摘要
目的:制备氯霉素固体脂质纳米粒(CAP-SLN)并考察其质量。方法:选取CAP与甘油棕榈酸硬脂酸酯(PrecirolATO5)比例(药脂比)、泊洛沙姆含量、乳化温度和初乳-分散相的体积比为考察因素,包封率和载药量为评价指标,设计正交试验并优化处方,利用乳化蒸发-低温固化法制备CAP-SLN;同时以粒径、Zeta电位、包封率、载药量、稳定性及体外释放度为指标评价其质量。结果:最佳制备处方药脂比为1∶10,泊洛沙姆含量为2%,乳化温度为70℃,初乳-分散相的体积比为1∶7。所制纳米粒平均粒径为227nm,Zeta电位为-30.5mV,平均包封率为65.9%,平均载药量为6.59%;于4℃环境中考察30d,其包封率、粒径无显著变化,25℃环境中包封率显著降低、粒径明显增大;在前4h内有明显突释现象,药物累积释放率达58.86%,48h时累积释放率达85.09%,体外释药行为符合Weibull方程。结论:该制剂处方设计和工艺方法可行,制剂质量符合要求,可达到缓释效果。
OBJECTIVE： To prepare Chloramphenicol solid lipid nanoparticles （CAP-SLN） and to study the quality of it. METHODS： The preparation technilogy of CAP-SLN was optimized by orthogonal test with the entrapment efficiency and drug loading amount as index and with proportion of CAP to Precirol ATO 5 （drug-to-lipid ratio）, amount of poloxamer, emulsifying temperature, volume ratio of emulsion-disperse phase as factors. CAP-SLN was prepared by emulsification evaporation-low temperature solidification technique. The quality of preparation was evaluated with particle size, Zeta potential, drug-loading amount, stability and in vitro drug release rate as index. RESULTS： The optimal formulation was as follows： drug-to-lipid ratio of 1 ： 10, the weight of poloxamer of 2%, emulsifying temperature of 70℃, drug-to-lipid of 1：7. The mean diameter of CAP-SLN was 227 nm. The zeta potential was --30.5 mV. The entrapment efficacy was 65.9%. The average drug-loading amount was 6.59%. CAP-SLN could keep stable at 4 ℃ at least for one month. The entrapment efficacy of CAP-SLN at 25 ℃ decreased significantly while particle size increased. The burst release of CAP-SLN was found during the former 4 h. The drug release rate of it was 58.86% at 4 h and reached 85.09% at 48 h. The in vitro drug release behavior was in line with Weibull equation. CONCLUSION： The preparation technique and formulation are practicable. CAP-SLN is up to quality standard and can achieve sustained-release effects.
出处
《中国药房》
CAS
CSCD
北大核心
2011年第17期1598-1601,共4页
China Pharmacy
