国产青霉素V钾颗粒剂的药动学及相对生物利用度

目的观察健康志愿者口服青霉素V钾颗粒剂的药动学及相对生物利用度。方法12名健康志愿者随机交叉口服等剂量青霉素V钾颗粒剂及青霉素V钾片剂(参比药)，并用微生物法测定青霉素V钾的血药浓度。结果单剂量空腹口服500mg受试药与参比药后T

Pharmacokinetics and bioavailability of domestic phenoxymethylpenicillin granules in healthy volunteers

OBJECTIVE：To study the pharmacokinetics and relativebioavailability of phenoxymethylpenicillin granules.METHODS：A randomized crossover study in the pharmacokinetics of phenoxymethylpenicillin (tablet and granules) at a single oral dose of 500mg was conducted in 12 healthy volunteers.In this paper,microbiologic assay was adopted.RESULTS：After oral administration of a single dose of 500mg phenoxymethylpenicillin,the peak concentration (Cmax) of phenoxymethylpenicillin in plasma averaged (9.1±3.1)μg.ml-1 and (9.7±2.5)μg.ml-1 at (36.7±7.8)min and (30.0±6.0)min,the areas under the drug concentration curves were (597.0±116.2)μg.min.ml-1 and (585.3±133.1)μg.min.ml-1 (tablet and granules) respectively.The relative bioavailability of phenoxymethylpenicillin was (98.0±11.8%).CONCLUSIONS：The pharmacokinetics of phenoxymethylpenicillin (tablet and granules) were similar and the results of statistics showed that the two formulations were bioequivalent.