多剂量口服萘普生缓释片及普通片的人体药代动力学研究

STUDIES ON PHARMACOKINETICS OF SUSTAINED-RELEASE AND CONVENTIONAL TABLETS OF NAPROXEN AFTER MULTIPLE DOSE IN HEALTHY HUMAN VOLUNTEERS

目的 :研究萘普生缓释片和普通片多剂量口服的体内药代动力学。方法 :根据生物利用度试验方法 ,比较了健康志愿受试者多剂量口服萘普生缓释片和普通片的体内药动学过程。结果 :多剂量口服萘普生缓释片 ( 2×2 5 0mg ,qd)和普通片 ( 2 5 0mg,bid)达稳态后的AUC0→ 2 4分别为 ( 115 3 5 7± 15 4 95 )和 ( 10 3 8 4 0± 2 0 1 19) ( μg·h) /ml,Cmax分别为 ( 70 72± 13 2 2 )和 ( 73 0 5± 13 82 ) μg/ml,Tmax分别为 ( 7 6± 2 7)和 ( 2 0± 0 9)h ,波动系数 (FI)分别为0 85± 0 16和 1 0 1± 0 18。结论 :缓释片与普通片的药动学参数AUC0→ 2 4,Cmax和FI均无显著性差异 (P >0 0 5 ) ,两制剂生物等效。

OBJECTIVE:The pharmacokinetics of a new sustained release tablets of naproxen (NP SRT) was investigated together with conventional tablets (NP CT) after multiple dosing oral administration METHODS:After multiple dosing oral administration, the pharmacokinetics in vivo of NP SRT (2×250 mg,qd) were compared with NP CT(250 mg,bid) in healthy volunteers on the basis of the testing method of bioavailability. RESULTS:After multiple dosing administration of NP SRT(2×250 mg, qd) and NP CT (250 mg,bid),the mean AUC 0→24 estimated at steady state were (1153 57±154 95) and (1038 40±201 19)(μg·h)/ml,respectively The mean C max values were (70 72±13 22) and (73 05±13 82) μg/ml The mean T max for the NP SRT (7 6±2 7)h was greater than that for the NP CT(2 0±0 9 )h The fluctuation index (FI) were 0 85±0 16 and 1 01±0 18 ,respectively CONCLUSION:There were no significant differences in pharmacokinetic parameters including AUC 0→24 , C max and FI between the NP SRT and NP CT ( P >0 05) It was found that the two formulations were bioequivalent