灯盏花素分散片在健康人体内的相对生物利用度研究  

Bioequivalence of breviscapine dispersible tablets in healthy volunteers

作　　者：杨铁耀[1] 吴小明[1] 李焕明[2] 李清[3] 毕开顺[3] 

机构地区：[1]深圳清华大学研究院中药及天然药物研究中心,广东深圳518057 [2]天津市第四中心医院心内科,天津300140 [3]沈阳药科大学药学院,辽宁沈阳110016

出　　处：《沈阳药科大学学报》2011年第9期732-735,共4页Journal of Shenyang Pharmaceutical University

摘　　要：目的研究灯盏花素分散片与灯盏花素片在健康男性志愿者体内的相对生物利用度。方法采用随机双周期自身交叉对照试验设计,18名健康男性受试者分别经口给予受试制剂灯盏花素分散片和参比制剂灯盏花素片80 mg,采用LC-MS-MS法测定给药后不同时间异灯盏乙素的血药质量浓度。利用DAS软件计算药动学参数和进行统计分析,通过方差分析和双单侧t检验及90%置信区间法进行生物利用度评价。结果受试制剂与参比制剂中异灯盏乙素的ρmax为(75.81±23.24)、(62.17±17.82)μg.L-1,tmax为(6.50±1.34)、(7.78±1.52)h,AUC0→t为(454.1±194.7)、(403.9±133.3)μg.h.L-1,AUC0→∞为(460.1±199.8)、(410.3±137.1)μg.h.L-1。结论受试制剂ρmax比参比制剂大,疗效更高;受试制剂tmax比参比制剂小,起效更快;受试制剂对参比制剂的相对生物利用度(F,以AUC0-∞作为评价依据)为(116.5±43.5)%,灯盏花素分散片生物利用度较普通片高。Objective To evaluate the bioequivalence of breviscapine dispersible tablets and breviscapine tablets. Methods A randomized crossed-over study was conducted in 18 healthy volunteers. After a single dose of test and reference preparations （containing 80 mg breviscapine）, the plasma drug levels were determined by LC-MS-MS. The related pharmacokinetic parameters were calculated by DAS 2.0 and the bioequiavailability of the two preparations was evaluated by variance analysis and two one sided t tests by 90% confidence interval method. Results The main pharmacokinetic parameters of the test and reference preparations were as followS：ρmax was （75.81 ±23.24） and （62. 17 ± 17.82）μg-L^-1;tmax was （6.50± 1.34） and （7.78 ± 1.52）h;AUC0-t was （454. 1 ± 194. 7） and （403.9 ± 133.3） μg·h·L^-1. AUC0→∞ was （460. 1 ± 199.8） and （410. 3 ± 137. 1 ）μg·h·L^-1. The relative bioavailability of breviscapine dispersible tablets was （ 116. 5 ± 43.5 ）% as against the reference preparation. Conclusions The two formulations are non-bioequivalent.

关 键 词：灯盏花素 高效液相色谱串联质谱法 生物利用度 分散片 

分 类 号：R97[医药卫生—药品]