阿莫西林聚氰基丙烯酸丁酯纳米粒的制备及其质量评价  

Preparation and quality evaluation of amoxicillin polybutylcyanoacrylate nanoparticles.

作　　者：杨雪峰[1,2] 欧阳五庆[1] 刘玉梅[1] 张文娟[1] 孙江才[1] 

机构地区：[1]西北农林科技大学动物医学院,陕西杨凌712100 [2]河南科技学院动物科学学院,河南新乡453003

出　　处：《浙江大学学报（农业与生命科学版）》2009年第2期195-200,共6页Journal of Zhejiang University:Agriculture and Life Sciences

基　　金：国家科技支撑计划奶业发展重大关键技术研究与示范"资助项目(2006BAD04A11)

摘　　要：以氰基丙烯酸丁酯(BCA)为载体,采用乳化聚合法制备阿莫西林聚氰基丙烯酸丁酯纳米粒(AMX-PBCA-NP),通过单因素试验考察和均匀设计法优化制备工艺,并对AMX-PBCA-NP进行质量评价.结果表明,经优化筛选出制备AMX-PBCA-NP的处方工艺为阿莫西林4g·L-1,BCA10mL·L-1,泊洛沙姆F6810g·L-1,dextran-7010g·L-1,反应液pH3.0.按优化条件制备的AMX-PBCA-NP形态圆整,无粘连,分布均匀,平均粒径为(222.33±1.53)nm,多分散系数为0.03±0.02,平均包封率为(73.47±0.96)%,平均载药量为(29.39±0.38)%,体外释药特性符合双相动力学释药规律,对大肠杆菌(Escherichia coli)ATCC25922和金黄色葡萄球菌(Staphylococcus aureus)ATCC25923的最小抑菌浓度(MIC)均为原料药的1/2倍.结果提示,AMX-PBCA-NP的制备工艺切实可行,阿莫西林纳米化后具有缓释特性且体外抗菌活性增强.Amoxieillin polybutylcyanoacrylate nanoparticles （AMX-PBCA-NP）were prepared by the emulsion polymerization method with butylcyanoaerylate（BCA） as a carrier material. The preparation procedure was optimized according to the results of single factor experiments and uniform design tests, and then the quality of AMX-PBCA-NP was evaluated. The results show that the screened optimum conditions for the preparation of AMX-PBCA-NP were 4 g·L^-1 amoxicillin, 10 mL· L^-1 BCA, 10 g· L^-1 pluronic F68, 10 g · L^-1 dextran-70 and pH 3.0. The prepared nanopartieles were globular, unconglutinate, well-distributed. The mean diameter of the particles was （222.33 ± 1.53 ） nm, polydispersity index was 0.03±0.02, the mean encapsulation ratio and drug-load was （73.47±0.96） and （29.39±0.38）%, respectively. The release characteristics in vitro were consistent with two phases kinetics rule. The minimal inhibitory concentration （MIC） against E. coli ATCC25922 and S. aureus ATCC25923 was 1/2 times of the MIC of active pharmaceutical ingredients, respectively. The results above suggested that the optimal preparation procedure of AMX-PBCA-NP is practicable, AMX-PBCA- NP has the slow-release character and the antibacterial activity of amoxicillin is enhanced in vitro.

关 键 词：阿莫西林 纳米粒 聚氰基丙烯酸丁酯 均匀设计 质量评价 

分 类 号：R944[医药卫生—药剂学] S859[医药卫生—药学]