量.在乙醇加入量相同的情况下,油酸乙酯体系形成的微球体外释放快于正庚烷体系形成的微球.2种不同固化液的对比研究为更好地理解相分离法微球形成过程提供了一种新的思路.

The purpose of this study is to compare the effects of ethyl oleate and n -heptane on the in vitro properties of octreotide microspheres prepared by phase separation technique. Under the same phase separation conditions, the content of ethanol is changed in the two systems. The morphology, particle size, drug loading, solvent residue and in vitro cumulative release are studied to compare the properties of the microspheres formed in the two systems. The results show that the drug loading, burst release and the residual of dichloromethane in the microspheres can be reduced with the increase of ethanol content. In the case of the same content of ethanol, the in vitro release rate of the microspheres solidified in ethyl oleate system is higher than that solidified in n -heptane system. The comparison of the two different solidification solutions provides a new idea to better understand the microsphere formation in phase separation process.