青霉素V钾咀嚼片的药动学和生物等效性研究

Pharmacokinetics and Bioequivalence of Phenoxymethylpenicillin Potassium Chewable Tablets in Healthy Volunteers

目的:研究青霉素V钾咀嚼片在健康人体的药物动力学及生物等效性。方法:19名健康志愿者随机双交叉、单剂量口服受试制剂和参比制剂0.472g,用液相色谱-串联质谱法(LC-MS/MS)测定人血浆中青霉素V的浓度,利用DAS 2.0药物动力学软件计算有关药物动力学参数、相对生物利用度,并评价2种制剂的生物等效性。结果:受试制剂和参比制剂的t_(max)分别为(0.54±0.09)h和(0.53±0.13)h;C_(max)分别为(10.64±3.84)μg·ml^(-1)和(10.87±4.43)μg·ml^(-1);t_(1/2)分别为(0.74±0.20)h和(0.75±0.10)h。AUC_(0-6h)分别为(11.92±4.04)μg·ml^(-1)·h和(12.34±4.17)μg·ml^(-1)·h;AUC_(0-∞)分别为(12.00±4.04)和(12.43±4.17)μg·ml^(-1)·h。青霉素V钾咀嚼片的相对生物利用度为(97.9±12.8)%。结论:两种制剂具有生物等效性。

Objective ： To study the pharmacokinetics and bioequivalence of phenoxymethylpenicillin potassium chewable tablets in healthy volunteers. Method： A single oral dose （0. 472g test and reference formulations）was given to 19 healthy volunteers according to an open randomized crossover design. Liquid chromatography-mass spectrometry/mass spectrometry （LC-MS/MS） method were used for the determination of phenoxymethylpenicillin in human plasma. The pharmaeokinetics parameters and the relative bioavailability were calculated and the bioequivalenee of two formulations were evaluated by DAS 2.0 software. Result ： The main pharmacokinetics parameters of phenoxymethylpenicillin potassium chewable tablets and phenoxymethylpenicillin potassium tablets were as follows： tmax were （0.54±0.09）h and （0.53±0.13）h;Cmax were （10.64±3.84） and （10.87 ±4.43）μg·ml^-1·h;t1/2 were （0.74±0.20）h and （ 0.75 ± 0. 1 0） h, A UC0-6h were （ 11.92± 4.04 ） and （ 12.34 ± 4.17 ） μg·ml^-1·h ; A UC0-∞ were （ 12.00 ± 4.04 ） and （ 12.43 ± 4.17 ） μg·ml^-1·h, respectively. The relative bioavailability of drug was （97.9 ± 12.8 ） %. Conclusion： The two phenoxymethylpenicillin potassium formulations are bioequivalence.