5-氟尿嘧啶羧甲基壳聚糖微球体的制备及体外释放

Chitosan-Fluorouracil Preparation and its Releasing Test in vitro

目的 探讨羧甲基壳聚糖包药微球体的制备及体外释药特性。 方法 采用乳化交联法制备 5 氟尿嘧啶羧甲基壳聚糖 (FU CMCS)微球体 ;用红外光谱 (IR)对其结构进行表征 ,扫描电子显微镜 (SEM )观察微球体形貌及表面结构 ,利用激光粒度分布仪考察微球体的粒径分布 ;考察包药微球体在人工胃液、人工肠液、人工结肠液中的释放。 结果 电镜扫描显示微球体表面结构规整、致密 ,FU CMCS微球体粒径 6 0 %在 2～ 15 μm ,药物含量为 8 39%。体外释放实验表明 ,包药微球体在 pH 1 2 2、pH 7 0 1、pH 7 4 5缓冲溶液中均具有缓释作用。 结论 FU CMCS微球体在体外具有缓释作用。

Objective To prepare carboxymethyl chitosan microspheres of fluorouracil(FU-CMCS-MS), and measure the releasing of FU-CMCS-MS in vitro. Methods FU-CMCS-MS was prepared by cross-linking-emulsion method. The surface structure of chitosan-fluorouracil preparation were checked with IR spectra and SEM photography. Grain size distribution of the micropheres was analysed. The releasing of FU-CMCS-MS were investigated in simulated gastric solution(pH 1.22), enteric fluid(pH 7.01) and simulated colon fluid(pH 7.45), respectively. Results The SEM photos group showed that the surface of FU-CMCS-MS was regular, smooth and dense. The diameter of the 60% of micropheres were about 2～15 μm. The drug content of micropheres was 8.39%(W/W). Sustained release of FU-CMCS-MS were observed both in pH 1.22, pH 7.01, pH 7.45 buffer solution. Conclusion Fluorouracil release from FU-CMCS-MS was sustained in different pH condition.