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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 in vivo kinetics of the synergistic effect of berberine hydrochloride on cyclosporine A in renal transplant recipients. Methods: Six months after cyclophosphamide treatment were given within 1 month after renal transplantation, 6 patients with stable liver and kidney function were treated with cyclosporine A for 6 weeks. The dose of cyclosporin A was 6 mg · kg -1 d -1. The FPIA method (monoclonal antibody) was used to detect the concentration of cyclosporine A whole blood before and after the administration of berberine. Results: The main pharmacokinetic parameters of cyclosporin A were: 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, respectively. The main pharmacokinetic parameters in combination with berberine were T max (h): 2.26 ± 1.15, · 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) L -1 h -1: 9213.17 ± 3802.6, CL / F (L · h -1): 22 ± 13. CONCLUSION: The combination of berberine and cyclosporine A can delay the T_ (max) and prolong the t_ (1/2) of the latter, with a decrease in clearance rate, an increase in AUC and an increase in bioavailability. There is no effect on liver and kidney function.