摘要
目的:研究葛根提取物经不同途径给药后葛根素在大鼠体内的药代动力学。方法:葛根提取物经大鼠尾静脉注射(i.v.)、鼻腔给药(i.n.)(20mg/kg)及灌胃给药(i.g.)(200mg/kg),以甲醇沉淀血浆蛋白质,反相高效高相液相色谱测定葛根素在大鼠血浆中的浓度,用Kinetica程序软件计算药代动力学参数。结果:葛根素在(0.05315-53.1500)mg/L线性关系良好(r=0.9999),回收率为95.72%,RSD=2.31%;计算出尾静脉注射给药途径主要药动学参数:AUC=(795.41±59.85)mg.L-1.min-1,Cmax=(65.74±7.71)μg/mL,MRT=(18.96±2.08)min,t1/2=(16.95±3.55)min;鼻腔给药途径主要药动学参数:AUC=(227.34±19.42)mg.L-1.min-1,Cmax=(3.78±1.80)μg/mL,Tmax=(7.50±2.74)min,MRT=(117.09±38.37)min,t1/2=(22.50±10.60)min;灌胃给药途径主要药动学参数:AUC=(732.48±471.57)mg.L-1.min-1,Cmax=(3.53±1.32)μg/mL,Tmax=(27.00±16.43)min,MRT=(394.22±209.24)min,t1/2=(237.84±112.39)min;结论:葛根提取物经3种途径给药的主要药动学参数具有显著性差异,鼻腔给药吸收迅速,生物利用度较口服高,该结果可以为葛根提取物的给药途径和剂型研究提供科学依据。
Objective: To study pharmacokinetics of Puerarin in Rats Following Different Methods of Administration of Puerarin Extract.Methods: Rats received 20 mg/kg puerarin extract by caudal vein injection,20 mg/kg puerarin extract by nasal administration and 200 mg/kg puerarin extract by oral administration.Plasma samples were extracted with methanol and the plasma concentration of puerarin was analyzed by RP-HPLC.The pharmacokinetic parameters and bioavailability were calculated with Kinetica software.Results: Within range of(0.05315-53.1500) mg/L,puerarin presented a fine linear relationship(r=0.9999).The average recovery of puerarin was 95.72% with RSD 2.3%.The main pharmacokinetic parameters were as follows: caudal vein injection: AUC=(795.41±59.85)mg·L-1·min-1,Cmax=(65.74±7.71)μg/mL,MRT=(18.96±2.08)min,t1/2=(16.95±3.55)min,nasal administration: AUC=(227.34±19.42)mg·L-1·min-1,Cmax=(3.78±1.80)μg/mL,Tmax=(7.50±2.74)min,MRT=(117.09±38.37)min,t1/2=(22.50±10.60)min;oraladministration: AUC=(732.48±471.57)mg·L-1·min-1,Cmax=(3.53±1.32)μg/mL,Tmax=(27.00±16.43)min,MRT=(394.22±209.24)min,t1/2=(237.84±112.39)min.Conclusion: There were significant differences among the main pharmacokinetic parameters of puerarin following different methods of administration of puerarin extract,nasal administration could lead to a quick absorption and its bioavailability was higher than oral administration,this result can provide some scientific basises for the method of administration and the reform of dosage form of puerarin extract.
出处
《中华中医药杂志》
CAS
CSCD
北大核心
2011年第10期2408-2411,共4页
China Journal of Traditional Chinese Medicine and Pharmacy
基金
"重大新药创制"科技重大专项(No.2009ZX09502-008)
教育部博士点基金(No.20090013110007)
国家自然科学基金面上项目(No.81073057)
中药生产技术及过程控制技术标准平台(No.2009ZX09308-003)~~
关键词
葛根提取物
不同途径给药
生物利用度
药代动力学
Puerariae extract
Different methods of administration
Bioavailability
Pharmacokinetics