唑来膦酸脂质体分析方法及处方工艺优化研究  

Study on analysis method and formulation optimization of zoledronic acid liposomes

作　　者：景莎莎 梁宇 胡海洋[3] Jing Shasha;Liang Yu;Hu Haiyang(Drug Clinical Trial Institution,Xi'an International Medical Center Hospital,Shaanxi710100,China;不详)

机构地区：[1]西安国际医学中心医院药物临床试验机构,710100 [2]深圳市博德维环境技术股份有限公司西安分公司 [3]沈阳药科大学药学院

出　　处：《山西医药杂志》2022年第19期2182-2185,共4页Shanxi Medical Journal

摘　　要：目的建立一种唑来膦酸脂质体(ZOL-LIPs)的包封率测定方法,以解决唑来膦酸水溶性强、含量不易测定的问题,并提高药物包封率。方法通过建立一种新的制备方法即逆相蒸发法制备ZOL-LIPs,利用高效液相色谱法(HPLC)与超滤离心法测定其包封率,并采用单因素考察法探索最佳处方工艺,使药物的包封率显著提高。结果采用HPLC法能够准确测定药物含量,超滤离心法能有效地将游离药物与脂质体分离,在得到的最佳处方和工艺条件下制备的ZOL-LIPs包封率为39.63%。结论即使唑来膦酸属于末端吸收,建立的HPLC-超滤离心法也可快速、准确地测定ZOL-LIPs的包封率,处方优化后的包封率相对于通常的制备方法得到大幅提高。Objective To establish a method for the determination of the encapsulation efficiency(EE)of Zoledronic Acid Liposomes(ZOL-LIPs),in order to solve the problem of strong water solubility and difficult determination of ZOL,and to improve the EE of ZOL.Methods ZOL-LIPs were prepared by an innovative method of reverse-phase evaporation.High-performance liquid chromatography(HPLC)and ultrafiltration centrifugation were used to determine the EE of the ZOL,and the Single-Factor Experiment was used to explore the optimal formulation process,in order to improve the EE of the ZOL.Results The drug content could be accurately determined,and the free drug could be separated through the ultrafiltration centrifugation method effectively from ZOL-LIPs.The EE of ZOL-LIPs was 39.63%under the optimal formulation and process conditions.Conclusion Even if zoledronic acid was terminal absorption,the EE of ZOL-LIPs could be determined by the established HPLC-ultrafiltration centrifugation method.The EE of the optimized formalation was greathy improved compared with the preparation method.

关 键 词：唑来膦酸 脂质体 色谱法 液相 超滤离心法 逆相蒸发法 包封率 

分 类 号：R943[医药卫生—药剂学]