中文摘要：

目的制备一种能够缓释盐酸环丙沙星的局部用纤维膜。方法以药物水溶液为水相,聚L-乳酸的二氯甲烷溶液为油相,Poloxamer188为乳化剂,探头超声制备W/O乳液后静电纺丝将体系拉制成纤维,采用扫描电子显微镜观察纤维形态,采用广角-X射线衍射扫描法观察纤维表面有无药物结晶析出,采用差示热分析评价药物在高分子纤维中的结合状态。采用碘-碘化钾络合显色法测定Poloxamer188的释放量,采用高效液相色谱法测定蛋白酶K存在下纤维中环丙沙星的释放量。结果扫描电子显微镜观察制备得到直径较为均一的纤维膜,乳液静电纺丝所得纤维直径大于均相溶液纺丝,乳液纺丝所得纤维表面有微小孔状结构。广角X-射线衍射结果表明纤维表面无药物结晶析出,差示热分析结果表明环丙沙星在纤维亦为非结晶状态存在。随着Poloxamer188添加量的增多,其本身从纤维中的释放量逐渐增大,纤维中药物释放速率加快,蛋白酶K亦能够加快药物的释放。结论 W/O乳液静电纺丝法能够制备得到对水溶性药物有缓释作用的纤维膜。

英文摘要：

Objective To prepare a kind of fibrous membrane for locally sustained delivery ciprofloxacin hydrochloride. Methods W / O emulsion were prepared under ultrasonic probe action by using drug solution as the aqueous phase,poly L-lactic acid dicloromethane soluiton as the oil phase and Poloxamer188as the emulsifier. Fibers were prepared by electrospinning the emulsion in a drawing way. Fibers morphology were observed by scanning electron microscope. Drug crystals on fibrous surfaces were detected by by WAXD and drug-polymer combination states were evaluated by differential thermal analysis. Iodine-potassium iodide complexing coloration was used for determining Poloxamer188release behavior. HPLC was used for determining ciprofloxacin hydrochloride release behavior under proteinase K degradation. Results Fibers with homogeneous diameters were prepared under the observation of scanning electron microscope. Fibers prepared by emulsion-electrospinning process presented diameter smaller than fibers prepared from homogeneous solution-electrospinning. There were tiny holes existing on the fiber surface,meanwhile,there were no drug crystal emerging on the fiber surface by wide angle X-ray diffraction detection,and differential thermal analysis indicated that drug existed in fibers as the non-crystal states. As the amount of Poloxamer188increased,it made itself release amount increased,and along with,drug released faster.Proteinase K increased the drug release speed. Conclusions By using W / O emulsion electrospinning method,fibrous membranes for sustained release hydrophilic drug could be prepared.