青霉素V钾颗粒剂在健康人体中的药动学及相对生物利用度

目的 :研究青霉素V钾颗粒剂在健康人体中的相对生物利用度 ,评价其生物等效性。方法 :以美国进口的青霉素V钾片为标准参比制剂 ,研究洛阳春都制药公司研制的青霉素V钾颗粒剂相对生物利用度。 10名健康受试者随机交叉口服青霉素V钾被试及参比制剂各 15 0 0mg后 ,采用微生物法测定不同时间血清中药物浓度 ,用3P87软件经微机处理药 时数据。结果 :2种制剂的体内过程均符合二房室开放模型。Cmax分别为 (12 92± 2 2 1)mg·L- 1 和 (12 91± 2 0 4)mg·L- 1 ,Tmax均为 (0 70± 0 11)h ,曲线下面积 (AUC)分别为 (2 0 30± 2 90 )mg·h·L- 1 和 (19 39±2 35 )mg·h·L- 1 。与参比制剂相比 ,被试制剂的相对生物利用度为 (96 0 0± 5 5 6 ) % (86 14%～ 10 5 35 % )。结论 :对2种制剂的AUC、Cmax等进行方差分析、双单侧t检验证明 ,2种制剂具有生物等效性。

Pharmacokinetics and relative bioavailability of penicillin V potassium inhealthy volunteers

To study the pharmacokinetics and relative bioavailability ofpenicillin V potassium in healthy volunteers.Mefthods: The serum concentrations of penicillin V potassium were determined by microbiological assay in 10 healthy male volun-teers after an oral dose of 1500 mg penicillin V potassium in crossways. Data of serum leveltime were processed with 3P87 software. Results: Findings revealed that the data of penicillin V potassium were fitted to two-compartment open model. The Cmax values were (12.92+2.21) and (12.91 +2.04) rng·L-1 and the Tmax(0.70+0.11) and (0.70+0. 11)h and the AUC were(20.30 ± 2.90) and ( 19.39 ± 2.35) mg· h· L -1, respectively. The relative bioavailability of granules to tablets were ( 96.00 ± 5.56) % (86.14%～105.35% ). Cornclusiofn: There is no significant difference in pharmacokinetic parameters between the two formulations, suggesting that both formulations are bioequivalent.