目的建立人血浆中阿比多尔的HPLC测定方法,测定志愿者口服盐酸阿比多尔颗粒剂后的血药浓度,并对受试制剂和参比制剂的生物等效性进行评价。方法血浆样品中加入内标SI-5后以0.1mol·L^-1的NaOH碱化,以环己烷提取,氮气吹干后用流动相溶解,进行HPLC分析,色谱柱为Alltech C₁₈(4·6mm×250mm,5μm);流动相为甲醇-1.32%三乙胺溶液(80∶20);流速为1.0mL·min^-1;检测波长为315nm,进样20μL。20名健康志愿者交叉口服受试制剂和参比制剂,剂量均为400mg,计算主要药动学参数及相对生物利用度以判断生物等效性。结果阿比多尔血浆样本线性范围为0.02～2.0mg·L^-1,检测限为0.01mg·L^-1;受试制剂和参比制剂的峰浓度分别为(0.879±0.175)和(0.741±0.167)mg·L^-1;达峰时间分别为(0.7±0.3)和(1.2±0.4)h;生物半衰期分别为(20.06±4.32)和(21.24±4.42)h,受试制剂的相对生物利用度为(100.4±10.5)%。结论本试验建立的分析方法简便、准确、灵敏、专属性强,统计学结果表明两种制剂生物等效。

OBJECTIVE To establish a HPLC method for bioavailability and pharmacokinetics of arbidol in human plasma.METHODS After adding SI-5,the internal standard,and 0.1 mol·L^-1 NaOH solution,the plasma samples were extracted with cyclohexane and determined by HPLC.The HPLC column was C₁₈ (4.6 mm×250 mm,5 μm),the mobile phase was CH₃ OH-1.32%TEA(80∶20),the flow rate was 1.0 mL·min^-1,the detection wavelength was 315 nm. A randomized crossover design was performed in 20 male volunteers after oral administration of arbidol test and reference preparations. RESULTS Calibration curves were linear over the range of 0.02～2.0 mg·L^-1,the limit of detection was 0.01 mg·L^-1.The main pharmacokinetic parameters of ρ_max,t_max and t_1/2 were (0.879±0.175)mg·L^-1,(0.7±0.3)h and (20.06±4.32)h for the test granules,and(0.741±0.167)mg·L^-1,(1.2±0.4)h and (21.24±4.42)h for the reference tablets, respectively. The relative bioavailability of the test granules was (100.4±10.5)%.CONCLUSION The method is simple,accurate and sensitive. The statistic analysis shows that the two preparations were bioequivalent.