复方丹参滴丸对人肝脏药物代谢酶CYP1A2活性的影响

目的:研究复方丹参滴丸对人肝脏药物代谢酶CYP1A2活性的影响,指导临床合理用药。方法:采用反相高效液相色谱法测定服用复方丹参滴丸前、后人尿液内咖啡因4种主要代谢产物的相对含量;采用(AFMU+1X+1U)/17U比率法评价人肝脏药物代谢酶CYP1A2活性的变化。结果:受试者用药前CYP1A2的平均活性为4·20±1·54,服用复方丹参滴丸14d后CYP1A2的平均活性为4·26±1·95,用药28d后CYP1A2的平均活性为4·35±1·26,二者分别比用药前升高1·42%和3·57%,但无统计学差异。结论:服用治疗剂量的复方丹参滴丸对人肝脏药物代谢酶CYP1A2的活性无明显影响,不会影响与之合用的需经CYP1A2代谢药物的疗效。

Effect of Compound Danshen Dripping Pills on Cytochrome CYP1A2 Activity

OBJECTIVE: To investigate the effect of Compound danshen dripping pills on cytochrome CYP1A2 activity for reference of clinical rational drug use. METHODS: The contents of four major metabolites of Caffeine, i.e. 5-acetylamino-6-formylamino-3-methyluracil(AFMU),1-methylxanthine(1X), 1-methyluric acid(1U) and 1, 7-dimethyluricacid (17U) in the urine before and after oral administration of Compound danshen dripping pills were determined by RP-HPLC. The activity of cytochrome CYP1A2 was derived from the ratio of (AFMU+1X+1U)/17U. RESULTS: The average activity of CYP1A2 was 4.20±1.54 before medication, which stood at 4.26±1.95 at 14 days and 4.35±1.26 at 28 days after medication, up 1.42% and 3.57%, respectively, yet there was no significant difference after medication as compared with before medication. CONCLUSION: No significant difference was noted on CYP1A2 activity after oral medication of Compound danshen dripping pills, nor does it modify the efficacy of the concurrent drugs that metabolized by CYP1A2.