青霉素V钾健康人体药物动力学及相对生物利用度

Study on the pharmacokinetics and relative bioavailability of penicillin V potassium in healthy volunteers

以美国进口的青霉素 V钾片为标准参比制剂 ,研究国产青霉素 V钾片和胶囊在健康人体药物动力学及相对生物利用度。按 3制剂、3周期的 3× 3拉丁方试验设计 ,9名健康男性受试者 ,分别口服进口及国产青霉素 V钾 15 0 0 mg,采用微生物法测定血药浓度 ,用 3P87软件经微机处理药 -时数据。结果证明 ,进口及国产青霉素 V钾的体内过程均符合二房室模型 ,与标准参比制剂相比 ,两种被试制剂的 AUC、Cmax、Tmax均无显著差异 ,相对生物利用度分别为 10 2 .5 1± 11.0 9% (84.6 1%～ 114.49% )与 92 .5 0± 8.47% (82 .88%～10 6 .6 3% )。结论 :国产青霉素 V钾片和胶囊均具有生物等效性。

Compared with imported penicillin V potassium tablets, the pharmacokinetics and relative bioavailability of domestic penicillin V potassium tablets and capsules were studied in 9 male healthy volunteers who received a single oral dose of 1500mg penicillin V potassium in crossways. The serum concentrations of penicillin V potassium were determined by microbiological assay. Data of serum level time were disposed with 3P87 software and computer. Results demonstrated that the data of penicillin V potassium were fitted to two compartment open model. The main parameters of imported penicillin V potassium tablets, the domestic penicillin V potassium tablets and capsules were as follows, C max : 13.80±3.35, 14.05±1.55, 14.85±1.45mg/L; T max : 0.72±0.15, 0.72±0.08, 0.69±0.11h; AUC: 21.51±2.38, 22.01±3.13, 21.14±2.81(mg·h)/L respectively. There were no significant differences in the pharmacokinetic parameters between imported tablets and domestic tablets or capsules, respectively. Compared with the imported tablets, the relative bioavailabilities of domestic tablets and capsules were 102.51±11.09% (84.61%~114.49%) and 92.50±8.47% ( 82.88% ~106.63%) respectively. The results showed that domestic tablets and capsules had the same efficacies as imported ones.