金银花提取物对茶碱在大鼠体内药代动力学的影响  

Effects of Jinyinhua(Honeysuckle)Extract on Pharmacokinetics of Theophylline in Rats

作　　者：谭文超[1] 张艳[1,2] 谭茗心[2] TAN Wenchao;ZHANG Yan;TAN Mingxin(Affiliated Hospital of Liaoning University of Traditional Chinese Medicine,Shenyang 110032,Liaoning,China;Liaoning University of Traditional Chinese Medicine,Shenyang 110847,Liaoning,China)

机构地区：[1]辽宁中医药大学附属医院,辽宁沈阳110032 [2]辽宁中医药大学,辽宁沈阳110847

出　　处：《中华中医药学刊》2023年第12期53-56,共4页Chinese Archives of Traditional Chinese Medicine

基　　金：国家自然科学基金项目(81774157)。

摘　　要：目的研究金银花提取物对茶碱在大鼠中的药代动力学行为的影响。方法将12只雄性SD大鼠随机分至对照组(6只)和实验组(6只)。对照组大鼠和实验组大鼠分别于第1~7天灌胃给予溶媒(纯净水溶液)或金银花提取物(20 g·kg^(-1)),在第7天灌胃给予溶媒或金银花提取物后灌胃给予茶碱溶液(10 mg·kg^(-1))。分别于茶碱给药前和给药后不同时间点采集血样,采用HPLC-MS/MS方法测定茶碱的血药浓度,使用DAS 2.0药代动力学软件计算药动学参数,并采用SPSS 17.0软件进行统计学分析。结果对照组大鼠的平均茶碱C_(max)、AUC_(0-t)和AUC_(0-∞)分别为11557.0 ng·mL^(-1)、96153.7 ng·mL^(-1)·h^(-1)和105524.7 ng·mL^(-1)·h^(-1);实验组大鼠的平均茶碱C_(max)、AUC_(0-t)和AUC_(0-∞)分别为8718.0 ng·mL^(-1)、67905.2 ng·mL^(-1)·h^(-1)和72811.8 ng·mL^(-1)·h^(-1)。与对照组相比,实验组大鼠的茶碱暴露显著降低,C_(max)、AUC_(0-t)和AUC_(0-∞)分别是对照组的0.77(90%CI:0.64,0.90)、0.73(90%CI:0.58,0.88)和0.71(90%CI:0.57,0.86)倍(P<0.05);实验组大鼠的茶碱清除率明显高于对照组(0.14 L·h^(-1)·kg^(-1)vs.0.10 L·h^(-1)·kg^(-1))。结论金银花提取物可影响茶碱在大鼠体内的药代动力学行为,降低其体内暴露水平。Objective To study the effect of Jinyinhua(honeysuckle)extract on the pharmacokinetics of theophylline in rats.Methods Twelve male SD rats were randomly divided into control group and test group(n=6).The rats were given vehicle(puri⁃fied water)in the control group and Jinyinhua(honeysuckle)extract(20 g·kg^(-1))the test group in by gavage from day 1 to day 7.On day 7,the rats were given theophylline solution(10 mg·kg^(-1))after vehicle or Jinyinhua(honeysuckle)extract adminstra⁃tion in the two groups respectively.The blood samples were collected at different time points before and after theophylline admin⁃stration.The plasma concentrations of theophylline were determined by an HPLC-MS/MS method.The pharmacokinetic param⁃eters were calculated by DAS 2.0 software and the statistical analysis was performed by using SPSS 17.0 software.Results The mean values of C_(max),AUC_(0-t)and AUC_(0-∞)of theophylline of the rats in control group were 11557.0 ng·mL^(-1),96153.7 ng·mL^(-1)·h^(-1)and 105524.7 ng·mL^(-1)·h^(-1),respectively;and the mean vales of C_(max),AUC_(0-t)and AUC_(0-∞)of theophylline of the rats in the test group were 8718.0 ng·mL^(-1),67905.2 ng·mL^(-1)·h^(-1)and 72811.8 ng·mL^(-1)·h^(-1),respectively.The ex⁃posure of theophylline was significantly decreased in the test group compared with that of the control group with the values of C_(max),AUC_(0-t)and AUC_(0-∞)being 0.77(90%CI:0.64,0.90),0.73(90%CI:0.58,0.88)and 0.71(90%CI:0.57,0.86)fold,respectively(P<0.05).The clearance rate of theophylline in the test group was increased significantly than that of the con⁃trol group(0.14 L·h^(-1)·kg^(-1)vs.0.10 L·h^(-1)·kg^(-1)).Conclusion Jinyinhua(honeysuckle)extract can affect the pharmaco⁃kinetic of theophylline in rats and decreased its exposure in vivo.

关 键 词：金银花提取物 茶碱 药代动力学 药物相互作用 LC-MS/MS 

分 类 号：R285.5[医药卫生—中药学]