盐酸多西环素羧甲基壳聚糖微球的制备

Study on the preparation technology of doxycycline hydrochloride-carboxymethyl chitosan-microspheres

目的:星点设计法优化盐酸多西环素羧甲基壳聚糖微球(doxycycline hydrochloride-carboxymethyl chitosan-micro-spheres,DXY-CMCTS-MS)的处方。方法:采用乳化-交联固化法制备DXY-CMCTS-MS。以载药量、包封率、收率为指标,采用星点设计优化制备工艺,扫描电镜和光学显微镜观察微球表面形态;体外动态透析法测定微球的释药性能。结果:制备的DXY-CMCTS-MS形态圆整,粒径分布较为均匀,平均粒径(25.0±8.0)μm,载药量18.90%,包封率64.64%,收率为58.96%。DXY-CMCTS-MS在PBS(pH7.4)溶液中具有明显的缓释效果。结论:优化的DXY-CMC-MS制备工艺可控易行,载药量高,缓释作用良好。

OBJECTIVE To optimize the preparation of doxycycline hydrochloride-carboxymethylchitosan-microspheres（DXY-CMCTS-MS） by central composite design.METHODS DXY-CMCTS-MS was carried out by emulsifying cross-linking process.The central composite design was applied to optimize the formulation and preparation procedure with loading dose,encapsulation efficiency,yield as index.The surface morphology of the microspheres was observed under scanning electron microscope（SEM） and the optical microscope,the dynamic dialysis method was used to determine the release characteristic of doxycycline hydrochloride from microspheres in vitro.RESULTS DXY-CMCTS-MS with a global shape and narrow distribution were prepared.The average diameter was（25.0±8.0）μm,the drug loading rate was 18.90%,and the envelop efficiency was 64.64%,the yield was 58.96%.The release behavior of drug had obvious sustained release effect in phosphate buffered saline（pH=7.4）.CONCLUSION The optimized preparation technique was controllable and feasible.The microspheres were demonstrated with high drug-loading rate and evident effect of sustained drug release.