论文部分内容阅读
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 dispersible tablets in healthy volunteers. Methods Twelve healthy male volunteers were randomized to receive a crossover study. A single oral dose of roxithromycin dispersible tablets and capsules (30 mg) was administered orally. Microbial assay was used to determine plasma concentrations at different time points. The 3P97 program fitting, calculation of pharmacokinetic parameters. Results The concentration-time curves of roxithromycin dispersible tablets and capsules were in accordance with the two-compartment model. The main pharmacokinetic parameters were: T1 / 2 β were (1.76 ± 2.77) h and (1.492 ± 3.1 2) h and Tmax were (1.38 ± 0.23) h and (1.63 ± 0.23) h, respectively, and the C max were (8.37 ± 0.66) mg / L and (8.2 3 ± 0.63 ) mg / L, AUC0 → ∞ were (91.84 ± 1.190) h · mg / L and (88.55 ± 1.07) h · mg / L, respectively. The statistical analysis showed that there was no significant difference between Cmax and AUC0 → ∞ of the two preparations (P> 0.05). The relative bioavailability of roxithromycin dispersible tablets was (1. 0 ± 3.75 ± 5.58)%. Conclusion The two preparations are bioequivalent.