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目的:研究7 名健康志愿者单剂量口服茶碱控释胶囊( 简称CRTC)400 mg 后的药物动力学。方法:用紫外法测定健康人血清中茶碱的血药浓度。结果:CRTC的药物动力学参数分别为:Tmax = (7 .9 ±1.1)h,Cmax = (4.0 ±0 .9)μg·ml-1 ,T1/2e =(17 .2±2 .6)h,Ke =(0.04±0.06)h-1 ,T1/2a= (2 .1±0 .9)h,Ka=(0.23±0.04)h- 1 ,AUC072 = (138 .0±17 .6)μg·h·ml- 1 。结论:CRTC的药物动力学参数与国产茶碱控释片( 简称DCRTT)[1] 相比:其吸收减慢,导致达峰时间延长,达峰浓度降低。但其消除减慢,CRTC在体内蓄积,致使其药时曲线下的面积较DCRTT 大。
OBJECTIVE: To study the pharmacokinetics of 400 mg single-dose oral theophylline controlled-release capsules (CRTC) in seven healthy volunteers. Methods: The plasma concentration of theophylline in healthy human serum was determined by UV method. Results: The pharmacokinetic parameters of CRTC were: Tmax = (7.9 ± 1.1) h, Cmax = (4.0 ± 0.9) μg · ml-1, T1 / 2e = Ke = (0.04 ± 0.06) h-1, T1 / 2a = (2.1 ± 0.9) h, Ka = 0.23 ± 0.04 h-1 , AUC0 72 = (138.0 ± 17.6) μg · h · ml-1. CONCLUSION: The pharmacokinetic parameters of CRTC are lower than those of domestic controlled-release tablets of theophylline (DCRTT) [1], leading to prolonged peak time and decreased peak concentration. However, its elimination slowed down and the accumulation of CRTC in the body resulted in a larger area under the drug curve than that of DCRTT.