氟尿嘧啶白蛋白微球的制备及体外性质研究

Study on the Preparation and Properties in Vitro of Fluorouracil Albumin Microspheres

对氟尿嘧啶白蛋白微球的制备及形态与粒径分布、载药量与包封率、体外释药动力学、初步稳定性等体外性质进行了研究。研究结果表明：微球呈规则球形,粒径范围为0.15～098μm,跨距为0.65,平均粒径为0.56μm;载药量与包封率分别为6.13％和90.38％;体外释药呈双相特征,快速释放相（0.5～4h）用Higuchi方程描述：Q=0.125t1/2-0.0484（r=0.9809）,t50=19.25h;缓慢释药相（6～120h）用HiguChi方程拟合;Q=0.0230t1/2＋0.218（r=0.9418）,t50=150.33h;所得微球于4℃密封保存三个月,稳定性良好。

The preparation of fluorouracil bovine serum albumin microspheres (Fu-BM) and properties in witro,including morphology and size distribution, drug loading and drug trapping efficiency, release characteristic and stability, are presented in this study. The results show that Fu-BM are spherical, the diameter of Fu-BM ranges from 0. 15-0. 98μm, span is 0. 65, and the average diameter is 0. 56μm. The drug loading, and drug trapping efficiency of Fu-BM is 6. 13% and 90. 38% respectively. In the process of 5-Fu release, there are two phases.The first phase (O. 5-4 h) is regarded as a quick release phase, and the release characteristics comply with Higuchi equation: Q=0.125t1/2-0.0484 (r=0.9809), t50= 19. 25 h. The second phase (6-120 h) is a slow release phase, and also follows the HiSuchi equation: Q=0.0230t1/2+0.218 (r=0.9418), t50=150. 33 h. Fu-BM stored at 4℃, was found to be stuble at least for 3 months as the results indicated.