目的:采用A23187制备重酒石酸长春瑞滨长循环脂质体,优化了处方工艺,并考察了含量、包封率、药脂比和体外释放等检测指标。方法:采用A23187介导的pH梯度法制备了重酒石酸长春瑞滨脂质体;用HPLC法检测了脂质体中重酒石酸长春瑞滨的含量和脂质(HSPC)的含量,考察了药脂比;采用阳离子交换树脂分离脂质体和游离药物,HPLC法检测包封率;以4 mmol.L-1NH4Cl-PBS(pH 7.4)为体外释放介质考察了脂质体的体外释放行为。结果:重酒石酸长春瑞滨脂质体包封率为96.1%,药脂比为1∶5(w/w);高药脂比有利于延长药物体外释放的时间。结论:采用A23187介导的pH梯度法制备重酒石酸长春瑞滨脂质体工艺可行、载药量大、包封率高;所建立体外释放的检测方法快速、准确。 OBJECTIVE: A23187 was used to prepare vinorelbine palmitate long-circulating liposomes, the prescription was optimized, and the detection indexes such as content, entrapment efficiency, drug-lipid ratio and in vitro release were investigated. Methods: The vinorelbine bitartrate liposome was prepared by A23187-mediated pH gradient method. The content of vinorelbine tartrate and the content of lipid (HSPC) in liposomes were determined by HPLC. The liposomes and free drugs were separated by cation exchange resin. The encapsulation efficiency was determined by HPLC. The in vitro release behavior of liposomes was investigated with 4 mmol·L-1 NH4Cl-PBS (pH 7.4) as in vitro release medium. Results: The entrapment efficiency of vinorelbine bitartrate liposomes was 96.1%, and the ratio of lipid to lipid was 1: 5 (w / w). The high drug-lipid ratio was beneficial to prolong the drug release in vitro. Conclusion: A23187-mediated pH gradient method for the preparation of vinorelbine bitartrate liposome technology feasible, drug loading, encapsulation efficiency; the established in vitro release of the detection method is fast and accurate.