摘要
目的大鼠灌胃给予射干合剂后，了解黄芩苷和黄芩素在其体内的药动学特征。方法大鼠予射干合剂10．0mL．kg-1，ig，收集给药后大鼠血清，采用液质联用技术测定血清中黄芩苷、黄芩素的含量，采用药动学软件计算求出药动学参数。收集给药后24h大鼠尿液、粪便，采用代谢笼技术，计算射干合剂中黄芩苷、黄芩素在大鼠尿、粪中24h内回收率。结果射干合剂中黄芩苷的药动学参数为tmax（1．85±0．21）h，t1／2（6．86±0．87）h，ρmax（227．96±21．65）μg·L-1,AUC0→∞（1198．30±383．56）μg·h·L-1，Vc／F（13．42±1．34）L；黄芩素的药动学参数为tmax（1．74±0．18）h，t1/2（24．30±2．39）h，ρmax（73．13±6．67）μg·L-1，AuC0→∞（550．92±38．66）μg·h·L-1，Ve／F（3．43±0．31）L。结论黄芩苷、黄芩素在大鼠体内24h基本排泄完全；服用射干合剂不会造成黄芩苷、黄芩素体内蓄积；黄芩苷和黄芩素经肾排泄只有原形药物的10％-20％，主要经粪便排泄；两者在体内会发生明显的相互转化。
AIM To determine the pharmacokinetic characteristics of baicalin and baicalein in rats after intragas- tric administration of Shegan Heji. METHODS Shegan Heji （1.0 mL/100 g） was administered to each rat by gavage. Blood samples were collected after drug administration. Plasma concentrations of baicalin and baicalein were determined by LC-MS/MS. The pharmacokinetic parameters of baicalin and baicalein were obtained using the pharmacokinetic soft- ware. Urine and fecal samples were collected 24 h after drug administration using metabolic cage to determine the recov- ery of baicalin and baicalein. RESULTS The pharmacokinetic parameters of baicalin was determined, tmax （ 1. 85 ± 0.21）h,t1/2（6.86±0.87）h,ρmax（227.96±21.65）μg·L-1,AUC0→∞（1 198.30±383.56）μg·h·L-1 and Vc/F （ 13.42 ±1.34） L. The pharmacokinetie parameters of baiealein was determined, t max （ 1.74 ± 0.18） h, t 1/2 （24.30± 2.39）h,ρmax（73.13 ± 6.67）μg·L-1 , AUC0→∞ （550.92 ± 38.66）μg·h· L-1 and Vc/F（3.43 ± 0.31）L. CONCLUSION Most of baicalin and baicalein is excreted completely in rats after 24 h, so Shegan Heji do not cause accumulation of baicalin and baiealein in rats. Baicalin and baicalein by renal excretion of unchanged drug is only 10% -20% ,mainly through fecal excretion; both will be significantly transformed in the body.
出处
《中国临床药学杂志》
CAS
2015年第1期34-38,共5页
Chinese Journal of Clinical Pharmacy
基金
上海市卫生局中医药科研基金(编号2012G003A)
上海市科委基金(编号11D21972500)
关键词
黄芩苷
黄芩素
射干合剂
排泄
药动学
baicalin
baicalein
Shegan Heji
excretion
pharmacokineties
