超微粉碎对川芎中阿魏酸在家兔体内药动学性质的影响

Effect of Superfine Comminution on Pharmacokinetics of Ferulic Acid in Rhizoma Chuanxiong in Rabbits

目的研究超微粉碎对川芎中阿魏酸在家兔体内的药动学性质的影响。方法家兔灌胃给药10 g(生药).kg-1,耳中动脉取血,采用高效液相色谱法测定兔血清中阿魏酸含量,色谱条件为:色谱柱Thermo Hypersil GOLD-C18柱(4.6 mm×250mm,5μm),流动相甲醇-水(含0.5%冰醋酸)(20∶80),流速0.8 mL.min-1,检测波长322 nm,柱温30℃。用3P97计算川芎超微粉和普通粉中阿魏酸在家兔体内的药动学参数。结果建立了HPLC测定家兔血清中阿魏酸含量的方法。口服普通粉和超微粉混悬液后阿魏酸在家兔体内符合一室模型,权重为1/C2。普通粉组和超微粉组的主要药动学参数为ke(0.004 97±0.000 60)和(0.005 89±0.000 78)min-1;ka=(0.065 4±0.012 5)和(0.134±0.033)min-1;t1/2(ka)=(10.590±3.323)和(5.162±1.200)min;t1/2ke=(139.52±17.01)和(117.78±15.13)min;tpeak=(42.640±6.882)和(24.359±3.72)min;ρmax=(345.97±50.79)和(387.58±42.58)ng.mL-1;AUC0-t(n)=(80 539±12 826)和(77 295±10 342)ng.min.mL-1;AUC0～Infinite=(93 360±15 832)和(91 058±18 673)ng.min.mL-1。结论川芎超微粉中阿魏酸在家兔体内的吸收和消除的速度都比普通粉快,AUC无显著差异。

OBJECTIVE To study the effect of superfine comminution on pharmacokinetics of ferulic acid（FA） in Rhizoma Chuanxiong in rabbits.METHODS The rabbits were given orally Rhizoma 10 g·kg^-1 and blood samples were drawn from the rabbits＇ ear arteries.FA in the serum of rabbits was determined by HPLC.The separation was performed on a Thermo Hypersil GOLD-C18 column（4.6 mm×250 mm,5 μm） at the temperature of 30 ℃.The mobile phase consisted of methanol-water（containing 0.5% acetic acid）（20∶80） at the flow rate of 0.8 mL·min^-1.The detective wavelength was 322 nm.The pharmacokinetic parameters were analyzed by 3P97.RESULTS A HPLC method for the determination of FA in the rabbit serum was established.The plasma concentration-time profiles were described by one compartment model with first order absorption.The weight was 1/C2.The main pharmacokinetic parameters of common power group and superfine powder group were as follows： ke（0.004 97±0.000 60） and（0.005 89±0.000 78） min-1;ka（0.065 4±0.012 5） and（0.134±0.033） min-1;t1/2（ka）（10.590±3.323） and（5.162±1.200） min;t1/2ke（139.52±17.01） and（117.78±15.13） min;tpeak（42.640±6.882） and（24.359±3.72） min;ρmax（345.97±50.79） and（387.58±42.58） ng·mL-1;AUC0-t（n）（80 539±12 826） and（77 295±10 342）ng·min·mL^-1;AUC0~Infinite（93 360±15 832） and（91 058±18 673） ng·min·mL^-1.CONCLUSION The absorption rate and elimination rate of FA in rabbits treated with superfine powder suspension of Chuanxiong was greatly increased,but there was no significant change in AUC.