摘要
目的建立HPLC-MS/MS法测定人血浆中氟桂利嗪的浓度,研究其在人体内的药物动力学行为,并评价其生物等效性。方法采用随机双周期交叉对照试验设计,20名男性健康志愿者分别单剂量口服含20 mg氟桂利嗪的受试制剂和参比制剂后,用HPLC-MS/MS法测定血浆中药物浓度,并利用DAS软件进行药动学参数计算和2种制剂的生物等效性评价。结果受试制剂和参比制剂的主要药物动力学参数:tmax分别为(2.43±0.75)和(2.40±0.77)h,Cmax分别为(56.9±18.5)和(54.8±18.9)μg.L-1,t1/2分别为(6.68±1.74)和(5.99±1.77)h,采用梯形法计算,AUC0-t分别为(382±134)和(405±151)μg.h.L-1,AUC0-∞分别为(417±149)和(436±167)μg.h.mL-1,以AUC0-t计算,氟桂利嗪的相对生物利用度平均为(96.9±16.9)%。结论建立的分析方法快速准确、专属性强,测得的数据可靠,2种制剂在体内生物等效。
Objective To establish an HPLC-MS/MS method for the determination of flunarizine in human plasma, and investigate the pharmacokinetics and bioequivalenee of flunarizine in healthy volunteers. Methods A single oral dose of 20 mg flunarizine of each kind of capsules was given to 20 male healthy volunteers respectively in an open, randomized crossover study. The concentration of flunarizine in the plasma was determined by HPLC-MS/MS. DAS program was used to calculate the pharmacokinetic parameters and evaluate the bioequivalence of the two formulations. Results The main pharmacokinetic parameters of the test and reference flunarizine capsules were as follows： tmax was （2.43±0.75） and （2.40±0.77） h, Camx was （56.9±18.5） and （54.8±18.9） μg·L^-1, tl/2 was （6.68±1.74） and （5.99±1.7？） h, AUC0-, was （382±134） and （405±151） μg·h·L^-1 , and AUC0 ~ was （417±149） and （436± 167）μg·h·mL^-1 , respectively. The relative bioavailability was （96.9±16.9）G. Conclusion The method is rapid, specific and accurate with reliable results. The test capsule is bioequivalent to the reference capsule.
出处
《中南药学》
CAS
2010年第4期276-280,共5页
Central South Pharmacy
