荜茇中胡椒碱在大鼠体内的药动学研究  

Pharmacokinetics of piperine from Piper longum in rats

作　　者：钟锋[1] 顾健[1] 李婧[1] 张亮亮[1] 廖敬礼[1] 姚峰[1] 

机构地区：[1]西南民族大学少数民族药物研究所,成都610041

出　　处：《中药药理与临床》2010年第2期34-36,共3页Pharmacology and Clinics of Chinese Materia Medica

基　　金：国家民委资助项目(No.07XN02)

摘　　要：目的:建立大鼠灌胃荜茇提取溶液后血浆中胡椒碱的HPLC测定方法,进行大鼠药动学研究。方法:大鼠灌胃给药(荜茇提取溶液)后,通过尾静脉取血获得血浆样品,以胡椒碱为指标,采取甲醇-水(77:23,v:v)为流动相,HypersilC18柱(250mm×4.6mm,10μm)为固定相,紫外检测波长为343nm进行测定。采用药代动力学软件DAS(ver2.0)处理,得到胡椒碱的药代动力学参数。结果:胡椒碱1.75～8.72g/ml范围内呈良好的线性关系,胡椒碱的三种浓度的平均回收率及相对标准偏差分别为88.4%(3.5%)、90.4%(2.8%)、85.9%(5.2%)。胡椒碱在大鼠体内的药代动力学过程符合一室吸收模型,主要药动学参数为tmax1/2=60min,高低剂量分别t1/2=138.78min和t1/2=125.87min,Cmax=0.46和0.27mg/L,AUC(0-t)=42.45和66.47mg/L.min,AUMC(0-t)=5355.17和7811.02。结论:荜茇在大鼠血浆中胡椒碱浓度的测定和临床前药代动力学研究。Objective：To study on the pharmacokinetics of piperine in rat by developing a high performance liquid chromatography （HPLC） method to determine the piperine in rat plasma after gastric administration with 80% methanol extract of Piper longum. Methods：After gastric administration of Piper longum extract,the plasma sample was collected from the tail vein of rat. The content of piperine in plasma was determined by HPLC using a Hypersil C18 column （250 mm×4.6 mm,10 μm） with the mobile phase of methanol-water （77：23,v/v）,while the compound was detected at the wavelength of 343 nm. Furthermore,the pharmacokinetic parameters of piperine was calculated by DAS （ver2.0）. Results：The results showed good linearity within the tested range of 1.75~8.72 μg/ml. The average recoveries and relative standard deviations （RSD） for three levels of piperine were 88.4%（3.5%）,90.4%（2.8%）,85.9%（5.2%）,respectively. The pharmacokinetic process of piperine was fitted with the one-compartment absorptive model with the parameters （tmax1/2=60 min,high and low dose）：AUMC（0-t） =5355.17 and 7811.02,AUC（0-t）=42.453 mg/L·min and 66.474 mg/L·min,Cmax are 0.266 mg/L and 0.459mg/L,t1/2=138.78 min and 125.87 min,respectively. Conclusion：The developed method is sensitive,accurate,reproducible and can be used in the preclinical pharmacokinetic study of piperine.

关 键 词：荜茇 胡椒碱 高效液相色谱法 萃取 

分 类 号：R285.5[医药卫生—中药学]