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目的:建立犬血浆中雷诺嗪的定量分析方法,测定其在犬体内的血药浓度经时过程,评价缓释片的药动学及相对生物利用度。方法:采用双周期自身交叉设计,分别单剂量给予犬雷诺嗪缓释片和普通片,用HPLC法测定血浆中的雷诺嗪浓度,用DAS2.0程序拟合药物浓度-时间曲线,计算药动学参数和相对生物利用度。结果:与普通片相比,雷诺嗪缓释片tmax、t1/2延长,Cmax降低,相对生物利用度为(100.47±42.55)%。结论:雷诺嗪缓释片具有缓释特征。
OBJECTIVE: To establish a quantitative method for the determination of ranolazine in canine plasma and to determine the pharmacokinetics and relative bioavailability of sustained-release tablets in dogs over time. Methods: Double-cycle self-crossover design was used to treat canine Ranolazine sustained-release tablets and normal tablets respectively. Plasma concentrations of Ranolazine were determined by HPLC. Drug concentration-time curves were fitted by DAS 2.0 program. Learning parameters and relative bioavailability. Results: The ranolazine sustained-release tablets extended tmax, t1 / 2 and Cmax decreased compared with conventional tablets. The relative bioavailability was (100.47 ± 42.55)%. Conclusion: Ranolazine sustained-release tablets have sustained-release characteristics.