Preparation and Quality Evaluation of Roxithromycin Microspheres / 中国药房

ABSTRACT

OBJECTIVE:To optimize the preparation technology of roxithromycin microspheres.METHODS:The microspheres of roxithromycin were prepared by the emulsion-solvent diffusion method with ethylcellulose used as capsule wall material.The preparation technology of microspheres was optimized by orthogonal experiment taking encapsulation efficiency as index with the ratio of roxithromycin to ethylcellulose(A),the concentration of ethylcellulose(B)and the ratio of water phase to oil phase(C)as factors.The appearance,particle diameter,drug-loading amount,encapsulation efficiency,in vitro release and bitter smell were studied.RESULTS:The optimal preparation conditions were as followsA was 1∶1,B was 30 ?g?mL-1 and C was 4∶1.The microspheres obtained were round and well-distributed with mean diameter of 75.0～90.0 ?m,drug-loading amount of 45%～46%,encapsulation efficiency of over 90% and sustained release for over 13 hours.No bitter taste of the roxithromycin-ethylcellulose microspheres was felt by the majority of subjects.CONCLUSION:The roxithromycin microspheres made by optimization technology was bitter-masked and sustained release.