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[摘要]
目的建立小鼠脑组织中天麻苷元的HPLC测定方法,并考察灌胃天麻素后小鼠脑中天麻苷元的药动学特性。方法脑匀浆用醋酸乙酯提取后,采用HPLC法测定。色谱柱为Diamonsil C18(250 mm×4.6 mm,5μm),流动相为乙腈-水(10.5∶89.5),体积流量1.0 mL/min;
检测波长221 nm;
柱温25℃;
进样量20μL。结果方法线性范围为50~1 616 ng/mL(r=0.999 6),回收率为93.8%~95.1%,日内及日间RSD均低于10%。小鼠脑组织中天麻苷元的质量浓度与时间曲线呈现双峰(tmax1=15 min,tmax2=90 min),药时曲线下面积为52 822.5ng.min/g,消除半衰期为54.8 min。结论该分析方法灵敏、准确,适合于脑组织中天麻苷元的测定。天麻素经小鼠口服给药后,能较快入脑并代谢为天麻苷元,消除也较快。
[Key word]
[Abstract]
Objective To establish an HPLC method for determination of gastrodigenin concentration in brain tissue of mice and investigate its pharmacokinetics after intragastric administration of gastrodin.Methods The brain homogenate was extracted with acetoacetate and analyzed by HPLC method.The separation was performed on a Diamonsil C18 column(250 mm × 4.6 mm,5 μm) under the following chromatographic conditions: mobile phase,acetonitrile-water(10.5∶89.5);column temperature,25 ℃;flow rate,1.0 mL/min;detection wavelength,221 nm;and sampling amount,20 μL.Results The calibration curve showed good linearity within the concentration range of 50-1 616 ng/mL(r= 0.999 6).The relative recoveries were 93.8%-95.1%,and the RSDs of the intra-and inter-day precision were less than 10%.The concentration-time profile of gastrodigenin in brain tissue of mice showed double peaks(tmax1=15 min,tmax2=90 min).The AUC was 52 822.5 ng·min/g,and t1/2(ke) was 54.8 min.Conclusion The analytical method established for assay of gastrodigenin in brain tissue of mice is sensitive and accurate.The result indicates that gastrodin could rapidly distribute to the brain,be metabolized into gastrodigenin,and be eliminated after oral administration.
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