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1. 西南医科大学附属医院肝胆外科
2. 西南医科大学药学院药剂学教研室
3. 西南医科大学附属医院肿瘤科
纸质出版日期:2016,
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[1]黎靖,魏郁梦,杨红茹,黄玉,赵领.氟尿嘧啶中空微球的制备、表征及释药性能[J].重庆医科大学学报,2016,41(05):448-452.
Li Jing, Wei Yumeng, Yang Hongru, et al. Preparation,characterization and drug release property of fluorouracil hollow microspheres[J]. Journal of Chongqing Medical University, 2016,41(5):448-452.
[1]黎靖,魏郁梦,杨红茹,黄玉,赵领.氟尿嘧啶中空微球的制备、表征及释药性能[J].重庆医科大学学报,2016,41(05):448-452. DOI: 10.13406/j.cnki.cyxb.000734.
Li Jing, Wei Yumeng, Yang Hongru, et al. Preparation,characterization and drug release property of fluorouracil hollow microspheres[J]. Journal of Chongqing Medical University, 2016,41(5):448-452. DOI: 10.13406/j.cnki.cyxb.000734.
目的:制备氟尿嘧啶(fluorouracil
FU)中空微球
并考察其体外释药行为。方法:在单因素考察基础上
选择主药FU(A)、乙基纤维素(ethyl cellulose
EC)(B)和聚乙烯吡咯烷酮(polyvinylpyrrolidone
PVP)(C)为因素
各因素取3个水平进行L9(33)拉丁正交设计试验
以释放度为指标优化处方工艺。结果:基于正交试验释放度指标的综合评分
筛选最佳处方配比为FU(0.6 g)、EC(1 g)、PVP(0.1 g);优化处方工艺制备的氟尿嘧啶中空微球在0.5、1、2、4、8、12、24 h的体外累积释放3批的平均百分率分别为(9.88±0.38)%、(14.64±0.09)%、(23.94±0.67)%、(39.21±0.36)%、(57.53±0.83)%、(67.99±0.58)%、(80.34±0.39)%
P值为0.001;其体外释药模型为:0
8
h按一级方程释药[Ln(1-Q)=-0.072 1t-0.563 7
r=0.998 6
P值为0.001]
8
2
4 h按Higuchi方程释药(Q=0.102 3t1/2+0.398 7
r=0.999 9
P值为0.001)。结论:制备的FU中空微球体外缓释效果良好
有望为FU长效制剂的开发奠定基础。
Objective:To prepare fluorouracil(FU)hollow microspheres
and to evaluate its in vitro release behavior. Methods:On the basis of single-factor test
three factors[FU
ethyl cellulose(EC)and polyvinylpyrrolidone(PVP)] three-leveled orthogonal experimental design L9(33)was carried out with the in vitro release as marker for optimization. Results:The optimization formulation composed of FU:EC:PVP(0.6:1.0:0.1
w/w)was obtained based on the orthogonal experiment with comprehensive score of the in vitro release.Mean cumulative in vitro release of three batches of FU hollow microspheres prepared using the optimization formulation at 0.5
1
2
4
8
12
24 h was(9.88±0.38)%
(14.64±0.09)%
(23.94±0.67)%
(39.21±0.36)%
(57.53±0.83)%
(67.99±0.58)%
(80.34±0.39)%
respectively(P=0.001). The in vitro release models at 0-8 h and 8-24 h were prescribed by the one-level equation[Ln(1-Q)=-0.072 1 t-0.563 7
r =0.997 3
P =0.001] and Higuchi equation(Q =0.102 3t1/2+0.398 7
r =0.999 9
P =0.001)
respectively.Conclusion:Perfect sustained release effect is obtained for fluorouracil hollow microspheres in this study. This study would lay the foundation for the development of fluorouracil prolonged action preparation.
氟尿嘧啶中空微球释放度正交实验
fluorouracilhollow microspheresrelease rateorthogonal experiment
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