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目的:建立比格犬血浆中阿克他利浓度的定量分析方法,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:比格犬6只采用双周期交叉给药的实验方法,测定阿克他利在比格犬血浆内的浓度,用DAS2.0程序拟合药物浓度-时间曲线,求算药物动力学参数。结果:阿克他利缓释片和普通片在比格犬体内过程均符合单室一级吸收模型,剂量校正后与普通片相比,阿克他利缓释片tmax,t1/2延长,Cmax降低,平均生物利用度为(108.9±11.5)%。结论:阿克他利缓释片具有明显的缓释特征,生物利用度与市售普通片等效。
OBJECTIVE: To establish a quantitative method for the determination of concentration of acitalin in Beagle dog plasma and to determine the pharmacokinetics and relative bioavailability of sustained-release tablets in dogs. Methods: Six beagle dogs were treated with double-cycle crossover test to determine the concentration of acetaliplatin in Beagle dog’s plasma. The drug concentration-time curve was fitted by DAS 2.0 program to calculate the pharmacokinetic parameters . Results: The contents of acetaminophen sustained-release tablets and common tablets in beagle dogs were in accordance with the single-chamber first-order absorption model. Compared with the normal tablets, the dextromethorphan sustained-release tablets tmax and t1 / 2 were prolonged, Cmax decreased, the average bioavailability was (108.9 ± 11.5)%. Conclusion: Acitally sustained-release tablets have a sustained-release characteristics, bioavailability and commercial tablets equivalent.