布洛芬片人体药代动力学及生物等效性研究

Pharmacokinetics and Bioequivalance of Ibuprofen Tablet in Healthy Volunteers

目的研究布洛芬片在健康人体内的药物代谢动力学及生物等效性。方法18名健康男性受试者单剂量、交叉口服400mg布洛芬供试制剂或参比制剂后,采用高效液相色谱?紫外检测法测定人体血浆中不同时间点布洛芬的浓度,计算其药代动力学参数和相对生物利用度,评价两制剂的生物等效性。结果布洛芬供试制剂和参比制剂主要药代动力学参数AUC0-10分别为(125.40±20.74)、(130.38±24.79)μg/(h.mL),Cmax分别为(34.60±7.12)、(37.88±7.13)μg/mL,Tmax分别为(2.0±0.5)、(1.7±0.5)h,t1/2分别为(2.1±0.21)、(2.19±0.29)h。受试制剂相对于参比制剂的生物利用度为(98.2±18.7)%。结论两制剂具有生物等效性。

Objective To investigate pharmacokinetic of Ihuprofen and to evaluate the hioequivalance. Methods Eighteen healthy male volunteers were enrolled into the single crossover study. After a single dose of the suspension equivalent to 400 mg Ihuprofen or a reference preparation were given by crossover. To develop a sensitive and specific HPLC-UV method for the determination of Ihuprofen in human plasma. The hioequivalence of the suspension and reference were evaluated by pharmacokinetic parameters and relative hioavailahility obtained. Results The main pharmacokinetic parameters of test and reference Ihuprofen were as the followings：AUC0-10 was（125.40±20. 74）μg/（mL · h）and （130. 38±24. 79）μg/（mL·h）;Cmax was（34. 60± 7.12）μg/mL and（37.88±7.13）μg/mL;Tmax was（2.0±0.5）h and （1.7±0.5）h;t1/2 was （2.1± 0.21）h and （2. 19 ±0. 29）h. The relative bioavailahility of test to reference preparation was （98.2± 18.7） %. Conclusion The two preparations are hioequivalent .