青藤碱乳酸羟基乙酸共聚物-水溶性维生素E纳米粒的制备及处方工艺优化  

Optimization of Preparation and Formula Technique of Sinomenine-loaded Polylactic-co-glycolic Acid/D-α-tocopherol Polyethylene Glycol 1000 Succinate Nanoparticles

作　　者：徐红[1] 高萌[2] 张成鸿[1] 徐静[1] 孙艺平[1] 王洪刚[3] 

机构地区：[1]大连医科大学基础医学院,辽宁大连116044 [2]大连医科大学药学院,辽宁大连116044 [3]大连医科大学附属第一医院药剂科,辽宁大连116011

出　　处：《中国药房》2015年第4期525-528,共4页China Pharmacy

摘　　要：目的:为了提高青藤碱的稳定性并减慢其释放,制备青藤碱乳酸羟基乙酸共聚物-水溶性维生素E(PLGA-TPGS)纳米粒(SPTN)并对其处方工艺进行优化。方法:以PLGA-TPGS为载体,采用超声乳化-溶剂挥发法制备SPTN,以粒径、载药量和包封率为评价指标,通过单因素考察和正交设计试验优化青藤碱与载体的配比、乳化剂TPGS水溶液的浓度(g/100 ml)、超声功率和超声时间,并对最优处方进行验证。结果与结论:成功制得SPTN。最优处方工艺为青藤碱与载体配比为3∶10、TPGS水溶液浓度为0.06 g/100 ml、超声功率为200W、超声时间为6min。所制备的3批SPTN的平均粒径、载药量和包封率分别为(194.6±2.8)nm、(9.5±0.7)%、(41.3±1.6)%。OBJECTIVE： To prepare Sinomenine （SIN）-loaded polylactic-co-glycolic acid/D-a-tocopherol polyethylene glycol 1000 succinate （PLGA-TPGS） nanoparticles （SPTN） and optimize its formula technical conditions in order to improve the stability of SIN and slow down the release of it. METHODS ： SPTN were prepared by ultrasonic emulsion/solvent evaporation technique us- ing PLGA-TPGS as carrier. Using particle size, drug-loading amount and entrapment efficiency as index, single factor and orthogo- nal design were adopted to optimize the ratio of SIN to PLGA-TPGS, concentration of TPGS, ultrasonic power and ultrasonic time. The optimal formula was validated. RESULTS ＆ CONCLUSIONS： SPTN is prepared successfully. The optimal formula was as fol- lows with the ratio of SIN to PLGA-TPGS 3 ： 10, concentration TPGS 0.06 g/100 ml, ultrasonic power 200 W, ultrasonic time 6 min. Mean particle size, drug-loading amount and entrapment efficiency were （194.6 ± 2.8） nm, （9.5 ± 0.7） % and （41.3 ± 1.6） %, respectively.

关 键 词：青藤碱 纳米粒 乳酸羟基乙酸共聚物-水溶性维生素E 粒径 载药量 包封率 

分 类 号：R284.62[医药卫生—中药学] R284.2[医药卫生—中医学]