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目的评价谱圣康口服液单次给药在健康受试者体内的药代动力学变化。方法用随机、三交叉试验设计。将12例受试者随机分为6组,每组2例,分别于3个周期口服谱圣康口服液60,90,120 m L各1次,洗脱期为1周。给药前后按时间点采集生物样本以检测血药浓度和尿药浓度,并计算血药及尿药的主要药代动力学参数。结果单次口服谱圣康口服液60,90,120 m L后,血浆中CKL-A03的主要药代动力学参数:Cmax分别为(3.08±0.92),(3.63±0.75),(4.29±1.00)μg·L~(-1);tmax分别为(57.50±17.90),(52.50±20.73),(56.25±19.32)min;t1/2分别为(197.51±106.35),(233.86±196.75),(141.34±65.16)min;AUC0-t分别为(383.28±86.42),(479.00±136.25),(540.59±102.87)μg·L~(-1)·min;AUC0-∞分别为(710.06±233.03),(916.59±378.62),(782.65±130.40)μg·L~(-1)·min。尿液中CKL-A03的主要药代动力学参数:t1/2分别为(1.29±0.33),(1.23±0.20),(1.11±0.11)h;总尿排率分别为(0.28±0.22)%,(0.20±0.11)%,(0.18±0.09)%;尿排总量分别为(74486.02±57923.42),(80015.14±43379.01),(93017.33±46658.61)mg。结论谱圣康口服液最大吸收量可能为90 m L,且随剂量增加,总尿排率与尿排总量变化无明显比例关系。
Objective To evaluate the pharmacokinetic changes of Compound Shengkang oral solution in healthy subjects. Methods Randomized, three-crossover trial design. Twelve subjects were randomly divided into 6 groups with 2 cases in each group. The oral administrations of Shengkang Oral Liquid 60,90,120 m L were administered orally in 3 cycles, and the elution period was 1 week. Before and after the administration of biological samples collected at the time point to detect the concentration of blood and urine concentration, and calculate the main pharmacokinetic parameters of blood and urinary drugs. Results The main pharmacokinetic parameters of plasma CKL-A03 were (3.08 ± 0.92), (3.63 ± 0.75) and (4.29 ± 1.00) μg respectively after oral administration of Shengkang Oral Liquid 60, 90 and 120 m L · L ~ (-1) and tmax were (57.50 ± 17.90) and (52.50 ± 20.73) and (56.25 ± 19.32) min, respectively; t1 / 2 were (197.51 ± 106.35) and (233.86 ± 196.75 and 141.34 ± 65.16) min; AUC0-t were (383.28 ± 86.42), (479.00 ± 136.25) and (540.59 ± 102.87) μg · L -1 · min, respectively; AUC0-∞ were (710.06 ± 233.03) and ± 378.62), (782.65 ± 130.40) μg · L -1 · min. The main pharmacokinetic parameters of urine CKL-A03 were (1.29 ± 0.33), (1.23 ± 0.20), (1.11 ± 0.11) h and (0.28 ± 0.22)%, respectively , (0.20 ± 0.11)% and (0.18 ± 0.09)%, respectively. The total urinary excretion were (74486.02 ± 57923.42), (80015.14 ± 43379.01) and (93017.33 ± 46658.61) mg, respectively. Conclusion The maximal absorption of Pu Shengkang Oral Liquid may be 90 m L, and with the increase of dosage, the total urinary discharge rate is not significantly proportional to the change of total urinary output.