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目的:研究国产与进口乌拉地尔缓释胶囊药动学及人体相对生物利用度。方法:18例健康男性志愿者,用随机双交叉试验方法,单剂量及多剂量口服乌拉地尔缓释胶囊受试或参比制剂30 mg,采用RP-HPLC法测定血浆中乌拉地尔浓度,进行药动学及相对生物利用度分析。结果:单剂量口服受试制剂和参比制剂的Tmax分别为(3.9±0.8)和(4.1±1.0)h;Cmax分别为(291.7±66.0)和(307.4±72.2)μg.L-1;t1/2分别为(5.1±1.1)和(4.7±0.8)h;Cl分别为(11.0±2.0)和(10.5±2.5)L.h-1;Vd分别为(1.6±0.5)和(1.6±0.4)L。多剂量口服受试制剂和参比制剂的Tmax分别为(4.3±1.0)和(5.1±0.9)h;Cmax分别为(323.6±65.8)和(347.8±60.7)μg.L-1;Cmin分别为(112.8±33.3)和(120.1±32.9)μg.L-1;Cav分别为(303.5±72.2)和(318.6±68.2)μg.L-1;Cl分别为(8.9±3.0)和(8.3±2.1)L.h-1;Vd分别为(1.3±0.4)和(1.2±0.4)L。单剂量和多剂量口服乌拉地尔缓释胶囊后,体内相对生物利用度分别为(95.5±14.0)%和(95.6±15.7)%。结论:2种制剂在人体内具有生物等效性。
Objective: To study the pharmacokinetics and relative bioavailability of Urapidil sustained-release capsules made in China and abroad. Methods: Eighteen healthy male volunteers were randomly divided into two groups: randomized double-crossover test, single or multiple doses of urapidil sustained-release capsules or reference preparations 30 mg, the plasma concentration of urapidil was determined by RP-HPLC, Pharmacokinetics and relative bioavailability analysis. RESULTS: The Tmax of the single-dose oral test formulation and the reference formulation were (3.9 ± 0.8) and (4.1 ± 1.0) h, respectively; the Cmax values were 291.7 ± 66.0 and 307.4 ± 72.2 μg.L- / (2) were (5.1 ± 1.1) and (4.7 ± 0.8) h respectively; Cl was (11.0 ± 2.0) and (10.5 ± 2.5) Lh- . The Tmax of the multi-dose oral test formulation and the reference formulation were (4.3 ± 1.0) and (5.1 ± 0.9) h, respectively, and the Cmax were (323.6 ± 65.8) and (347.8 ± 60.7) μg.L- (112.8 ± 33.3) and (120.1 ± 32.9) μg.L-1, respectively, and were respectively (303.5 ± 72.2 and 318.6 ± 68.2) μg · L-1 for Clc and 8.9 ± 3.0 and 8.3 ± 2.1 for Cl ) Lh-1; Vd were (1.3 ± 0.4) and (1.2 ± 0.4) L, respectively. The relative bioavailability in vivo was (95.5 ± 14.0)% and (95.6 ± 15.7)%, respectively, after oral administration of urapidil sustained-release capsules. Conclusion: The two formulations are bioequivalent in humans.