目的 建立Beagle犬血浆中2,3,5,4'-四羟基二苯乙烯-2-O-β-D-葡萄糖苷(SBGC)的RP-HPLC含量测定方法,研究Bea-对e犬灌胃何首乌二苯乙烯苷有效部位后体内药动学。方法色谱条件:Agilent Zorbax Extend-C18色谱柱(4.6mm×250min,5μm);流动相:乙腈-水(15:85);检测波长:320nm;柱温:30℃;流速:1.0mL·min^-1。Beagle犬灌胃何首乌二苯乙烯苷有效部位后定时取血,测定血浆药物浓度,采用DAS软件计算药动学参数。结果 SBGC在0.206d~8.256mg·L^-1内线性关系良好(r=0.999d);Beagle犬灌胃何首乌二苯乙烯苷有效部位1.0,1.5,2.0g·kg^-1后符合二室开放式模型,t1/2a分别为0.20,0.10和0.14h;t1/2β分别为0.56,0.60和0.64h;V/F分别为0.08,0.15和0.08L·kg^-1;CL/F分别为0.11,0.20和0.16L·h^-1。结论 该法快速、简便、准确,可满足药动学研究需要。
OBJECTIVE To establish a RP-HPLC method for the determination of 2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glucoside in Beagle dog plasma and to investigate the pharmacokinetics of the effective fraction of stilbene glycoside of Polygonum multiflorum after intragastric administration. METHODS The analysis was performed on a Agilent Zorbax Extend C18 column (4. 6 mm×250 mm,5 μm ) at 30 ℃ with the mobile phase of acetonitrile-water ( 15 : 85) at a flow rate of 1.0 mL·min^-1. The detective wavelength was 320 nm. The plasma samples were collected after intragastric administration of the effective fraction of stilbene glycoside of Polygonum multiflorum in Beagle dogs. The concentrations of 2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glucoside in plasma were measured by RP-HPLC method and the pharmacokinetic parameters were calculated by DAS. RESULTS The calibration curve of 2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glucoside was linear in the range of 0. 206 4~8. 256 mg·L^-1 with the correlation coefficient of 0. 999 4. The concentration-time curves of 2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glucoside in plasma were fitted with a two-compartment open pharmacokinetic model after intragastric administration of the effective fraction of stilbene glycoside of Polygonum multiflorum in Beagle dogs. The main phar-macokinetic parameters of 2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glucoside after a single dose of 1.0, 1.5, 2.0 mg·kg^-1 of the effective fraction stilbene glycoside of Polygonum multiflorum in Beagle dogs plasma were:t1/2a 0. 20, 0. 10 and 0. 14 h;t1/2β 0. 56, 0. 60 and 0. 64 h;V/F 0. 08, 0. 15 and 0. 08 L·kg^-1; CL/F 0. 11,0. 20 and 0. 16 L·h^-1. CONCLUSION The method is sensitive, stable and easy to process. It is practical and suitable for the pharmacokinetic study of 2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glucoslde.