异硫氰酸烯丙酯在大鼠体内的生物利用度及组织分布  

Study on the bioavailability and tissue distribution of allyl isothiocyanate in rats

作　　者：曹银[1] 夏清荣[1] 梁俊[1] 汪电雷[2] 

机构地区：[1]合肥市第四人民医院药剂科,安徽合肥230022 [2]安徽中医药大学,安徽合肥230031

出　　处：《中国医院药学杂志》2014年第17期1442-1445,共4页Chinese Journal of Hospital Pharmacy

基　　金：国家自然科学基金资助项目(编号:81001592);教育部科学技术重点项目(编号:210101);安徽高校省级自然科学研究重点项目资助(编号:KJ2010A210)

摘　　要：目的:采用超高效液相色谱法(UPLC)研究异硫氰酸烯丙酯在大鼠体内的生物利用度和组织分布。方法:以SD大鼠为实验对象,经灌胃异硫氰酸烯丙酯20 mg·kg-1后,采用UPLC法测定大鼠体内不同时间点异硫氰酸烯丙酯浓度,估算体内生物利用度及静脉注射异硫氰酸烯丙酯20 mg·kg-1后在20,60,100 min时各主要组织药物浓度。结果:灌胃异硫氰酸烯丙酯20 mg·kg-1后,所得的血药浓度-时间数据,采用DAS2.1.1程序进行拟合及矩量法求算异硫氰酸烯丙酯在大鼠体内主要药动学参数,AUC0-t为(1 891.6±87.4)min·mg·L-1,t1/2为(107.5±5.4)min,Cmax为(4.87±0.37)mg·L-1,CL为(0.01±0.007 5)L·min-1·kg-1等,异硫氰酸烯丙酯在大鼠体内生物利用度高,其绝对生物利用度约为84.95%。静脉注射异硫氰酸烯丙酯20 mg·kg-1后,异硫氰酸烯丙酯在大鼠体内主要分布于肾、肺、肝、心、脾和胃等血流量较大的组织中。结论:异硫氰酸烯丙酯在大鼠体内具有较高的生物利用度,并在各主要组织中有广泛分布,UPLC法成功用于异硫氰酸烯丙酯在大鼠体内的生物利用度及组织分布研究。OBJECTIVE A UPLC method was developed to study the bioavailability and tissue distribution of allyl isothiocy anate in rats. METHODS After intragastrie administration of allyl isothiocyanate at doses of 20 mg, kg 1, the concertrations ofallyl isothiocyanate in rats plasma at different times were determined by using a UPLC method to estimate the bioavailability in wiwo. After intravenous injection of 20 rag. kg-1 allyl isothiocyanate, the concertrations of allyl isothiocyanate in rats major tissues at the times of 20 min,60 min and 100 min were determined. RF.SULTS After intragastric administration of 20 mg.kg-1 allyl isothiocyanate, the main pharmacokinetic parameters of allyl isothiocyanate were calculated by using DAS 2. 1.1 software and the moment method. The AUG ,tl/2 ,Cmax and CL were （1 891.6 ±87. 4） min-mg.L-1, （107. 5 ±5.4） min, （4. 87 ± 0. 37） mg·L-1 and （0. 01 ±0. 007 5） L·,min 1·kg-1, respectively, The absolute bioavailability of allyl isothiocyanate were 84. 95%. After intravenous injection of 20 mg, kg-1 allyl isothiocyanate, allyl isothiocyanate was maily distributed in kidney, lung, liver, heart, spleen and stomach. CONCLUSION The bioavailability of allyl isothiocyanate in rats is high and allyl isothioeyanate is widely distributed in the main tissue. The UPLC method was successfully developed to study on the bioavailability and tissue distribution of allyl isothiocyanate in rats.

关 键 词：异硫氰酸烯丙酯 超高效液相色谱法 绝对生物利用度 组织分布 

分 类 号：R927.2[医药卫生—药学]