摘要
目的:制备胸腺五肽脂质体并进行质量评价。方法:采用复乳法制备胸腺五肽脂质体,以聚乳酸-羟基乙酸共聚物(PLGA)及卵磷脂为成球材料、以胸腺五肽为主药制备脂质体。以明胶浓度、PLGA浓度和卵磷脂浓度为考察因素,以包封率和载药量为考察指标设计L(934)正交试验优化基质处方并进行验证试验。通过测定优化处方所制脂质体粒径、包封率、体外累积释放百分率等评价脂质体质量。结果:优化基质处方为明胶、PLGA和卵磷脂浓度分别为100、200、100mg.mL-1。所制脂质体形态完整,平均粒径为(9.03±0.83)μm,载药量与包封率分别为(1.81±0.03)与(74.4±1.4),20d的累积释药百分率达90以上。结论:所制胸腺五肽脂质体工艺简单、重现性好,包封率和载药量高,具有显著的缓释作用。
OBJECTIVE： To prepare thymopentin liposomes and to evaluate the quality of it. METHODS： Thymopentin liposomes were prepared by double emulsion process using poly （lactic-co-glycolic acid） （PLGA） and lecithin as carrier and thymopentin as main components. The preparation method was optimized by orthogonal experiment L9（34） using the concentration of gelatin, PLGA and lecithin as factors and with encapsulation coefficency and drug loading capacity as index. The particle size, encapsulation coefficency and in vitro accumulative release rate of liposomes were determined to evaluate the quality of it. RESULTS： The concentrations of gelatin, PLGA and lecithin in optimal base formula were 100 mg. mL^-1, 200 mg. mL^-1, 100 mg. mL^-1, respecetively. Prepared liposomes were complete in shape with mean particle size of （9.03 ± 0.83） μm. The drug loading capacity and encapsulation coefficiency were （1.81 ± 0.03）% and （74.4 ±1.4）%. Accumulative release rate was more than 90% in 20 days. CONCLUSION： Preparation technology is simple and reproducible. Prepared thymopentin liposomes have high drug loading capacity and encapsulation coefficiency, and sustained-release effect.
出处
《中国药房》
CAS
CSCD
北大核心
2011年第17期1595-1597,共3页
China Pharmacy
关键词
胸腺五肽
聚乳酸-羟基乙酸共聚物
脂质体
制备
优化基质处方
正交试验
质量评价
Thymopentin
Poly （lactic-co-glycolic acid）
Liposomes
Preparation
Optimal base formula
Orthogonal experiment
Quality evaluation
作者简介
硕士研究生。研究方向：药物新剂型。E-mail：p03570311@163．com
通讯作者：教授，硕士研究生导师。研究方向：生化制药。E-mail：hongxinsong@163．com
