8名中国患者中茶碱代谢物的药代动力学
Pharmacokinetics of theophylline metabolites in 8 Chinese patients.
作者信息
Cao W, Zhuo H T, Chen G, Ling S S
机构信息
Department of Clinical Pharmacology, Jinling Hospital, Nanjing, China.
出版信息
Zhongguo Yao Li Xue Bao. 1998 Sep;19(5):437-9.
AIM
To study theophylline metabolites pharmacokinetics in patients after a therapeutic dose.
METHODS
Eight adult patients with mild bronchial asthma and normal liver function were infused aminophylline intravenously (6.6 mumol.kg-1). The plasma concentrations of theophylline and its 4 metabolites: 1,3-dimethyluric acid (DMUA), 3-methylxanthine (3-MX), 1-methyluric acid (MUA), and the intermediate 1-methylxanthine (1-MX) were monitored by HPLC throughout 24 h.
RESULTS
The plasma concentration of DMUA was the highest one among the 4 metabolites. 3-MX showed the slowest elimination rate. The plasma concentration of 1-MX throughout a 24-h period showed that there was a picking up of 1-MX (from 0.04 mumol.L-1 to 1.05 mumol.L-1) in the next morning.
CONCLUSION
The formation of DMUA was the main metabolites. During night there was an accumulation of 1-MX.
目的
研究治疗剂量后患者体内茶碱代谢物的药代动力学。
方法
8例轻度支气管哮喘且肝功能正常的成年患者静脉输注氨茶碱（6.6 μmol·kg⁻¹）。通过高效液相色谱法在24小时内监测茶碱及其4种代谢物的血浆浓度：1,3-二甲基尿酸（DMUA）、3-甲基黄嘌呤（3-MX）、1-甲基尿酸（MUA）和中间产物1-甲基黄嘌呤（1-MX）。
结果
DMUA的血浆浓度是4种代谢物中最高的。3-MX的消除速率最慢。1-MX在24小时内的血浆浓度显示，第二天早晨1-MX有所升高（从0.04 μmol·L⁻¹升至1.05 μmol·L⁻¹）。
结论
DMUA的形成是主要代谢产物。夜间1-MX会蓄积。
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