β-细辛醚及石菖蒲挥发油中β-细辛醚在家兔体内的药代动力学  

Pharmacokinetics of β-asarone and β-asarone in volatile oil from Acorus Tatarinowii Schott in rabbits

作　　者：魏立平[1] 吴玫涵[1] 

机构地区：[1]总后卫生部药品仪器检验所,北京100071

出　　处：《第四军医大学学报》2005年第15期1431-1434,共4页Journal of the Fourth Military Medical University

摘　　要：目的:研究β细辛醚及石菖蒲挥发油中β细辛醚的药物代谢动力学.方法:采用气相色谱法测定β细辛醚的血药浓度,色谱柱:HP35毛细管气相色谱柱;程序升温:起始温度为30℃,6℃/min升至220℃,保持5min;进样口温度250℃;检测器温度320℃;进样量2.0μL;无分流进样;溶剂:甲醇;载气:氦气;柱头压:5.5×104Pa;内标物:α萘酚.结果:建立了用气相色谱法测定β细辛醚血药浓度的方法,线性方程:Y=0.01889ρ+1.755×10-3(n=6,r=0.9999),线性范围:0.04～40.00mg/L.兔全血中最低检测浓度为:0.04mg/L.β细辛醚灌胃ig后,在兔体内符合一级吸收二室模型,T1/2(α)为7.5min,T1/2(β)为69.6min.家兔灌胃石菖蒲挥发油后,β细辛醚在体内的药时过程为线性动力学过程,同样符合一级吸收二室模型,T1/2(α)为18.3min,T1/2(β)为114.5min.结论:本实验的研究结果为中药石菖蒲的合理用药以及进一步开发石菖蒲新制剂提供了参考依据,同时,也为中药材中挥发油类有效成分的药代动力学研究提供了可供借鉴的方法.AIM： To study the pharmacokinetics of β-asarone and β-asarone in volatile oil from Acorus Tatarinowii Schott in rabbits. METHODS： Gas chromatography （GC）was applied to determine the concentration of β-asarone in blood. The GC system used a capillary HP-35 column and helium as carrier gas, the oven temperature starting at 30℃, then raised to 220℃; by 6℃/min and kept for 5 minutes, the injector temperature of 250℃ and the detector temperature of 320℃. The injection volume was 2.0μL with splitless injection mode. Methanol was used as solvent and α-naphthol as interior standard substance. RESULTS： Acapillary GC method was established for the determination of β-asarone in rabbit blood. The linear equation [ Y =0.01889f ＋1.755×10^-3（ n=6, r=0.9999）] was obtained in the range of 0.04 - 40.00 mg/L （ Y： ratio of the peak area of 15-asarone and of α-naphthol, f： concentration of β-asarone in blood）. The limit of quantification （0.04 mg/L）and 95.3% recovery of β-asarone in blood （ RSD =3.92% ）were achieved respectively. After oral administration of β-asarone standard, the inner body process of β-asarone accorded with 2-compartment model with 1 st order absorption.7.5 min and 69.6 min were obtained as T1/2α） and T1/22β） respectively. After oral administration of volatile oil from Acorus Tatarinowii Schott, the inner body process of β-asarone also accorded with 2-compartment model with 1st order absorption. 18. 3 min and 114. 5 rain were obtained as T1/2（α） and T1/2（β） respectively. CONCLUSION： The result of our study provides some evidence for the rational administration and the further development of Acorus Tatarinowii Schott and some method for pharmacokinetics study of volatile oils from traditional Chinese medicinal materials.

关 键 词：Β-细辛醚 石菖蒲 药物代谢动力学 气相色谱法 

分 类 号：R969.1[医药卫生—药理学] R285.1[医药卫生—药学]