罗红霉素分散片的人体药物动力学及相对生物利用度

Pharmacokinetics and relative bioavailability of roxithromycin dispersive tablets in healthy volunteers

目的 研究罗红霉素分散片在健康人体内的药物动力学和相对生物利用度。方法 1 2名健康男性志愿者 ,采用随机交叉试验设计 ,单剂量口服国产罗红霉素分散片和胶囊 30 0mg ,用微生物检定法测定不同时间的血药浓度。经 3P97程序拟合 ,计算药物动力学参数。结果 罗红霉素分散片和胶囊血药浓度 -时间曲线均符合二室模型 ,主要药物动力学参数 :T1 / 2 β分别为(1 4.76± 2 .77)h和 (1 4.92± 3.1 2 )h ,Tmax分别为 (1 .38± 0 .2 3)h和 (1 .63± 0 .2 3)h ,Cmax分别为(8.37± 0 .66)mg/L和 (8.2 3± 0 .63)mg/L ,AUC0→∞ 分别为 (91 .84± 1 1 .90 )h·mg/L和 (88.55± 1 0 .70 )h·mg/L。经统计学分析 ,两制剂的Cmax和AUC0→∞ 均无显著性差异 (P >0 .0 5) ,罗红霉素分散片的相对生物利用度为 (1 0 3.75± 5.58) %。结论 两制剂具有生物等效性。

Objective To study the pharmacokinetics and relative bioavailability of roxithromycin dispersive tablets in healthy volunteers.Methods A single oral dose of 300?mg roxithromycin dispersive tablets and capsules were given to 12 healthy male volunteers according to an open randomized crossover design.The concentrations of roxithromycin in serum were determined by microbioassay. The pharmacokinetic parameters of roxithromycin were calculated with 3P97 program.Results The concentration time curves of roxithromycin dispersive tablets or roxithromycin capsules conformed to a two compartment model. The main pharmacokinetic parameters of the two formulations were as follows: the T 1/2β was (14.76±2.77) h and (14.92±3.12) h, the T max was (1.38±0.23) h and (1.63±0.23) h, the C max was (8.37±0.66) mg/L and (8.23±0.63) mg/L, the AUC 0→∞ was (91.84±11.90)h·mg/L and (88.55±10.70)h·mg/L,respectively.The results of statistical analysis showed that there was no significant difference between the two formulations in the C max and AUC 0→∞ . The relative bioavailability of roxithromycin dispersive tablets to capsules was (103.75±5.58)%.Conclusion The two formulations were bioequivalent.