头孢匹胺钠脂质体的制备及其理化性质研究

目的：制备头孢匹胺钠脂质体并进行质量评价。方法：采用逆相蒸发法制备头孢匹胺钠脂质体，在单因素考察基础上，以药脂比（A）、磷脂与胆固醇质量比（B）、有机相（乙醚）与水相体积比（C）、超声时间（D）为因素，以包封率为考察指标，按Lq（3‘）正交试验设计表优化最佳处方和工艺，并进行处方验证；考察脂质体的形态，测定其粒径、Zeta电位、包封率、栽药量和72h体外累积释放度并进行模型拟合。结果：正交试验设计优化的A为1：6、B为5：1、C为4：1、D为5min，验证试验证明处方合理；所得的脂质体为封闭的多层囊状或圆球体，大小均匀，平均粒径为（7．146±O．29）gm，Zeta电位为一11．75mV，包封率为（82．10±4．21）％，载药量为（愠42±O．67）％；72h体外累积释放度为76．84％，体外释药行为符合We~bull模型（r=0．9910）。结论：采用逆相蒸发法制备的头孢匹胺钠脂质体，包封率较高，体外释药有明显的缓释效果。

Preparation and Physicochemical Property of Cefpiramide Sodium Liposome

OBJECTIVE： To prepare Cefpiramide sodium liposome, and to evaluate its physicochemical property. METHODS： Cefpiramide sodium liposome was prepared by reverse phase evaporation method. Based on single factor test, the formulation and preparation technology were optimized by L~（34） orthogonal experiment with the ratio of drug to lipid （A）, the ratio of phospha- tides to cholesterol （B）, the ratio of organic phase （ether） to water phase （C） and ultrasound time （D） as factors using entrapment efficiency as index. The morphology of the liposome was investigated, and particle size, Zeta potential, entrapment efficiency, drug-loading amount and 72 h accumulative release rate in vitro were determined. RESULTS： The optimal formulation was as fol- lows ： A was 1 ： 6, B was 5 ： 1, C was 4 ： 1 and D was 5 rain. Validation test showed that the formulation was reasonable. Prepared liposome was closed multilayer cystiform or spherical shape, with uniform size. The mean diameter, Zeta potential, entrapment effi- ciency, drug-loading amount and 72 h accumulative release rate in vitro were （ 7.146 ± 0.29） gm, -- 11.75 mV, （82.10 ± 4.21 ） %, （15.42 ± 0.67）% and 76.84%, respectively. The drug release of the liposome was consistent with Weibull＇ s model （r=0.991 0）. CONCLUSIONS： Cefpiramide sodium could be encapsulated liposome with higher encapsulation efficiency using reverse phase evaporation method, and the liposome has a good sustained-release property in vitro.