摘要
目的 用唾液法和血液法比较得理多 (Tegretol)在人体内的药代动力学特征 ,动态观察唾液和血液药物浓度的相关性 .方法 以 HPL C法测定 8名健康志愿者口服 2 0 0 mgTegretol后的唾液和血液浓度 ,分别计算其药代动力学参数并进行统计学比较 .结果 唾液和血液中的 Tegretol药 -时曲线可用一室开放模型拟合 ,其峰浓度 (Cmax)分别为 (1.45± 0 .2 1)、(4 .2 1± 0 .85 ) mg· L- 1 ;达峰时间 (Tmax)分别为(6.2 5± 4.88)、(7.75± 1.75 ) h,吸收半衰期 (T1 / 2 ka)为 (1.45± 1.2 1)、(1.69± 1.18) h,消除半衰期 (T1 / 2 ke)为 (5 2 .43±19.90 )、(5 1.5 8± 9.5 7) h,曲线下面积 AU C为 (135 .91±16.81)、(34 1.86± 48.10 ) h· mg· L- 1 ,清除率 (CL /F)为(0 .0 15± 0 .0 0 5 )、(0 .0 13± 0 .0 0 2 ) (mg· kg- 1 ) /(mg· L- 1 ) ,唾液和血液药动学参数中的 Tmax,T1 / 2 ka,T1 / 2 ke和 CL /F无显著性差异 (P>0 .0 5 ) .Tegretol的唾液 /血液浓度比值 (S/P)平均为 0 .367± 0 .0 5 6,吸收相略高于消除相 ;服药 3～ 144 h的 Tegretol唾液和血液浓度的相关系数 (r)平均为 0 .90 5 .结论 Tegretol的唾液和血液浓度在用药 3～ 144 h具有较高的相关性 ,这种相关性存在动态的平行关系 ;除
AIM To compare the saliva and blood in pharmacokinetics of Tegretol and monitor the correlationship of their concentrations between saliva and serum dynamically. METHODS Saliva and serum concentrations were measured by HPLC in eight healthy volunteers with roal dose of 200 mg Tegretol, their pharmacokinetic parameters being calculated respectively. RESULTS The saliva and serum concentration time curves appeared to fit the one compartment open model. The pharmacokinetic parameters showed: C max were (1.45±0.21) and (4.21±0.85) mg·L -1 ; T max were (6.25± 4.88) and (7.75±1.75) h, T 1/2ka were(1.45±1.21) and (1.69±1.18) h, T 1/2ke were(52.43±19.90) and (51.58± 9.57) h, AUC were (135.91±16.81) and (341.86±48.10) h·mg·L -1 , CL/F were(0.015±0.005) and (0.013± 0.002) (mg·kg -1 )/(mg·L -1 ) respectively. The differences of T max , T 1/2ka , T 1/2ke and CL/F between saliva and serum were no statistic significance ( P >0.05). The ratio of saliva concentration to serum was 0.367±0.056, higher in absorption phase than in elimination phase. During 3~144 h postdose , the mean correlation coefficient was 0.905. CONCLUSION High correlationship may exist between the concentrations of Tegretol in saliva and serum which is dynamic and parallel. Saliva and blood pharmacokineics of Tegretol is similar except Cmax and AUC, so it is feasible to make saliva as a blood substituent which is also fit for the pharmacokinetics study and clinical TDM of Tegretol.
出处
《第四军医大学学报》
北大核心
2001年第16期1508-1511,共4页
Journal of the Fourth Military Medical University
