论文部分内容阅读
目的研究2种苯磺酸氨氯地平片的相对生物利用度及其生物等效性。方法采用双周期、随机、交叉试验设计,将20名男性健康受试者随机分成2组,单剂量、交叉口服受试制剂及参比制剂苯磺酸氨氯地平片10 mg,采集不同时间点的静脉血样,用超高效液相色谱—串联质谱法测定给药后不同时间氨氯地平的血药浓度。结果受试试剂及参比试剂的主要药代动力学参数如下:Tmax分别为(6.32±0.85)h和(5.95±1.23)h;Cmax分别为(6.231±1.734)ng·mL-1和(6.138±1.352)ng·mL-1;T1/2分别为(39.89±9.43)h和(40.02±7.49)h;AUC0-144分别为(273.473±97.167)ng·h·mL-1和(278.314±80.340)ng·h·mL-1;AUC0-∞分别为(303.480±106.054)ng·h·mL-1和(306.412±91.351)ng·h·mL-1。受试制剂对参比制剂的相对生物利用度为(99.7±20.2)%。统计分析结果表明2种苯磺酸氨氯地平片在不同制剂间和不同周期间差异无统计学意义(P>0.05)。结论苯磺酸氨氯地平片的受试制剂与参比制剂具有生物等效性。
Objective To study the relative bioavailability and bioequivalence of amlodipine besylate tablets. Methods A total of 20 male healthy volunteers were randomly divided into two groups. One dose, crossover oral administration of test preparation and reference preparation of amlodipine besylate tablets (10 mg) were collected by double-cycle, randomized, crossover design. Of venous blood samples were determined by ultra performance liquid chromatography-tandem mass spectrometry at different times after administration of amlodipine plasma concentration. RESULTS The main pharmacokinetic parameters of the test and reference agents were as follows: Tmax (6.32 ± 0.85) h and (5.95 ± 1.23) h, respectively; and Cmax were (6.231 ± 1.734) ng · mL-1 and ± 1.352 ng · mL-1; T1 / 2 was (39.89 ± 9.43) h and (40.02 ± 7.49) h respectively; AUC0-144 was (273.473 ± 97.167) ng · h · mL- 1 and (278.314 ± 80.340 ) ng · h · mL-1; AUC0-∞ were (303.480 ± 106.054) ng · h · mL-1 and (306.412 ± 91.351) ng · h · mL-1, respectively. The relative bioavailability of the test preparation to the reference preparation was (99.7 ± 20.2)%. Statistical analysis showed that there was no significant difference in the contents of amlodipine besylate between different preparations and in different weeks (P> 0.05). Conclusion Amlodipine besylate tablets are bioequivalent to the reference formulation.