眼科用汉防已甲素联合5-氟尿嘧啶壳聚糖微球的制备及其质量评估

Preparation and characteristics of tetrandrine combined with 5-fluorouracil chitosan microspheres for ophthalmology

目的制备汉防已甲素(Tet)联合5-氟尿嘧啶(5-FU)壳聚糖缓释微球并观察微球质量。方法以壳聚糖为载体,采用乳化交联法制备Tet联合5-FU壳聚糖微球。在单因素考察的基础上,利用正交试验设计,优化微球制备工艺,并对制得微球的粒径、形态、工艺重复性及稳定性、体外突释情况等进行观察。结果制得的微球形态圆整,粒径为(80.4±1.34)μm,其中粒径60～100μm的微球占总数的89.5%;载药量:5-FU为10.42%,Tet为16.83%;微球包封率:5-FU为58.23%,Tet为47.02%;最佳工艺条件重复性良好。结论成功制备了Tet联合5-FU壳聚糖微球,其质量优良。

Objective To prepare the tetrandrine（Tet） combined with 5-fluorouracil（5-FU） chitosan microspheres（Tet-5-FU-CS-MS）,and evaluate its characteristics.Methods The microspheres were prepared by emulsion chemical crosslinking method using chitosan as carrier.Based on the result of single factor selecting experiment,the preparation methods were evaluated by orthogonal experiment method.The mean diameter,the size distribution of microspheres,the drug loading rate,the encapsulation efficiency,the reproducibility of pharmaceutical technology and the stability of optimized microspheres were all examined.Results The Tet-5-FU-CS-MS was morphological regular.The average particle size of the microspheres was（80.4 ± 1.34） μm,with 89.5% of the microspheres being in the range of 60 ～ 100 μm.The drug loading rate of 5-FU and Tet was 10.42% and 16.83% respectively.The encapsulation efficiency of 5-FU and Tet was 58.23% and 47.02 % respectively.The reproducibility and stability of pharmaceutical technology was desirable.Conclusion The optimized preparation could prepare Tet-5-FU-CS-MS of eligible quality.