离心造粒法制备酒石酸美托洛尔缓释微丸及其在犬体内生物利用度

程娟 ,田丽娟,周建平,谢俊*

中国药学杂志 ›› 2013, Vol. 48 ›› Issue (14) : 1174-1177.

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中国药学杂志 ›› 2013, Vol. 48 ›› Issue (14) : 1174-1177. DOI: 10.11669/cpj.2013.14.009
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离心造粒法制备酒石酸美托洛尔缓释微丸及其在犬体内生物利用度

  • 程娟1 ,田丽娟1,周建平2,谢俊1*
作者信息 +

Preparation of Metoprolol Tartrate Sustained-Release Pellets by Centrifugal Granulation and the Relative Bioavailability in Beagle Dogs

  • CHENG Juan1, TIAN Li-juan1,ZHOU Jian-ping2,XIE Jun1*
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文章历史 +

摘要

目的 制备酒石酸美托洛尔缓释微丸并考察其在Beagle犬体内生物利用度。方法 离心造粒法制备酒石酸美托洛尔载药丸芯,以圆整度、粒度分布和收率、脆碎度和流动性为指标,采用正交设计法优化丸芯的处方,以苏丽丝水分散体包衣制备缓释微丸。结果 最佳处方工艺为载药量90%、黏合剂用量40 mL·100 g-1、滚圆速率30 Hz;包衣增重12%,老化条件为60 ℃、2 h。 结论 制备酒石酸美托洛尔缓释微丸,与市售制剂相比在犬体内具有生物等效性。

Abstract

ObjectiveTo prepare metoprolol tartrate sustained-release pellets and investigate the relative bioavailability in Beagle dogs. Methods Taking aspect ratio(AR), circularity, yield, friability, fluidity as key indexes, orthogonal design was atopted to optimize the formulation,and sustained-release pellets were prepared with Surelease. Results The optimal formulation was as follows: drug loading rate 90%, adhesive 40 mL·100 g-1, spheronization rate 30 Hz, coating weight gain 12%, and aging at 60 ℃ for 2 h. Conclusion The prepared metoprolol tartrate sustained-release pellets are bioequivalent with Betaloc in Beagle dogs.

关键词

酒石酸美托洛尔 / 离心造粒 / 缓释微丸 / 生物利用度

Key words

metoprolol tartrate / centrifugal granulation / sustained-release pellet / bioavailability

引用本文

导出引用
程娟 ,田丽娟,周建平,谢俊*. 离心造粒法制备酒石酸美托洛尔缓释微丸及其在犬体内生物利用度[J]. 中国药学杂志, 2013, 48(14): 1174-1177 https://doi.org/10.11669/cpj.2013.14.009
CHENG Juan, TIAN Li-juan,ZHOU Jian-ping,XIE Jun*. Preparation of Metoprolol Tartrate Sustained-Release Pellets by Centrifugal Granulation and the Relative Bioavailability in Beagle Dogs[J]. Chinese Pharmaceutical Journal, 2013, 48(14): 1174-1177 https://doi.org/10.11669/cpj.2013.14.009
中图分类号: R944   

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