液中干燥法制备阿莫西林微囊及其溶出度考察

Preparation of Amoxicillin-ethylcellulose Microcapsule by In-liquid Drying Method and Its Dissolution Study

目的：制备阿莫西林微囊，并考察其溶出度。方法：采用液中干燥法制备微囊。以囊心与囊材的质量比（A）、分散相与连续相的体积比（B）、聚乙二醇4000（PEG4000）的用量（C）为因素，以微囊的圆整度和产率为指标，采用L9（3^4）正交试验优化工艺条件，验证处方并考察其粉体学性质、粒径和12h内的累积溶出度。结果：正交试验优化的A为1：0．8、B为1：3．5、C为8．O％；验证试验证明处方合理，所得的微囊大小均匀，其粉体学性质中平均圆整度为13．97°、平均堆密度为0．787g／ml、平均脆碎度为O．89、平均产率为72．0％；粒径在24-28目间可达70％以上；12h内的累积溶出度为90％～95％。结论：制备的微囊符合缓释制剂要求，处方较为合理，工艺较好控制。

OBJECTIVE： To prepare Amoxicillin microcapsule, and to investigate the dissolution of the microcapsule. METH- ODS： The microcapsule was prepared by in-liquid drying method. The preparation technology of the microcapsule was optimized by L（34） orthogonal test with mass ratio of capsule core to material （A）, volume ratio of dispersed phase to continuous phase （B）, the amount of PEG4000 （C） as factors with roundness and yield as index. The powder property, particle size and 12 h accumulative release rate of microcapsule were investigated and the formulation was validated. RESULTS： Optimized preparation technology was as follows： A was 1 ： 0.8; B was 1 ： 3.5; C was 8.0%. Validation test showed that the prescription was reasonable and the microcapsule was uniform in size. The property of microcapsule power was as follows： roundness of 13.97 o, average bulk density of 0.787 g/ml, average friability of 0.89, average yield of 72.0% ; particle size of 70% microcapsule above ranged 24 to 28 meshes; 12 h accumulative release rates were 90%-95%. CONCLUSIONS： The prepared microcapsule conforms to the requirements of the sustained-release preparations, and the formulation is reasonable and controlled in process.