论文部分内容阅读
目的 研究 12名男性健康受试者单剂量口服国产与进口硝苯地平缓释胶囊 (2 0mg)后的人体内药物动力学和相对生物利用度。方法 12名男性健康受试者随机分为两组 ,进行双交叉自身对照试验。以尼莫地平为内标 ,用高分辨毛细管气相色谱 电子捕获 (ECDNi- 6 3)检测法测定人血浆中硝苯地平的浓度。对血药浓度 时间数据以非房室模型依赖性方法估算药物动力学参数。结果 国产与进口制剂的AUC0～∞ ,cmax,tmax,t1/2 分别为 (46 4.8± 16 9.1)和 (46 2 .2± 15 2 .1)ng·h·ml-1,(39.7±9.1)和 (41.4± 9.1)ng·ml-1,(2 .6± 0 .6 )和 (3.4± 1.3)h ,(10 .4± 4.0 )和 (10 .1± 4.4)h ;经方差分析均无显著性差异 (α =0 .0 5 )。国产缓释胶囊的相对生物利用度为 (10 6 .4± 13.6 ) %。结论 国产与进口缓释胶囊生物等效 ,口服国产硝苯地平缓释胶囊 2 0mg可维持有效血药浓度达 12h。
Objective To study pharmacokinetics and relative bioavailability of 12 single-dose oral Chinese and imported nifedipine sustained-release capsules (20 mg) in 12 male healthy subjects. Methods Twelve male healthy subjects were randomly divided into two groups to conduct double-cross self-controlled trials. Nimodipine was used as an internal standard to determine the concentration of nifedipine in human plasma by high resolution capillary gas chromatography electron capture (ECDNi-63) assay. Pharmacokinetic parameters were estimated on plasma concentration time data in a non-compartmental model-dependent manner. Results The AUC0 ~ ∞, cmax, tmax and t1 / 2 of domestic and imported preparations were (46 4.8 ± 16 9.1) and (46 2 ± 15 2 .1) ng · h · ml- ) And (41.4 ± 9.1) ng · ml-1, (2.6 ± 0.6 and 3.4 ± 1.3) h, (10.4 ± 4.0) and (10.1 ± 4.4) There was no significant difference (α = 0.05). The relative bioavailability of domestic sustained release capsules was (106.4 ± 13.6)%. Conclusion Domestic and imported sustained-release capsules are bioequivalent, oral administration of nifedipine sustained-release capsules 20mg can maintain effective plasma concentration of 12h.