[关键词]
[摘要]
目的 建立反相高效液相色谱(RP-HPLC)法测定大鼠粪便和尿液中2,5'-二溴-4,5,2'-三羟基二苯甲酮(LM49),并研究大鼠ig 给予LM49 后在粪便和尿液中的排泄特征。方法 采用甲醇提取生物样品中的LM49,Diamonsil C18(250 mm×4.6 mm,5 μm)色谱柱,甲醇/乙腈/水(磷酸调pH 至3.0)(68:5:27)为流动相,体积流量0.8 mL/min,检测波长261 nm,柱温25 ℃。雄性SD 大鼠单次ig 给予100 mg/kg 的LM49 后,收集0~12、13~24、25~36、37~48 h 的粪便和尿液,采用RP-HPLC 法测定LM49,计算排泄量、排泄率、累积排泄率。结果 单次口服给予大鼠100 mg/kg 的LM49 后,48 h 内LM49 在粪便中的排泄主要集中在13~36 h,占整个排泄量的77.4%,累积排泄率为13.9%;其尿液中0~12 h 的累积排泄率为0.05%,13~48 h 未检测到LM49。结论 LM49 口服吸收不完全,有较高的粪便排泄率,原型尿排泄甚少,推测可能被代谢分解或在组织器官中蓄积。
[Key word]
[Abstract]
Objective To establish an RP-HPLC method to determine the content of 2,5'-dibromo-4,5,2'-trihydroxydiphenylmethanone (LM49) in feces and urine of rats, and to study the excretion of LM49 after oral administration to rats. Methods LM49 was extracted from biological samples with methanol as extracting reagent, and separated on a Diamonsil C18 column (250 mm × 4.6 mm, 5 μm) with the mobile phase of methanol-acetonitrile-water (68:5:27, pH was adjusted to 3.0 with phosphoric acid) at a flow rate of 0.8 mL/min at 25 ℃, and the detection wavelength was 261nm. After the oral administration with LM49 (100 mg/kg) to male SD rats, the feces and urine were collected in 0—12 h, 13—24 h, 25—36 h, and 37—48 h. The concentration of LM49 in excretion samples was detected by RP-HPLC. And the content of excretion, excretion ratio and accumulative excretion ratio of LM49 were determined. Results After the oral administration with LM49 (100 mg/kg) to male SD rats, the excretion of LM49 in the feces was mainly accumulated in 13—36 h, the content of which attained to 77.4 % of the total excretion in the feces, and the accumulative excretion ratio of LM49 was 13.9 % within 48 h. The accumulative excretion ratio of LM49 was 0.05 % in the urine within 12 h, and LM49 was not detected in the urine after 13 h. Conclusion The oral absorption of LM49 is not complete with higher excretion rate in the feces and rare LM49 in the urine, which implies that LM49 is metabolized or stored in tissues and organs.
[中图分类号]
[基金项目]
国家高技术研究发展计划( “863”计划) (2013AA092903); 国家自然科学基金(81473100);山西省自然科学基金(2013011060-2);山西医科大学科技创新基金(01201116);山西医科大学博士启动基金(B03201213)