【摘要】 目的研究格列齐特的人体相对生物利用度和生物等效性。方法健康志愿者20例,随机双交叉单剂量口服格列齐特片的试验和参比制剂,剂量均为80 mg,剂间间隔为2周。分别于服药后60 h内多点抽取静脉血;用高效液相色谱法测定血浆中格列齐特的浓度。用DAS药动学程序计算相对生物利用度并评价两种制剂生物等效性。AUC(0-60),AUC(0-inf)和Cm ax经方差分析和双单侧t检验,tm ax进行秩和检验。结果单剂量口服试验和参比制剂后血浆中的格列齐特的Cm ax分别为(5.34±0.66)和(5.12±0.39)mg.L-1;tm ax分别为(4.30±0.92)和(4.15±0.67)h;AUC(0-60)分别为(92.67±12.12)和(89.82±13.33)mg.h.L-1;AUC(0-inf)分别为(96.36±12.87)和(93.37±13.83)mg.h.L-1。Cm ax、AUC(0-60)和AUC(0-inf)的90%可信区间分别为100.52%~107.56%,99.16%~107.97%和99.16%~107.97%。结论格列齐特试验制剂与参比制剂的人体相对生物利用度均为(104.5±15.5)%,两者具有生物学等效性。更多还原

【Abstract】 Objective To study the relative bioavailability and bioequivalence of gliclazide tablets in healthy volunteers. Methods A single oral dose（80 mg of tested and reference formulation） was given to 20 healthy volunteers in a randomized crossover study.The concentrations of gliclazide in plasma were determined by HPLC.The pharmacokinetics parameters were calculated and the bioavailability and bioequivalence of two formulations were evaluated by DAS program. Results After a single dose,the pharmacokinetics parameters for gliclazide were as follows: C_max were（5.34±0.66） mg·L^-1and（5.12±0.39） mg·L^-1;t_max were（4.30±0.92） h and（4.15±0.67） h;AUC_（0-60）were（92.67±12.12） mg·h·L^-1 and（89.82±13.33） mg·h·L^-1;AUC_（0-inf） were（96.36±12.87） mg·h·L^-1 and（93.37±13.83） mg·h·L^-1 for T and R,respectively.The 90% confidential interval of C_max,AUC_（0-60） and AUC_（0-inf） of tested formulation were 100.52%～107.56%,99.16%～107.97% and 99.16%～107.97% respectively. Conclusion The relative bioavailability is（104.5±15.5）%.The results of the statistic analysis show that the two formulations exhibit bioequivalence.更多还原