Alcohol Affect the Pharmacokinetics of Doxofylline and its Metabolite Theophylline in Rats

作者：Lin Yuxian; Pan Peipei; Xiong Jianhua^*; Chen Lianguo; Wang Qiong; Wang Shujun; Sun Lirong; Hu Guoxin

来源：Latin American Journal of Pharmacy, 2015, 34(6): 1065-1069.

• doxofylline
• ethanol
• pharmacokinetics
• rat
• theophylline
• UPLC

The aim of the study was to evaluate the pharmacokinetic effect of alcohol on doxofylline and its metabolite theophylline in rats by using UPLC. The rats were randomL y divided into three groups and orally treated with purified water, low-dose alcohol and high-dose alcohol for one week. 80.0 mg.kg(-1) Doxofylline was administrated on the eighth day and blood samples were obtained via tail vein at the time points of 0.1667, 0.5, 1, 1.5, 2, 3, 4, 6, 8 and 12 h. Long-term low-dose alcohol significantly decreased the C-max and AUC((0-t)) values of doxofylline by 34.83% and 14.02%. Long-term high-dose alcohol significantly decreased the Cmax, AUC((0-t)), and AUC((0-infinity)) values of doxofylline by 49.97%, 17.57% and 15.20%, and increased T-max, t(1/2z) and CLz/F by 193.00%, 74.96% and 20.00%. Though the effects of ethanol on the biotransformation of doxofylline were dose-related, long-time treatment of alcohol apparently lowered the bioavailability of doxofylline.

• 出版日期2015
• 单位温州医科大学