阿莫西林-克拉维酸钾(14:1)颗粒剂生物等效性研究

Bioequivalence of amoxicillin-clavulanate potassium (14 : 1) granules

目的:测定阿莫西-林克拉维酸钾(14:1)颗粒剂生物等效性。方法:18名健康男性志愿者分别采用2制剂、2周期(周期间隔为5 d)双交叉试验方法,口服受试和参比片剂1片(每片含阿莫西林600 mg,克拉维酸钾42.9 mg),采用微生物学方法测定血浆中药物浓度。结果:受试及参比制剂的主要药动学参数分别为:阿莫西林AUCo-sh分别为(25.5±4.12)mg·h/L和(25.0±4.05)mg·h/L;Cmax分别为(9.95±1.45)mg/L和(9.48±1.66)mg/L。克拉维酸钾的AUC0-8h分别为(1.38±0.467)mg·h/L和(1.46±0.508)mg·h/L;Cmax分别为(0.648±0.586)mg/L和(0.586±0.167)mg/L。结论:经统计分析结果显示两制剂生物等效。

Objective: To determine the bioequivalence of amoxicillin-clavulanate potassium (14 : 1) granules in healthy volunteers. Methods: A randomized cross-over (5 days in distance) study on the bioequivalence of amoxicillin-clavulanic acid granules compared with amoxicillin-clavulanic acid tablet were done in 18 healthy male volunteers. One granules tablet (each tablet contains amoxicillin 600 mg + clavulanic acid 42. 9 mg) or one common form tablet (each tablet contains the same amount of amoxi cillin and clavulanic acid ) were given to every volunteer in each experiment. Serum samples at different time were taken and drug concentration were measured by bioassay method. Results: The pharmacokinetic parameters of granule tablet and common form tablet were amoxicillin AUC0-8h (25. 5 ±4. 12) mg · h/L and (25.0±4.05) mg · h/L, Cmax(9. 95 ± 1. 45) mg/L and( 9. 48 ± 1. 66) mg/L, clavulanate potassium AUC0-8h(1. 38 ±0. 467) mg · h/L and (1. 46 ± 0. 508) mg · h/L, Cmax(0. 648 ± 0. 586 )mg/L and (0. 586 ± 0. 167) mg/L respectively. Conclusions: The two preparations of amoxicillin-clavulanate potassium are bioequivalent.