甘氨酸茶碱钠缓释片与普通片药物动力学对比

采用一步液液提取反相高效液相色谱法对甘氨酸茶碱钠缓释片 (受试制剂 )与普通片 (参比制剂 )在人体内药物动力学行为进行了对比检测 ,绘制了 12名健康男性志愿受试者分别单剂量和多剂量随机交叉口服上述两种制剂后的茶碱血浆浓度 时间曲线并计算主要的药动学参数 .经统计检验 ,两种制剂的AUC无显著性差异 .单剂量和多剂量口服甘氨酸茶碱钠缓释片的相对生物利用度分别为 (91.7± 16 .8) %和 (10 7.5± 18.6 ) % .与普通片相比 ,甘氨酸茶碱钠缓释片的Cmax较低 ,而Cmin较高 ,Tmax明显滞后 ,MRT延长 ,血药浓度波动幅度显著减小 ,符合缓释制剂的特点 ,可较为安全地应用于临床 .

Comparative Study of the Pharmacokinetics of Theophylline Sodium Glycinate Sustained-Release Tablets and Conventional Tablets

The pharmacokinetics of a new sustainedrelease Tablet,theophylline sodium glycinate sustainedrelease tablet (Test formulation) was studied in comparison with that of a conventional tablet,Ganfeilin Tablet (Reference formulation).The theophylline concentrations in plasma were determined by the liquidliquid extractionRPHPLC method with UV detector and the plasma concentrationtime curves were plotted after a single oral dose as well as multiple oral doses of a 100 mg sustainedrelease tablet and 165 mg conventional tablet in 12 Chinese healthy male volunteers according to a randomized 2way crossover design.The main pharmacokinetic parameters of the two formulations and the relative bioavailability of the sustainedrelease tablet were obtained.The results of the statistical analysis showed no significant difference between the AUC values of the two formulations.The oral relative bioavailabilities of the sustainedrelease tablet if compared with the conventional tablet were (91.7±16.8)% for a single dose and (107.5± 18.6 )% for multiple doses respectively. Compared with the conventional tablet, the sustainedrelease tablet had lower C max , higher C min and prolonged T max and MRT.The peak to trough fluctuation index(FI) of the sustainedrelease tablet was less than that of the conventional tablet.The above data demonstrated that the theophylline sodium glycinate sustainedrelease tablet possessed good characteristics of sustainedrelease formulation and was fitted to be safely used in clinical treatment.