Preparation of Atenolol Sustained-Release Pellets and Its Pharmacokinetics in Rat

Objective:To prepare Atenolol(AT) 24-hour sustained-release pellets and to investigate its pharmacokinetics in rats.Methods:The pellets which containing AT were prepared through the method of extrusion-spheronization and then coated with Glatt fluidized bed.The rats were given AT immediate-release and sustained release pellets,respectively,and their plasma were extracted by methylene dichloride and determined by HPLC.Finally,the pharmacokinetic parameters were calculated by PKsolver software.Results:The cumulative release percents of AT sustained-release pellets in 2,12 and 24 h were(21.31± 1.12)%,(70.82±1.47)% and(91.87±1.71)%,respectively.The technological process could be steadily performed.The data calculated by PKsolver software showed that AT immediate-release and sustained release pellets were fitted to two-and one-compartment models,respectively.The Tmax value of AT immediate-release and sustained release pellets were(2.679±0.142)h and(10.430±1.225)h,respectively;Cmax value were(1.238±0.144)mg·L-1 and(0.356±0.031)mg·L-1,MRT value were(12.559±0.414)h and(21.764± 1.992)h,respectively.Conclusion:The prepared AT sustained release pellets showed evident effect of sustained release both in vitro and in vitro.