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目的制备包封率高、稳定性好,具有缓释效果的硫酸黄连素多囊脂质体,并对其体外释放进行考察。方法采用复乳法制备硫酸黄连素多囊脂质体,以包封率为指标,采用正交实验优选处方,并考察体外释放及缓释效能。结果制得硫酸黄连素多囊脂质体,显微镜下可见其圆整均匀,内部具有规整囊泡结构;正交设计优选药脂质量比为1∶8,卵磷脂与胆固醇质量比为2∶1,中性磷脂三油酸甘油酯的浓度为70 mmol/L,海藻酸钠的浓度为0.5%,按优选处方制得硫酸黄连素多囊脂质体包封率为85.88%,具有良好缓释效能,72h累积释放度为83.28%,释放曲线符合Weibull模型方程。结论采用复乳法制得硫酸黄连素多囊脂质体圆整均匀,包封率高,具有良好的缓释效能。
OBJECTIVE To prepare polyclonal liposomes with high encapsulation efficiency, good stability and sustained release effect and to investigate its in vitro release. Methods Polyclonal liposomes were prepared by double emulsion method. The encapsulation efficiency was used as an index, and the prescription was optimized by orthogonal test. The release and sustained release of berberine sulfate were investigated. Results The berberine sulfate multilocularis liposomes were found to be round and uniform under the microscope with a regular vesicle structure inside. The optimum orthogonal design was that the mass ratio of lipid to lipid was 1: 8, the mass ratio of lecithin to cholesterol was 2: 1 , Neutral phospholipid triolein concentration of 70 mmol / L, sodium alginate concentration of 0.5%, according to the preferred prescription obtained berberine sulfate encapsulation efficiency of 85.88%, with good sustained release Efficacy, cumulative release 72h was 83.28%, release curve in line with Weibull model equation. Conclusions The double-liposome-encapsulated liposomes obtained by double-emulsion method are round and uniform, with high encapsulation efficiency and good sustained-release efficiency.