目的 建立反相高效液相色譜(RP-HPLC)法測定大鼠糞便和尿液中2,5'-二溴-4,5,2'-三羥基二苯甲酮(LM49),并研究大鼠ig 給予LM49 后在糞便和尿液中的排泄特征。方法 采用甲醇提取生物樣品中的LM49,Diamonsil C₁₈(250 mm×4.6 mm,5 μm)色譜柱,甲醇/乙腈/水(磷酸調(diào)pH 至3.0)(68:5:27)為流動相,體積流量0.8 mL/min,檢測波長261 nm,柱溫25 ℃。雄性SD 大鼠單次ig 給予100 mg/kg 的LM49 后,收集0～12、13～24、25～36、37～48 h 的糞便和尿液,采用RP-HPLC 法測定LM49,計算排泄量、排泄率、累積排泄率。結(jié)果 單次口服給予大鼠100 mg/kg 的LM49 后,48 h 內(nèi)LM49 在糞便中的排泄主要集中在13～36 h,占整個排泄量的77.4%,累積排泄率為13.9%;其尿液中0～12 h 的累積排泄率為0.05%,13～48 h 未檢測到LM49。結(jié)論 LM49 口服吸收不完全,有較高的糞便排泄率,原型尿排泄甚少,推測可能被代謝分解或在組織器官中蓄積。

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.

國家高技術(shù)研究發(fā)展計劃( “863”計劃) (2013AA092903); 國家自然科學(xué)基金(81473100);山西省自然科學(xué)基金(2013011060-2);山西醫(yī)科大學(xué)科技創(chuàng)新基金(01201116);山西醫(yī)科大學(xué)博士啟動基金(B03201213)