【摘要】 目的 比较氨苄西林/丙磺舒颗粒剂与市售同成分胶囊剂在健康志愿音体内的药动学及相对生物利用度。方法 交叉口服单剂量氨苄西林/丙磺舒颗粒剂和氨苄西林/丙磺舒胶囊剂,采用反相高效液相色谱法分别测定人血清中氨苄西林和丙磺舒的浓度。利用3P97程序对各药动学参数进行方差分析和双单侧ι检验。结果 受试制剂及参比制剂中氨苄西林AUC0→8分别为(27.6±7.9)和(31.1±7 1)μg·h·mL-1:AUC0→∞分别为(29.4±8.1)和(33.2±7.3)1.μg·h·L-1;Cmax分别为(8.2±2.8)和(8.1±2.2)μg·mL-1;ιmax分别为(2.0±0.6)和(2.1±0.5)h;ι1/2分别为(1.62±0.48)和(1.57±0.43)h。受试制剂和参比制剂中丙磺舒的AUC0→24分别为(174.3±35.8)和(178.2±40.7)μg·h·mL-1;AUC0→∞分别为(180.5±37.9)和(186.6±43.1)μg·h·mL-1;Cmax分别为(21.8±4.5)和(24.3±5.O)μg·mL-1;ιmax分别为(2.4±0.8)和(2.3±0.6)h;ι1/2分别为(4.73±0.79)和(4.98±1.03)h。受试制剂中氨苄西林和丙磺舒的相对生物利用度分别为(89.0±17.6)％和(99.4±15.4)％。经交叉试验方差分析,上述药动学参数无统计学差早(P>0.05)。结论 受试制剂和参比制剂AUC,ιmax与Cmax经双单侧ι检验分析,结果表明两者具生物等效性更多还原

【Abstract】 OBJECTIVE To study the pharmaeokineties and relative bioavailability oi ampicillin and probenecid oral suspension in Chinese healthy volunteers. METHODS According to crossover design, each volunteer was given a single oral dose of test preparation and reference preparation. The serum concentrations of ampicillin and probenecid were determined by high performance liquid chromatograpby. Phanna-cokinetic paramters were calculated. The analysis oi variance and two one-side t test were used to evaluate the variance between 2 groups. RESULTS The AUC0→8, AUC0→∞ , Cmax, tmax and t1/2 of ampieillin in lest oral suspension arid the reference capsules were (27.6 ± 7.9) and (31.1±7.1),μg·h·mL-1, (29.4±8.1) and (33.2±7.3) μg·h·mL-1 , (8.2±2.8) and (8.1 ?.2)μg·mL-1 , (2.0 ± 0.6) and (2.1± 0.5)h, (1.62 ± 0.48) and (1.57 ± 0.43)h, respectively. The AUC0→24 , AUC0→∞, Cmax, tmax and t1/2 of probenecid in test oral suspension and the reference capsules were (174.3 ± 35.8) and (178.2 ± 40.7)μ·h·mL-1, (180.5 ± 37.9) and (186.6 ± 43.1)μg·h·mL-1 , (21.8±4.5) and (24.3±5.0)μg·ML-1, (2.4±0.8) and (2.3 ±0.6)h, (4.73±0.79) and(4.98±1.03)h, respectively. There were no significant differences in the pharmacokinetic parameters between test preparation and reference preparation. Compared with reference preparation, the relative bioavailability of ampieillin and probenecid of test preparation were (89.0±17.6)% and (99.4±15.4)% respectively. CONCLUSION The result of statistical analysis shows that the 2 preparations are bioequivalent.更多还原