摘要
目的通过优化手段筛选最佳处方及工艺,制备马钱子碱长循环脂质体,并评价其质量。方法采用乙醇注入式硫酸铵梯度法制备马钱子碱长循环脂质体,用聚乙二醇修饰脂质体膜。考察马钱子碱长循环脂质体的形态、粒径分布、pH值、包封率、初步稳定性和体外释放行为。结果优化后的脂质体颗粒圆整、平均粒径为120 nm,平均pH值为6.655,包封率达到93.72%,在4℃条件下稳定性良好,体外释放效果优于马钱子碱磷酸缓冲液。结论脂质体制备工艺可行,药剂学性质稳定。
OBJECTIVE To determine optimized prescription and technique for preparing brucine long-circulating liposomes（BLCL） by means of optimization screening, and to evaluate its quality, METHODS BIlL were prepared by the technique of ammonium sulphate gradients with ethanol injection. The poly（ ethylene glycol） （PEG） was added to modify the membrane of the lipesomes. The shape of BIlL is surveyed under the microscope. The size of BLCL was investigated by laser particle analyzer. The pH, the entrapment efficiency and the result of stability experiment were examined. The in vitro release of brucine from long-circulating liposomes in PBS（pH 7.4） was determined by HPLC. RESULTS BLCL were round, regular in morphology with mean particle size of 120 um, and its average pH of 6.655. The entrapment efficiency of BLCL was up to 93.72%. The stability was good in 4℃ and BLCL had better sustained-released effect than brueine phosphoric acid buffer solution. CONCLUSION This preparation of BLCL is practicable and the pharmaceutical characterization showed stable.
出处
《中国药学杂志》
CAS
CSCD
北大核心
2006年第18期1397-1400,共4页
Chinese Pharmaceutical Journal
基金
国家自然科学基金资助项目(90209052)
关键词
马钱子碱
长循环脂质体
硫酸铵梯度法
质量评价
brucine
long-circulating liposomes
ammonium sulphate gradients
quality evaluation
