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目的:对常规剂量时茶碱非线性代谢进行研究。方法:20例肝肾功能正常,呼吸道疾病患者,给予二个不同剂量的氨茶碱(0.3~0.6g·d-1)治疗,达稳态后,用高效液相色谱法分别测定二个谷浓度值,以Δ%浓度比Δ%剂量≥1.5为判定非线性代谢的标准。结果:有11例患者出现了非线性代谢,发生率55%。其药动学常数:Vm=707.7±175.4mg·d-1,Km=5.8±3.8μg·ml-1。结论:本实验结果对临床更安全的应用氨茶碱有新的提示。
Objective: To study the non-linear metabolism of theophylline in conventional dosage. Methods: Twenty patients with normal liver and kidney function were treated with two different doses of aminophylline (0.3-0.6 g · d -1). After reaching the steady state, they were determined by high performance liquid chromatography Two trough concentration values, Δ% concentration ratio Δ% dose ≥ 1.5 to determine the non-linear metabolic criteria. RESULTS: Eleven patients developed non-linear metabolism with a 55% incidence. Its pharmacokinetic constants: Vm = 707.7 ± 175.4 mg · d-1, Km = 5.8 ± 3.8 μg · ml-1. CONCLUSIONS: The results of this experiment have new implications for the more clinically safe use of aminophylline.