【摘要】 目的探讨对以羧甲基壳聚糖为载体的氟尿嘧啶微球体外释药特性的影响因素。方法超声作用下采用乳化交联法制备氟尿嘧啶羧甲基壳聚糖微球(Fu-CMCS-MS);光镜观察微球的形态和粒径分布;恒温振荡透析法和紫外分光光度法测定Fu-CMCS-MS的药物释放,考察5种因素对微球体外释药的影响。结果超声作用下制得Fu-CMCS-MS成球性良好,粒径分布均匀,微球76.4%在1~3μm,平均粒径1.6μm。微球体外释药受投药方式、投药量、交联剂、释放介质和超声作用的影响显著,前期释药速率快,遵守溶胀控制机制,缓释后期释药缓慢,遵守扩散控制机制。结论超声作用下以戊二醛乳化交联所制Fu-CMCS-MS在体外具有缓释作用。更多还原

【Abstract】 Objective To study the release characteristics of fluorouracil-loaded carboxymethyl chitosan microspheres(Fu-CMCS-MS) in vitro.Methods Fu-CMCS-MS was prepared by emulsion cross-linking technique in ultrasonication.The surface morphology and grain size distribution of the microspheres were analyzed by light microscope.The effects of different factors on fluorouracil released from Fu-CMCS-MS were observed by vibration dialysis assay and ultraviolet spectrophotometry.Results The diameter of 76.4% of microspheres was about 1~3 μm,and the average diameter was 1.6 μm.Fluorouracil release from Fu-CMCS-MS significantly influenced by administration modality,drug loading,release medium,and ultrasonication,etc.Drug release at the initial period was fast in parallel to swelling behavior and was slow at the later period by a diffusion mechanism.Conclusion Fluorouracil released from Fu-CMCS-MS was sustained in vitro.更多还原