摘要
目的观察联合应用盐酸小檗碱(黄连素,berberine hydrochloride,BBR)对心脏移植受者服用环孢素A(Cyclosporine,CsA)药代动力学的影响。方法选取心脏移植长期存活(>1年)受者15例,年龄18～65岁,体重45～78 kg,无肝肾功能异常。受者在原有免疫抑制方案基础上服用BBR 0.3 g/d(分3次服用),在加药前1天和加药后第14天的不同时间点各检测全血CsA血药浓度。采血时间点分别为服药前(0 h)和服药后0.25 h,期函数0.5、0.75、1.0、1.5、2.0、3.0、4.0、6.0、8.0、10.0、12.0(h)。观察合用BBR前后CsA浓度、药代动力学参数和生化指标[血清总胆红素(TBIL)、谷丙转氨酶(ALT)、血浆总蛋白(TP)、尿素氮(BUN)、肌酐(Cr)]的变化。结果在合用BBR后吸收相(0～0.75 h)及消除相(3～12 h)CsA全血浓度均较合用前明显增高(P<0.05)。合用BBR后血药浓度-时间曲线下面积(AUC_(0～12h))平均增加(33.49±20.72)%,达峰时间(t_(max))延迟(均P<0.05)。合用BBR前后TBIL、ALT、TP、BUN、Cr比较,差异无统计学意义(P>0.05)。结论联合应用BBR与CsA后,可以使CsA的达峰时间(t_(max))延迟,半衰期(t_(1/2))延长,清除率减少,AUC增大,生物利用度增加;减少CsA的服用剂量,且无明显不良反应。
Objective To observe the effect of berberine hydrochloride （BBR） on the pharmacokinetics of Cyclosporine A（CsA） in heart transplant recipients. Methods Totally 15 heart transplant recipients（more than 1 years）with long-term survival were recruited, they were aged between 18 to 65 years old, weighed 45 -78 kg, without abnormal liver and kidney function. The recipients took BBR 0.3 g/d （3 times a day）, based on the original immuno suppression program. The blood concentration of CsA were detected at different time points in 1 d before and 14 d after taking the medicine. The time points for blood sampling were before taking medicine （0 h） and 0.25 h after taking medicine, and the functions were 0.5, 0.75, 1.0, 1.5,2.0, 3.0,4.0,6.0, 8.0, 10.0 and 12.0 （h）.The CsA concentration, main pharmacokinetic parameters and biochemical indexes E total bilirubin （ TB IL）, alanine transam inase （ALT）, total plas m a protein （TP） ,blood urea nitrogen （ BUN ）, creatinine （Cr） 1 BBR were observed before and after applying. Results The total blood concentration of CsA was significantly higher than before applying BBR in the absorption phase（0 -0.75 h） and the elimination phase （3 - 12 h） （P 〈0.05）. It was found that AUCo 12 h increased （33.49 ± 20.72）% and Tmax delayed after applying BBR（ail P 〈0.05）in the pharmacokinetic parameters. There was no statistical difference in biochemical indexes（TBIL,ALT,TP,BUN,Cr）after applying BBR. Conclusion The combined application of BBR and CsA could delay the CsA T prolong t1/2,decrease the clearance rate, increase AUC and the bioavailability,reduce the dose of CsA,no obvious adverse reaction,
出处
《中国中西医结合杂志》
CAS
CSCD
北大核心
2018年第3期306-309,共4页
Chinese Journal of Integrated Traditional and Western Medicine
基金
福建省卫生厅青年基金资助项目(No.2012-01-19)
关键词
盐酸小檗碱(黄连素)
心脏移植
环孢素A
血药浓度
berberine hydrochloride
heart transplantation
cyclosporin A
plasma concentration
