阿莫西林/双氯西林钠分散片的人体生物等效性研究

Study on Bioequivalence of Amoxicillin and Dicloxacillin Sodium Dispersible Tablets in Human Body

目的：研究阿莫西林／双氯西林钠分散片的人体生物等效性。方法：采用双周期交叉设计试验，20名健康男性受试者随机交叉单剂量口服阿莫西林／双氯西林钠分散片（受试制剂）和阿莫西林／双氯西林钠胶囊（参比制剂）750mg，以高效液相色谱法测定人血浆中阿莫西林、双氯西林经-时血药浓度，用DAS软件拟合计算药动学参数。结果：受试制剂与参比制剂阿莫西林的tmax分别为（1．16±0．26）、（1．24±0．27）h，Cmax分别为（6．32±2．56）、（6．59±2．33）／μg·mL^-1，AUC0～7分别为（12．27±2．25）、（12．66±2．68）／μg·h·mL^-1，AUC0-∞。分别为（15．48±2．38）、（15．47±3．71）／μg·h·mL^-1；双氯西林的tmax分别为（0．94±0．23）、（0．93±0．18）h,Cmax分别为（12．12±5．71）、（12．12±4．15）μg·mL^-1，AUC0～7分别为（23．49±4．20）、（23．25±3．64）μg·h·mL^-1，AUC0～∞分别为（24．93±3．96）、（24．50±3．66）／μg·h·mL^-1受试制剂阿莫西林与双氯西林的相对生物利用度分别为（97．7±8．2）％、（102．0±16．8）％。结论：阿莫西林／双氯西林钠分散片与阿莫西林／双氯西林钠胶囊具有生物等效性。

OBJECTIVE：To study the relative bioequivalence of Amoxicillin and Dicloxacillin Sodium dispersible tablets in human body.METHODS： The plasma concentrations of amoxicillin and dicloxacillin in 20 healthy male volunteers were determined by HPLC method after being orally administered with single dose of 750mg test and reference preparation by randomized crossover way;the pharmacokinetic parameters and the relative bioequivalence of the two preparations of amoxicillin and dicloxacillin were calculated by DAS software.RESULTS：The main pharmacokinetic parameters of amoxicillin were as follows： tmax were（1.16±0.26） and （1.24±0.27） h,C were（6.32±2.56） and （6.59±2.33）μg·mL^-1 1, AUC0-7 were （12.27±2.25） and （12.66± 2.68）μg·h·mL^- 1, AUC0-∞were（15.48±2.38） and （15.47±3.71）μg·h·mL^- 1.Pharmacokinetic parameters of dicloxacillin were as follows： tmax were （0.94±0.23）and（0.93±0.18）h,Cmax were （12.12±5.71）and（12.12±4.15）μg · mL^- 1, AUC0 -7 were （ 23.49 ± 4.20） and （ 23.25 ± 3.64）μg · h · mL ^-1 AUC0- ∞ were （ 24.93 ± 3.96） and （ 24.50 ± 3.66）μg · h · mL ^-1. The relative bioavailability of amoxicillin were（97.7 ± 8.2） % and（102.0 ±16.8） % for dicloxacillin.CONCLUSION： Amoxicillin and Dicloxacillin Sodium dispersible tablets and capsules were bioequivalent.