克林霉素几丁糖缓释微球的制备及其体外缓释作用的研究

Preparation of Clindamycin Loaded Chitosan Sustained-Release Microspheres and Drug Release Study in Vitro

目的:制备克林霉素几丁糖缓释微球,测定其载药量和包封率,考察其体外缓释作用和抑菌作用。方法:采用乳化化学交联法制备克林霉素几丁糖缓释微球,应用透射电子扫描显微镜和激光衍射式粒度分布测量仪观察微球的形态和粒径,采用紫外分光光度法测定克林霉素几丁糖缓释微球的载药量和包封率。建立体外释放体系,研究微球的体外药物缓释作用和体外抑菌作用。通过绘制抑菌环时间面积曲线观察微球的体外抑菌作用。结果:克林霉素几丁糖缓释微球的大小均匀,分散性较好,平均粒径为(153.2±13.7)μm,载药量为(39.8±1.6)%,包封率为(79.6±3.5)%。在PH7.4的磷酸盐缓冲液中,克林霉素几丁糖缓释微球的累计释放率第1小时为16.5%,第2小时为21.6%,第3小时为33.2%,第24小时达53.7%;克林霉素对照品第3小时的累计释放率已达99.6%。载药微球的抑菌面积时间曲线表明,释药3 d后载药微球仍具有明显的抑菌作用。结论:克林霉素几丁糖缓释微球具有良好的药物包封率,故体外缓释作用和体外抑菌作用较好。

Objective：To prepare clindamycin loaded chitosan sustalned‐release microspheres ,determine drug loading and drug encapsulation efficiency of the microspheres ,and observe the effect of sustalned‐release and bacteriostasis in vitro .Methods：The microspheres were prepared by emulsified chemical cross‐linking method . The morphology and particle size of microspheres were observed by transmission electron microscopy and laser diffraction particle size analyzer .The drug loading and drug encapsulation efficiency of clindamycin loaded chitosan sustalned‐release microspheres were tested by UV spectrophotometry method .The effect of drug sustalned‐release and bacteriostasis in vitro was studied by establishing release system in vitro .The bacteriostasis of microspheres in vitro was observed by plotting the area‐time curve of inhibition ring . Results：The size of clindamycin loaded chitosan sustalned‐release microspheres was uniform ,while the dispersion was good . The average particle size of the microspheres was （153 .2 ± 13 .7）μm .The average drug loading was（39 .8 ＆± 1 .6）% .The mean encapsulation efficiency was （79 .6 ±3 .5）% .The cumulative release percentage of clindamycin loaded chitosan sustalned‐release microspheres in pH 7 .4 phosphate buffer saline（PBS） was 16 .5% at the first hour ,21 .6% at the second hour ,33 .2%at the third hour and 53 .7% at the twenty‐fourth hour .The cumulative release percentage of clindamycin control was 99 .6% at the third hour .The microspheres still had obvious bacteriostasis after 3 days’ release ,as the bacteriostasis time area curve of the drug loaded microsphere showed .Conclusions：The encapsulation efficiency of clindamycin loaded chitosan sustalned‐release microspheres was good ,so that the sustalned‐release effect and bacteriostsis in vitro was also good .