HPLC-荧光法测定α-细辛醚热熔压敏胶贴剂的相对生物利用度  

HPLC with fluorescence determination of relative bioavailability of hot melt pressure sensitive adhesive cα-asarone patch

作　　者：俞振伟[1] 梁文权[2] 

机构地区：[1]浙江大学医学院附属邵逸夫医院,杭州310016 [2]浙江大学药学院,杭州310058

出　　处：《药物分析杂志》2011年第8期1444-1447,共4页Chinese Journal of Pharmaceutical Analysis

摘　　要：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 an HPLC method for the determination of α-asarone in rabbit plasma and to study the relative bioavailability of hot melt pressure sensitive adhesive patch.Methods：The plasma samples were collected at the predetermined time points after oral or transdermal administration.The plasma concentrations of α-asarone were determined by HPLC method using ZORBAX Eclipse XDB-C18（250 mm×4.6 mm,5 μm） column,methanol-water（75∶ 25） as mobile phase,flow rate at 1.0 mL·min-1 after pretreatment.The excitation wavelength and emission wavelength were 265 nm and 365 nm,respectively.The pharmacokinetics and relative bioavailability were studied.Results：A good linearity was obtained in the range of 0.01-1 μg·mL-1（r=0.9998） with a detective limit of 0.005 μg·mL-1.The method recovery was between 96.2%-102.0%.The relative standard deviations of within-day and between-day were less than 4.52%.The AUC0→t of α-asarone after oral and transdermal administration were（0.53±0.23）μg·h·mL-1and（7.86±2.15）μg·h·mL-1,respectively;the relative bioavailability of patch was 1494%.Conclusion：The established method is simple,accurate and suitable for the determination of α-asarone in rabbit plasma.The hot melt pressure sensitive adhesive patch containing α-asarone had shown high relative bioavailability.

关 键 词：细辛醚 细辛脑 高效液相 荧光检测 热熔压敏胶 相对生物利用度 

分 类 号：R917[医药卫生—药物分析学]