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目的:制备缓释1月以上的氟尿嘧啶(Fu)聚丙交酯微球。方法:溶剂挥发法制备Fu聚丙交酯微球,比较外水相Fu饱和与否,有机相Fu/聚丙交酯投料比对载药量及包封率的影响。光学及电子显微镜下对微球的外观形态进行考察,并对其体外释放进行初步探讨。结果:制得的微球光滑圆整。Fu饱和外水相后可以提高其载药量及包封率,投料比对载药量、微球的粒径和跨距影响不大,包封率随投料比增大而减小。Fu从聚丙交酯微球中4周时约释放总量的65％,符合一级动力学,没有明显的突释效应。结论:外水相Fu饱和后可减少Fu向外水相的逸失,制得的微球可作为每月1次的给药系统。
Objective: To prepare fluorouracil (Fu) polylactide microspheres sustained release for more than 1 month. Methods: Fu polylactide microspheres were prepared by solvent evaporation method. The effect of Fu / poly (lactide - co - glycolide) ratio on drug loading and entrapment efficiency of organic phase Fu was compared. Optical microscopy and electron microscopy of the morphology of microspheres were investigated, and its in vitro release of a preliminary study. Results: The prepared microspheres were smooth and round. Fu saturated external aqueous phase can increase its drug loading and encapsulation efficiency, feed ratio on drug loading, microspheres particle size and span less, encapsulation efficiency decreases with the feed ratio increases. Fu from polylactide microspheres about 4 weeks release about 65% of the total, in line with the first-order kinetics, there is no obvious burst effect. Conclusion: After the outer aqueous phase Fu is saturated, the escape of Fu to the outer aqueous phase can be reduced. The prepared microspheres can be used as a once-a-month delivery system.