盐酸黄连素对环孢素A增效作用的药物动力学研究  

Pharmacokinetics of Synergistic Effect of Coadministration of Cyclosporin A with Berberine Hydrocholride in Renal Transplantation Recipients

作　　者：李罄[1] 吴笑春[1] 辛华雯[1] 余爱荣[1] 冷金华[1] 仲明远[1] 朱敏[1] 唐礼功[1] 谢森[1] 刘幼英[1] 

机构地区：[1]广州军区武汉总医院,武汉430070

出　　处：《华南国防医学杂志》2002年第1期12-15,共4页Military Medical Journal of South China

摘　　要：目的:研究盐酸黄连素对肾移植受者使用环孢素A增效作用的体内动力学过程。方法:选择肾移植术后1个月以内、连续服用环孢素A2周、肝肾功能稳定的患者6名,环孢素A剂量6mg·kg^(-1)d^(-1),用FPIA方法(单抗)检测合用黄连素前后各时间点环孢素A全血浓度。结果:单服环孢素A的主要药动学参数分别为T_(max)(h):0.93±0.47,C_(max)(μg·L^(-1)):1176.7±405.88,C_(min)(μg·L^(-1)):173.95±78.71,T_(1/2)(h):2.62±1.00,AUC(μg·L^(-1))·h^(-1):5237.7±1776.5,CL/F(L·h^(-1)):35±15;与黄连素合用的主要药动学参数为T_(max)(h):2.26±1.15,C_(max)(μg·L^(-1)):919.17±330.87,C_(min)(μg·L^(-1)):319.22±163.45,T_(1/2)(h):5.33±2.60,AUC(μg·L^(-1))·h^(-1):9213.17±3802.6,CL/F(L·h^(-1)):22±13。结论:盐酸黄连素与环孢素A合用可使后者T_(max)滞后,t_(1/2)延长,清除率减少,AUC增大,生物利用度增加;对肝肾功能没有影响。Objective To study the pharmacokinetics of cyclosporin A (CsA) with or without combination of berberine hy-drochloride (Ber) in renal transplantation recipients. Methods Our study included 6 patients treated with CsA at 6 mg·kg-1d-1 for two weeks within one month after the renal transplantation. CsA content in the blood was determined by fluorescence polarization im-munoassay before and after coadministration of Ber in the patients. Results The pharmacokinetic parameters of CsA before the coadministration of Ber were T11/2, (2.62 ±1.00)h; Tmax(0.93±0.47)h; Cmax(11.76.7±405.88)μg·L-1; Cmin,/173.95?8.71)μg·L-1; AUC, (5237.7±1776.5)μg-L-1·h-1; CL/F, (35±15) L·h-1. The pharmacokinetic parameters of CsA after the coadministration of Ber were T1/2, (5.33±2.60)h; Tmax, (2.26±1.15)h; Cmax, (919.17 ±330.87) μg·L-1; Cmin, (319.22±163.45) μg ·L-1; AUC, (9213.7± 3802.6) μg·h· L-1; CL/F, (22 ±13) L·h-1. Conclusion Ber could significandy elevate the blood concentration of CsA in the renal transplantation recipients. After the coadministration of Ber, Tmax, of CsA was delayed and CL/F was decreased while T1/2 as well as AUC was increased. Two drugs coadministration had no effects on liver and renal functions.

关 键 词：环孢素A 盐酸黄连素 肾移植受者 药物动力学 

分 类 号：R[医药卫生] 969.2