医药学论文：阿莫西林舒巴坦匹呋酯匹呋酯片剂生物等效性测定

【摘要】 目的 研究国产阿莫西林/舒巴坦匹呋酯（1：1）片剂在22名男性健康志愿者中的生物等效性。方法 22名健康志愿者分别双交叉空腹口服国产阿莫西林1000mg/舒巴坦匹呋酯1000mg片剂（国产品）和对照品进口阿莫西林1000mg/舒巴坦匹呋酯1000mg片剂（进口品）各一次。用高效液相色谱法测定血浆中的浓度。采用双向单侧t检验进行生物等效性评价。结果 22名受试者单剂空腹口服国产品和进口品后的体内过程均符合血管外一室模型。口服国产品和进口品后，阿莫西林实测平均高峰血药浓度(Cmax)分别为（12.48±3.05）mg/L和（10.86±2.75）mg/L，达峰中位时间（Tmax）分别为1.5（1.0，2.0）h和2.0（1.0，4.0）h，平均药时曲线下面积 (AUC0～∞) 分别为（33.42±7.58）h·mg/L和（32.71±7.18）h·mg/L；舒巴坦匹呋酯实测平均高峰血药浓度(Cmax)分别为（8.44±2.43）和（9.20±3.00）mg/L，达峰中位时间（Tmax）分别为2.0（1.0，5.0）h和2.0（0.75，5.0）h，平均药时曲线下面积 (AUC0～∞) 分别为（35.31±10.81）h·mg/L和（36.52±12.94）h·mg/L。对国产片剂与进口片剂中阿莫西林和舒巴坦匹呋酯的Cmax、AUC0～8和AUC0～∞对数值进行方差分析，结果除国产品与进口品中阿莫西林Cmax对数值在两制剂间差异具统计学意义外(P＜0.05)、其他参数在两制剂间、试验阶段间、服药顺序间的差异均无统计学意义(P＞0.05)。但在服药顺序组中受试者间差异具统计学意义(P＜0.05)，国产品与进口品相比，制剂中阿莫西林相对生物利用度为(102.47±9.70)％。 舒巴坦匹呋酯相对生物利用度为(98.61±14.91)％。结论 受试国产片剂与对照进口片剂具生物等效性。

【关键词】 阿莫西林/舒巴坦；生物等效性

The evaluation of bioequivalence of amoxycillin/sulbactum pivoxil

【Abstract】 Objective To study the bioequivalence of amoxycillin/sulbactum pivoxil.Methods Twenty two normal volunteers were enrolled in a randomized crossover study. Each volunteer was given orally a single dose of 1000mg domestic amoxycillin/sulbactum pivoxil (tested preparation) or 1000mg imported amoxycillin/sulbactum pivoxil (reference preparation) in empty. The plasma concentrations were determined by high performance liquid chromatography (HPLC) . Two one-sided t-test was used to evaluate the bioequivalence.Results The concentration-versus-time data in both groups were fitted to a one-compartment model. The pharmacokinetic parameters of amoxycillin in domestic and imported tablets were : Cmax (12.48±3.05)mg/L and (10.86±2.75)mg/L; Tmax 1.5 (1.0～2.0 )h and 2.0 (1.0～4.0 )h ; AUC0→∝ (33.42±7.58)h·mg/L and (32.71±7.18) h·mg/L，respectively. The pharmacokinetic parameters of sulbactum in domestic and imported tablets were:Cmax (8.44±2.43)mg/L and (9.20±3.00)mg／L ; Tmax 2.0 (1.0～5.0 )h and 2.0 (0.75～5.0 )h ; AUC0→∝ (35.31±10.81)h·mg/L and (36.52±12.94) h·mg/L ，respectively. Analysis of variance (ANOVA) was used to analysed the logarithm of Cmax， AUC0→8， AUC0→∝ of amoxycillin and sulbactum pivoxil in the two preparations . The difference of all the parameters between the two tablets， test phases， administration sequence had no statistical significance (P＞0.05) ，except the difference of Cmax between the two preparations (P＜0.05) . But there was statistical difference among the participants in administration sequence (P＜0.05). Compared with the imported!tablets ，the relative bioavailability of amoxycillin and sulbactum pivoxil in domestic tablets were (102.49±9.70)% and (98.61±14.91)%， respectively.Conclusion Domestic and imported amoxicilin/sulbactum pivoxil were bioequivalent.