摘要
目的 :研究地尔硫 卓艹 缓释片在健康人体的药物动力学及相对生物利用度。方法 :以上海产地尔硫 卓艹 缓释片为参比制剂 ,焦作市第二制药厂产地尔硫卓艹 缓释片为受试制剂 ,分别进行单次和多次用药试验 ,12名受试者采用随机交叉口服单剂量 (12 0mg)和多剂量 (6 0mg ,3次 /d ,共用 5d)地尔硫卓艹 缓释片。高效液相色谱 (HPLC)法测定用药后不同时间血清中地尔硫 卓艹质量浓度 ,用 3P87软件处理药 时数据。结果 :单次用药后 ,2制剂的体内过程均符合一房室开放模型 ,血药浓度分别在用药后 (2 .0 0± 0 .5 2 )h和 (1.88± 0 .43)h达峰值 (131± 17) μg·L-1和 (12 2± 11)μg·L-1,药时曲线下面积 (AUC)分别为 (112 2± 2 5 6 ) μg·L-1和 (110 9± 2 32 ) μg·h·L-1,受试制剂的相对生物利用度为(10 0 .0± 11.9) % (84.4%～ 117.5 % ) ;多次用药血药浓度达稳态后 ,峰浓度 (Cmax)分别为 (111± 8) μg·L-1和 (10 9± 9)μg·L-1,谷浓度 (Cmin)分别为 (35± 9) μg·L-1和 (38± 10 ) μg·L-1。两者血药浓度波动系数 (FI)分别为 (1.2 3± 0 .2 9)和 (1.12± 0 .2 3)。结论 :受试制剂在健康人体具有明显的缓释特征 ,且和参比制剂具有生物等效性。
Aim:To study the pharmacokinetics and relative bioavailability of diltiazem slow release tablets in healthy volunteers. Methods: Using the preparation from Shanghai as the reference preparation and using the preparation from Jiaozuo as the tested preparation. Twelve male healthy volunteers orally took a single and multiple doses of diltiazem slow release tablets in an open randomized crossover study. Serum concentrations of diltiazem were measured by HPLC. Results: The serum concentration time curves of the two preparations appeared to fit oral first order absorption and one compartment open model after a single oral dose. The peak levels in serum averaged (131±17)μg·L 1 and(122±11) μg·L 1 at (2.00±0.52)h and (1.88±0.43)h and the AUC were (1 122±256)μg·L 1 and (1 109±232)μg·L 1 , respectively. The relative bioavailability of the tested preparations were (100.00±11.9)%. Following multiple dosing mean steady state , C max values were (111±8)μg·L 1 and (109±9)μg·L 1 and C min values were (35±9)μg·L 1 and (38±10)μg·L 1 ,respectively. The peak to through fluctuation index ( FI ) for the two preparations were (1.23±0.29)and (1.12±0.23), respectively. Conclusion: The tested preparations have an obvious sustained released specialty in healthy people, and the two preparations were bioequivalent.
出处
《河南医科大学学报》
2000年第3期250-253,共4页
Journal of Henan Medical University
基金
河南省卫生厅下达研究项目
