肝动脉栓塞米托蒽醌乙基纤维素微球的制剂学研究

肝动脉栓塞米托蒽醌乙基纤维素微球的制剂学研究

张志荣, 王丹, 廖方义, 廖工铁

成都华西医科大学药学院, 成都 610044

收稿日期:1996-04-11 修回日期:1996-09-16 出版日期:1996-12-15 发布日期:1996-12-15

Mitoxantrone Ethylcellulose Microspheres for Liver Arte-rial Embolization

Zhi-Rong Zhang, Dan Wang, Fang-Yi Liao, Gong-Tie Liao

School of pharmacy, West China University of Medical Sciences Chengdu 610044

Received:1996-04-11 Revised:1996-09-16 Online:1996-12-15 Published:1996-12-15

摘要/Abstract

摘要： 利用正交实验设计法优选适用于肝动脉栓塞的米托蒽醌乙基纤维素微球制备条件和工艺, 采用动态透析法模拟体内情况研究了该微球的体外释药规律; 根据混悬液的稳定性理论, 优选并制备了适于临床肝动脉介导栓塞使用的米托蒽醌乙基纤维素微球混悬注射液。结果表明: 在优化工艺条件下制得的米托蒽醌乙基纤维素微球外观圆整, 球径在50~150 μm范围内的占总数的86.5%, 平均球径为110.24±38.19 μm; 包封率为55.6%; 载药量为12.5%, 体外释药符合单指数模型, 释药方程为log(Y∞-Y) = -0.116t - 1.198 × 10^-3 (r = 0.9992, t50 = 2.6 h); 其混悬注射液理化性质稳定, 可适于临床应用。

关键词: 米托蒽醌, 乙基纤维素微球, 肝动脉栓塞

Abstract: Herein, the orthogonal test was used to optimize the preparation conditions and technique of mitoxantrone ethylcellulose microsphere (DHAQ-EC-MS)for liver arterial embolization.The dynamic dialysis method was used to study the drug release characteristics ofthe DRAQ-EC-MS.The suspension of DHAQ-EC-MS for clinical liver arterial embolization was prepared.The results show that the DHAQ-EC-MS is regular in morphology with a mean diameter of 110.24±38.19 μm and 86.5% of them within the range of 40-150μm, The drug loading is 12.5% and the embedding ratio is 55.6%. The release characteristics were in accordance with the single exponential model.The drug release equation is log(Y∞-Y) = -0.116t - 1.198 × 10^-3 (r = 0.9992, t50 = 2.6 h). The suspension is ofstable physical and chemical properties and is suitable for clinical use.

Key words: Mitoxantrone, Ethylcellulose microsphere, Liver arterial embolization

Supporting:

张志荣, 王丹, 廖方义, 廖工铁. 肝动脉栓塞米托蒽醌乙基纤维素微球的制剂学研究[J]. .

Zhi-Rong Zhang, Dan Wang, Fang-Yi Liao, Gong-Tie Liao. Mitoxantrone Ethylcellulose Microspheres for Liver Arte-rial Embolization[J]. .

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