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
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Key words
metoprolol tartrate /
centrifugal granulation /
sustained-release pellet /
bioavailability
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中图分类号：
R944
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参考文献
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