摘要
目的通过对健康志愿者静脉滴注3个不同剂量异甘草酸镁注射液后的药代动力学研究,探讨异甘草酸镁注射液在人体内的药代动力学特征.方法 9名健康志愿者单剂量静脉滴注异甘草酸镁注射液(100, 200及300 mg),在设计的时间点取静脉血,采用高效液相色谱-紫外检测法测定血浆药物浓度.结果受试者血药浓度-时间数据用3P87软件拟合,符合一级消除的二房室模型,主要药动学参数如下:Cmax(实测值)分别为(28.79±3.54),(67.56±8.84)及(99.28±17.57) mg·L-1;T(1)/(2)α分别为(1.72±0.27),(1.46±0.35)及(1.13±0.33) h;T(1)/(2)β分别为(23.10±3.30),(23.95±4.72)及(24.25±4.12) h; Vd分别为(3.332±0.471),(2.921±0.382)及(2.921±0.622) L; CL分别为(0.209±0.041),(0.186±0.048)及(0.166±0.039) L·h-1;k10分别为(0.063±0.012),(0.064±0.016)及(0.057±0.009) h-1 ;AUC0-72(以梯形法计算)分别为(448.68±75.06),(1015.29±225.14)及(1688.42±367.44) mg·h·L-1.结论健康志愿者静脉滴注异甘草酸镁注射液(100~300 mg )后的体内过程呈线性特征.本品与甘草酸及其它甘草酸盐类药物相比,消除速度较慢,有利于慢性肝炎的治疗.
Aim To investigate the pharmacokinetics of intravenous injection of magnesium isoglycyrrhizinate in single dose in Chinese healthy volunteers. Methods 9 healthy volunteers received magnesium isoglycyrrhizinate injections in single dose of 100,200,300 mg respectively. The concentrations of magnesium isoglycyrrhizinate in plasma at different time were assayed with HPLC-UV method. The pharmacokinetic parameters of magnesium isoglycyrrhizinate injections were calculated with program 3P87. Results It was found that the plasma concentration-time curves of the preparetion fitted two-compartment model. The main pharmaeokinetie parameters were as follows: C were (28.79±3.54), (67.56±8.84) and (99.28± 17.57) mg· L^-1 ;T1/2α were (1.72±0.27), (1.46±0.35) and (1.13 ±0.33) h;T1/2β were (23.10 ± 3.30), (23.95 ± 4.72) and (24.25 ±4. 12) h;Vd were (3.332±0.471 ), (2.921±0.382) and (2.921 ±0.622) L; CL were (0.209±0.041 ), (0. 186±0.048) and (0. 166 ±0.039) L · h^-1;klo were (0.063±0.012), (0.064±0.016) and (0. 057±0. 009 ) h^-1 ; AUC0.72 were ( 448.68 ± 75.06), (1015.29 ± 225. 14) and ( 1688.42 ±367.44 ) mg · h · L^-1. Conclusion The pharmacokinetics of the drug in the dosage range of 100 - 300 mg in human body approximately fit linear dynamic features. Compared with glycyrrhizic acid and other glycyrrhizinate salts, magnesium isoglycyrrhizinate is eliminated more slowly. This is beneficial to the treatment of chronic hepatitis.
出处
《中国药理学通报》
CAS
CSCD
北大核心
2005年第11期1348-1351,共4页
Chinese Pharmacological Bulletin
基金
国家十五重大科技专项资助课题(No2003AA2Z3161)