【摘要】 目的:研制甲硝唑缓释微球并装于结肠溶胶囊,评价其体外释放特性。方法:用乳化交联法制备甲硝唑羧甲基壳聚糖微球,测定平均粒径、载药量、包封存率等指标;将微球和原料药分别装于结肠溶胶囊,测定微球、原料药及结肠溶胶囊剂型在人工胃液、人工小肠液、人工结肠液中的释放性能。结果:重复制备6批微球,微球平均粒径为(197.1±3.9)μm,载药量为(48.2±1.5)%,包封率为(37.5±1.9)%;体外释放甲硝唑原料药0.75h释放完全,甲硝唑微球7h释放完全;甲硝唑原料药结肠溶胶囊和甲硝唑微球结肠溶胶囊,在人工胃液、人工小肠液5h均无释放,移至人工结肠液后,前者于6.25h释放完全,后者于13h释放完全。结论:甲硝唑羧甲基壳聚糖微球的制备工艺稳定,甲硝唑羧甲基壳聚糖微球结肠囊胶囊具有结肠定位及缓释性能。更多还原

【Abstract】 OBJECTIVE To prepare metronidazole-loaded sustained-release microspheres,filled in colonic-coated capsules,and investigate the in vitro release characteristics.METHODS The metronidazole-loaded carboxymethyl chitosan microspheres were prepared by emulsification and cross-linking process. The mean diameter of the microspheres,the amount of drug in the microspheres and the entrapment efficiency were surveyed. The mertonidazole-loaded microspheres and the mertonidazole powder were respectively put into colonic-coated capsules. The in vitro release was observed in the artificial gastric juice,the artificial small intestinal juice and the artificial large intestinal juice.RESULTS The microspheres were repeatedly prepared for 6 times. The mean diameter of the microspheres was (197.1±3.9)μm ,the amount of drug in the microspheres was (48.2±1.5)%,and the entrapment efficiency was (37.5±1.9)%. The release of metronidazole in powder reached to about 100% at 0.75 h. The release of metronidazole in microshperes reached to about 100% at 7 h. The release of metronidazole in the colonic-coated capsule containing mertonidazole powder was not not surveyed within 5 h in the artificial medium of stomach and small intestine,while in the artificial large intestinal juice the release reached to about 100% at 6.25 h. The release of metronidazole in colonic-coated capsules containing mertonidazole-loaded microshperes was not surveyed within 5 h in the artificial medium of stomach and small intestine,while in the artificial large intestinal juice the release reached to about 100% at 13 h.CONCLUSION The technology of preparing metronidazole-loaded carboxymethyl chitosan microspheres is dependable,and the colonic-coated capsule containing mertonidazole-loaded microshperes has the colon-targeted and sustained-release characteristics.更多还原