解热药YL2000中小檗碱在正常和发热大鼠体内的药物动力学比较

Comparison of berberine between normal and febrile rats——pharmacokinetic study of antifebrile complex YL2000

目的 探讨解热药YL2 0 0 0中小檗碱在正常和发热大鼠体内的药物动力学。方法 采用高效液相技术分别测定正常大鼠和干酵母致发热大鼠血浆中小檗碱的含量 ,使用3P87软件处理小檗碱的时量数据 ,计算各药代动力学参数。结果 在正常和发热大鼠体内 ,小檗碱的达峰时间分别为(3 4± 0 3)h和 (0 3± 2 1)h(P <0 0 5 ) ,峰值血药浓度分别达 (0 15 4± 0 0 2 3)mg·L-1和 (0 2± 0 6 )mg·L-1,T1/ 2(ke)分别长达 (6± 3)h和 (6± 5 )h ,T1/ 2 (ka)分别为 (1 2±0 4 )h和 (0 1± 2 8)h ,CL/F(s)值分别为 (4 0± 1 9)mg·kg-1·h-1/ (mg·L-1)和 (6± 6 )mg·kg-1·h-1/ (mg·L-1) ,AUC( 0～T) 值分别为 (1 8± 0 3)mg·L-1·h-1和 (0 7± 0 5 )mg·L-1·h-1(P <0 0 5 )。结论 发热降低小檗碱在体内的AUC( 0～T) 。

AIM To explore pharmacokinetics of Berberine in YL2000 in normal and febrile rats. METHODS The levels of Berberine in plasma were measured through HPLC and secondary parameters were obtained by fitting the dose time data of Berberine making use of 3P87 programme. RESULTS In normal and febrile rats, the plasma concentration of Berberine was peaked at (3 4±0 3) h vs (0 3±2 1) h( P <0 05)with a level of (0 154±0 023) mg·L -1 vs (0 2±0 6) mg·L -1 , and the T 1/2 (ke), T 1/2 (ka) , CL/F(s) and AUC (0～T) of Berberine was (6±3) h vs (6±5) h, (1 2±0 4) h vs (0 1±2 8) h, (4 0±1 9) mg·kg -1 ·h -1 ·( mg·L -1 ) vs (6±6) mg·kg -1 ·h -1 (mg·L -1 ) and (1 8±0 3) mg·h -1 ·L -1 vs (0 7±0 5) mg·h -1 ·L -1 ( P <0 05), respectively. CONCLUSION AUC (0～T) of Berberine was cutted remarkably and its absorption was accelerated in febrile rats.