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

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

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。

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.