在Y型微通道反应器中,采用反溶剂沉淀法制备头孢呋辛酯纳米颗粒。通过正交实验,系统研究药物溶液质量浓度、沉淀温度、溶剂流量和反溶剂流量等因素对产物粒径的影响。得到的适宜制备工艺条件为:药物溶液质量浓度0.08g/mL、沉淀温度5℃、溶剂流量3mL/min,以及反溶剂流量80mL/min,制备出了粒径为260—340nm,且粒径分布窄的纳米颗粒。实验还进一步利用扫描电镜、X射线衍射、红外光谱分析和体外溶出实验对原料药及产品性质进行表征,结果表明:微粉化产品为无定形,溶出度明显优于原料药。
Nanosized cefuroxime axetil (CFA) particles have been prepared by using an antisolvent precipitation method in a Y-junction microchannel. The effects of the CFA concentration, precipitation telnperature, CFA solution flow rate and antisolvent flow rate on the particle size were investigated by orthogonal tests, and the following optimum conditions were obtained : a CFA solution mass concentration of 0.08 g/mL, a precipitation temperature of 5 ℃ , a CFA solution flow rate of 3 mL/min and an antisolvent flow rate of 80 mL/min. Under these conditions, CFA nanoparticles with an average size of 260 - 340 nm and narrow particle size distribution were obtained. The crude drug and the as-prepared nanosized product were characterized by SEM, XRD, FT-IR and dissolution tests. The results indicated that as-prepared CFA nanoparticles were amorphous, and displayed significantly enhanced dissolution properties compared to the crude CFA.