摘要
目的 比较不同方法制得布比卡因人血清白蛋白微球的理化特性。方法 采用乳化热固化法和高压电场法制备布比卡因人血清白蛋白微球 ,通过均匀设计考察乳化热固化法制备工艺条件对微球粒径、释药速率、载药量和包封率的影响 ,以高效毛细管电泳法 (HPCE)测定微球的体外释放度。结果 搅拌速度和药物 蛋白浓度比可分别显著影响粒径大小和药物包封率。不同粒径大小微球的释放行为表明 ,随着微球粒径增大 ,其释放行为愈符合Higuchi方程 ,微球粒径愈小 ,愈符合一级动力学释放模式。高压电场法与乳化热固化法制备工艺相比 ,高压电场法制备微球的粒径分布集中 ,跨度由 1 98缩小为 0 5 2 ,包封率由原来的 5 0 87%提高到 91 6 2 %。结论 高压电场法是一种简单、可行的白蛋白微球制备新方法。
OBJECTIVE: To prepare bupivacaine human serum albumin microspheres (Bupi-HSA-MS)by two different methods and compare the physical and chemical characteristics of the two products. METHODS: The emulsifing heat-denatured method and high voltage electric electrostatic heat-denatured method were used to prepare Bupi-HSA-MS using uniform design. The effect of preparing condition on particle size, release rate, drug content and drug entrapment efficiency were researched. High performance capillary electrophoresis (HPCE) was established to determine the release of Bupi-MS. RESULTS: The result showed that particle size and the drug entrapment efficiency were affected by stirring rate (P < 0.01) and drug/HSA concentration ratio evidently (P < 0.01). The release experiment showed that the release rate was faster with smaller particle size and the release mode of Bupi-HSA-MS with large particle size could be described by Higuchi equation better, and that of small particle could be described by First order equation. High voltage electric electrostatic heat-denatured method increased the drug entrapment efficiency, decreased the burst effect and improved the reproduction ratio of preparation. The span of particle size was decreased from 1.98 to 0.52, the drug entrapment efficiency was increased from 50.87% to 91.62% with the new method compared with emulsifing heat-denatured method. CONCLUSION: High voltage electrc electrostatic heat-denatured method is a simple and feasible method for preparing Bupi-HSA-MS.
出处
《中国药学杂志》
EI
CAS
CSCD
北大核心
2004年第6期446-449,共4页
Chinese Pharmaceutical Journal
关键词
布比卡因
白蛋白微球
制备工艺
理化特性
Capillarity
Electric potential
Electrophoresis
Electrostatics
Emulsification
Mass spectrometry
Particle size analysis
Proteins
