脉络宁注射液酚酸类成分在大鼠体内的药代动力学研究(英文)  

Pharmacokinetics and excretion of phenolicacids from mailuoning injection in rats

作　　者：王玮[1] 王广基[1] 郝海平[1] 崔楠[1] 孙璇嵘[1] 

机构地区：[1]中国药科大学江苏省药物代谢动力学重点实验室

出　　处：《中国临床药理学与治疗学》2008年第7期776-781,共6页Chinese Journal of Clinical Pharmacology and Therapeutics

基　　金：National Natural Science Foundation of P.R. China ( No.30572228 ,30630076);the"eleventh-five years"supporting programs fromthe Ministry of Science and Technology of P.R.China (2006BAI08B04-05)

摘　　要：目的：研究脉络宁注射液中酚酸类成分在大鼠体内药代动力学规律。方法：大鼠尾静脉注射给予脉络宁注射液10 mL/kg,给药前及给药后不同时间采集血样或尿样,LC-MS法测定酚酸类成分浓度,血药浓度-时间数据和尿药排泄量-时间数据用DAS软件进行动力学分析。结果：绿原酸（CGA）、1 ,5-二咖啡酰奎宁酸（1 ,5-DCQA）、3 ,4-二咖啡酰奎宁酸（3 ,4-DCQA）、3 ,5-二咖啡酰奎宁酸（3 ,5-DCQA）和咖啡酸（CA）血药浓度迅速下降达峰,消除t1/2分别为0 .649、0 .334、0 .479、0 .486、0 .330 h,AUC0 -∞分别是（22 .522±2 .716）（CGA）、（0 .353±0 .062）（1 ,5-DCQA）、（3 .620±1 .246）（3 ,4-DCQA）、（5 .287±1 .627）（3 ,5-DCQA）和（2 .257±0 .360）（CA） mg.L-1.h。CGA、1 ,5-DCQA、3 ,4-DCQA、3 ,5-DCQA和CA在尿中0 -24 h累积排泄率分别为（122 .22±26 .49） %、（3 .30±1 .26） %、（0 .24±0 .11） %、（1 .93±0 .77） %和（18 .61±4 .99） %,尿排泄t1/2在1 -4 h。结论：脉络宁注射液中酚酸类成分在体内迅速被排泄出体外,CGA、1 ,5-DCQA、3 ,4-DCQA、3 ,5-DCQA和CA均可从尿排泄,但其中1 ,5-DCQA、3 ,4-DCQA、3 ,5-DC-QA和CA尿药排泄量较少,存在其他代谢途径。AIM： To study the pharmacokinetics of phenolic acids from Mailuoning injection in rats. METHODS： SD rats were given a single i.v. administration dose of Mailuoning injection 10 mL/kg, plasma and urine were collected before and after injection. Phenolic acid components in plasma and urine were measured by LC/MS. Pharrnacokinetic parameters were determined from the plasma concentration-time data and urinary excretion-time data with the DAS software package. RESULTS： After i.v. of Mailuoning injection, chlorogenic acid （CGA）, 1, 5-dicaffeylquinic acid （1,5-DCQA）, 3, 4-dicaffeylquinic acid （3, 4- DCQA）, 3, 5-dicaffeylquinic acid （3,5-DCQA） and caffeic acid （CA） were quickly excrectioned. The t1/2 of CGA, 1,5-DCQA, 3,4-DCQA, 3,5-DCQA and CA were 0.649, 0. 334, 0.479, 0.486 and 0. 330 h, respectively. AUC0-∞ were （22.522 ± 2.716）, （0.353 ±0.062）, （3.620± 1.246）, （5.287 ± 1.627） and （2.257 ± 0.360） mg·L^-1·h, respectively. After i.v. of Mailuoning injection, CGA, 1,5-DCQA, 3,4-DC- QA, 3, 5-DCQA and CA can all be detected in the urine. The amounts of CGA, 1,5-DCQA, 3,4-DCQA, 3,5-DCQA and CA excreted from urine during 0 - 24 h were （122.22±26.49）%, （3.30± 1.26）%, （0.24 ±0.11）%, （1.93 ± 0.77）% and （18.61 ±4.99） % of dose given in rats, respectively. CONCLUSION： After i.v. of Mailuoning injection, phenolic acids can be excreted quickly. Only a small quantity of 1,5-DCQA, 3,4-DCQA, 3,5-DCQA and CA were excreted from urine. 3,4-DCQA and 3,5-DC- QA may be metabolized into CGA in the rat plasma.

关 键 词：酚酸类 脉络宁注射液 药代动力学 高效液相色谱-质谱联用法 

分 类 号：R285.5[医药卫生—中药学] R969.1[医药卫生—中医学]