谱圣康口服液单次给药在中国健康人体药代动力学研究  

Pharmacokinetics of single dose of Picika oral solution in Chinese healthy volunteers

作　　者：朱珍真[1] 段锋[1] 毕京峰[1] 陈贞[1] 王敏[1] 张丽[1] 姬慧[1] 郎丽巍[1] 陈本超[1] 魏振满[1] 

机构地区：[1]中国人民解放军第302医院新药临床试验中心,北京100039

出　　处：《中国临床药理学杂志》2016年第3期230-234,共5页The Chinese Journal of Clinical Pharmacology

摘　　要：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 Picika oral solution in healthy subjects after single dose. Methods This study taken random, three cross experiment design, 12 subjects were randomly divided into 6 groups, each group was 2 cases~ then they were respectively given single oral doseof Picika oral solution （60, 90, 120 mL） in each cycle. Before and after administration, biological samples were collected for detection of blood drug concentration and urine drug concentra- tion, furthermore, calculation of blood and urine drug pharmacokinetic parameters. Results After single oral dose of 60, 90, 120 mL Picika oral solution, the main pharmacokinetic parameters of plasma CKL - A03, Cmax were （3.08 ±0.92）, （3.63 ±0.75）, （4,29±1. 00）ug·L-1, tmax were （57.50 ± 17.90）, （52.50 ± 20. 73 ）, （56. 25 ± 19. 32） min, tl/2 were （ 197.51 ± 106.35 ）, （233.86 ± 196.75 ）, （ 141.34 ± 65. 16） min, AUC0 were （ 383.28 ± 86.42 ）, （ 479, O0 ± 136.25 ）, （540.59±102.87）pg · L-1 . min, AUC0-1 were （710.06 ±233.03）, （916. 59±378.62）, （782. 65± 130. 40）ug·L-1 min, respectively.The main pharmacokinetic parameters of urine CKL -A03, tl/2 were （1.29 ±0, 33）, （1.23 ±0. 20）, （1.11±0. 11） h, total urine discharge rates were （0. 28 ± 0.22） %, （0. 20 ± 0. 11 ） %, （0. 18 ± 0, 09 ） %, urine discharge amount were （74486. 02 ± 57923.42）, （80015.14 ± 43379.01 ）, （93017.33± 46658.61 ） mg. Conclusion The maximum oral absorption amount of Picika oral solution is possible 90 mL. And there is no apparent proportional relationship between the total urine discharge rate, urine discharge amount and the increased doses.

关 键 词：谱圣康口服液 单次给药 药代动力学 血药浓度 尿药浓度 

分 类 号：R979.5[医药卫生—药品] R969.1[医药卫生—药学]