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目的:建立家兔血浆内α-细辛醚的HPLC-荧光测定法,研究α-细辛醚热熔压敏胶贴剂在家兔体内的相对生物利用度。方法:家兔给予α-细辛醚混悬液或α-细辛醚贴剂后于不同时间点采血,血浆样品处理后以甲醇-水(75∶25)为流动相,使用ZORBAX Eclipse XDB-C18色谱柱(250 mm×4.6 mm,5μm)进行分离,流速1.0 mL·min-1,荧光检测器激发波长为265 nm,检测波长为365 nm,测定血浆药物浓度,计算药物动力学参数和相对生物利用度。结果:α-细辛醚在浓度0.01～1μg.mL-1(r=0.9998)范围内线性关系良好,检测限为0.005μg·mL-1,方法学回收率为96.2%～102.0%,日内与日间RSD均<4.5%。家兔口服α-细辛醚混悬液后的AUC0→t为(0.53±0.23)μg.h·mL-1,贴剂给药的AUC0→t为(7.86±2.15)μg.h·mL-1,贴剂的相对生物利用度为1494%。结论:该法简便准确,可用于家兔血浆内α-细辛醚浓度的测定;α-细辛醚热熔压敏胶贴剂的相对生物利用度高。
Objective: To establish a HPLC-fluorescence method for the determination of α-asarone in rabbits plasma and to study the relative bioavailability of α-asarone hot-melt adhesive paste in rabbits. Methods: Rabbits were given α-asarone suspension or α-asarone patch at different time points after the blood sample, the plasma sample treated with methanol - water (75:25) as the mobile phase, using ZORBAX Eclipse XDB- C18 column (250 mm × 4.6 mm, 5 μm) at a flow rate of 1.0 mL · min-1. The excitation wavelength of the fluorescence detector was 265 nm and the detection wavelength was 365 nm. The plasma drug concentration was measured to calculate the pharmacokinetic parameters and relative bioavailability. Results: The linear relationship of α-asarone in the range of 0.01 ~ 1μg.mL-1 (r = 0.9998) was good with the detection limit of 0.005μg · mL-1 and the methodological recovery of 96.2% -102.0% Daytime RSDs were <4.5%. The AUC0 → t after oral administration of α-asarone in rabbits was (0.53 ± 0.23) μg.h · mL-1, and the AUC0 → t was (7.86 ± 2.15) μg.h · mL- 1, the relative bioavailability of the patch is 1494%. Conclusion: The method is simple and accurate and can be used to determine the concentration of α-asarone in rabbits plasma. The relative bioavailability of α-asarone hot melt pressure-sensitive adhesive patch is high.