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目的 研究国产和进口盐酸地尔硫控释胶囊在健康人体内的代谢动力学过程 ,并评价这两种制剂的生物等效性。方法 单剂量 (180mg)、多剂量 (180mg·d-1× 6d)试验各选 2 0例受试者 ,受试者随机分组、自身对照口服药物 ,采用反相HPLC测定血浆中地尔硫的浓度。结果 单剂量时 ,参比制剂与受试制剂主要药动学参数cmax分别为 (80 .8± 2 5 .0 )及 (89.0±2 5 .6 ) μg·L-1;tmax分别为 (5 .75± 2 .0 2 )及 (6 .0 0± 2 .5 5 )h ;t1/2 分别为 (11.4 4± 1.4 1)及 (10 .80± 1.4 4 )h ;AUC0～t分别为(16 35 .6± 35 5 .7)及 (16 10 .5± 311.7) μg·h·L-1;AUC0～∞ 分别为 (16 81.1± 35 6 .9)及 (16 4 8.8± 312 .1) μg·h·L-1;受试制剂相对于参比制剂的生物利用度F为 (10 0 .0± 17.1) %。多剂量时 ,参比制剂与受试制剂主要药动学参数cmax分别为 (177.6± 4 7.0 )及 (16 4 .3± 36 .8) μg·L-1;cmin分别为 (44 .3± 16 .3)及 (40 .3± 14 .7) μg·L-1;tmax分别为 (3.88± 2 .2 1)及 (3.73±2 .2 0 )h ;t1/2 分别为 (10 .2 7± 3.0 5 )及 (10 .73± 2 .72 )h ;AUCSS分别为 (2 32 8.9± 6 37.3)及 (2 16 8.8± 5 4 4 .5 ) μg·h·L-1;cav分别为 (97.0± 2 6 .6 )及 (90 .4± 2 2 .7) μg·L-1;DF分
Objective To study the metabolic kinetics of domestic and imported diltiazem hydrochloride controlled-release capsules in healthy volunteers and to evaluate the bioequivalence of the two preparations. Methods A single dose (180mg), multiple doses (180mg · d-1 × 6d) test each 20 subjects, the subjects were randomly divided into self-control oral medication, reverse phase HPLC determination of plasma Diltiazem concentration. Results The main pharmacokinetic parameters (cmax) were (80.8 ± 2.5) and (89.0 ± 2.56) μg · L-1, respectively, for the reference formulation and the test formulation at a single dose; tmax was .75 ± 2.02) and (6.0 ± 2.55) h, respectively; t1 / 2 were (11.4 4 ± 1.4 1) and (10.8 ± 1.4 4) h respectively; AUC0 ~ t were (16 35.6 ± 35 5 .7) and (16 10 .5 ± 311.7) μg · h · L -1, respectively; AUC0 ~ ∞ were (16 81.1 ± 35 6 .9) and (16 4 8.8 ± 312. 1) μg · h · L -1; and the bioavailability F of the test preparation relative to the reference preparation was (100.0 ± 17.1)%. The main pharmacokinetic parameters (cmax) were (177.6 ± 4 7.0) and (16 4 .3 ± 36.8) μg · L-1, respectively, for the reference drug and the test compound at multiple doses. The cmin values were (44.3 ± 16.3 and 40.3 ± 14.7 μg · L-1, respectively; tmax was (3.88 ± 2.21) and (3.73 ± 2.02) h respectively; t1 / 2 was (10. 2 7 ± 3.0 5) and (10.73 ± 2.72) h respectively; AUCSS was (2 32 8.9 ± 6 37.3) and (2 16 8.8 ± 5 4 4 .5) μg · h · L -1, respectively; cav (97.0 ± 26.6) and (90.4 ± 22.7) μg · L-1, respectively; DF