国产盐酸乙哌立松片剂人体生物等效性研究

Bioequivalence of eperisone hydrochloride tablets in healthy volunteers

目的 :了解国产盐酸乙哌立松片剂的相对生物利用度 ,评价其生物等效性。方法 :1 2名健康受试者单剂量口服被试制剂或参比制剂 1 5 0mg后 ,采用高效液相 质谱联用 (HPLC MS)测定血浆中盐酸乙哌立松的浓度。 结果 :经 3P97拟合 ,两者的体内过程皆符合血管外口服给药一室模型 ,采用梯形法计算的两者AUC0～t均值分别为 (1 2 .6 1± 7.79) ,(1 3.1 7± 7.44 ) μg·h·L-1,实测cmax均值分别为 (7.2 2± 4.6 3) ,(7.2 3± 4.0 3) μg·L-1,实测tpeak均值分别为 (0 .92± 0 .1 2 ) ,(0 .94± 0 .1 1 )h。经统计学分析 ,被试制剂和标准参比制剂具有生物等效性。被试制剂的相对生物利用度为 (94.1± 1 2 .3) %。结论 :国产盐酸乙哌立松片剂和进口片剂具有生物等效性。

OBJECTIVE:To study the relative bioavailability and bioequivalence between eperisone tablets (test drug) and its standard tablets (reference drug)in 12 healthy male volunteers.METHODS:A dose of 150 mg of domestic or imported eperisone (test and reference preparation) was give in a randomized 2 way cross over design.Blood samples were withdrawn up to 10 hours after administration.The plasma concentration of eperisone was determined by a high performance liquid chromatography mass spectrometry (HPLC MS) method.RESULTS:The concentration time curves of two preparations fitted to a one compartment model.The peak plasma levels ( c max ) of eperisone test drug and reference drug were (7.22±4.63) μg·L -1 and (7.23±4.03) μg·L -1 ,respectively.The times approached to peak concentration ( t peak ) were (0.92±0.12) and (0.94±0.11) h,respectively;and AUC 0～t were ( 12.61 ±7.79) and (13.17±7.44) μg·h·L -1 ,respectively.CONCLUSION:The relative bioavailability of the test durg was (94.1± 12.3 )% of the imported eperisone tablets.They were bioequivalent.