Preparation of metoprolol tartrate sustained-release pellets by centrifugal granulation and the relative bioavailability in Beagle dogs / 中国药学杂志

ABSTRACT

OBJECTIVE: To 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°C for 2 h. CONCLUSION: The prepared metoprolol tartrate sustained-release pellets are bioequivalent with Betaloc in Beagle dogs.