HPLC梯度洗脱法测定大鼠血清和结肠组织中瑞巴派特的浓度

目的:建立测定大鼠血清和结肠组织中瑞巴派特浓度的高效液相色谱(HPLC)法。方法:给大鼠口服含瑞巴派特4mg的壳聚糖胶囊、明胶胶囊和羧甲基纤维素钠溶液,分别于给药不同时间取血浆和结肠组织,用HPLC梯度洗脱法测定瑞巴派特浓度并计算Cmax。结果:瑞巴派特检测浓度线性范围为20～2 000ng·mL-1;血浆及组织样品平均提取回收率分别为88.4%、90.8%。3种制剂在结肠组织中的Cmax分别为5 963.9、2 190.7和1 185.8ng·g-1,在血浆中的Cmax分别为252.7、949.0和1 023.3ng·mL-1。结论:本方法可定量检测瑞巴派特在血液和结肠组织中的浓度,以用于其结肠定位释药制剂的开发。

Determination of Rebamipide in Rats' Plasma and Colonic Tissue by HPLC Gradient Elution

OBJECTIVE： To establish an HPLC method for the determination of rebamipide in rats＇ plasma and colonic tissue. METHODS： The rats were assigned to receive 4 mg rebamipide chitosan capsule or its gelatin capsule or its CMC-Na solution peros. Then the plasma and colon tissue samples were taken at different time for a determination of the concentration of rebamipide by HPLC gradient elution with C computed. RESULTS： The linear range for rebamipide was from 20--2 000 ng · mL^-1. The average extracting recoveries of rebamipide from the plasma and the colon were 88.4% and 90.8%, respectively. After oral administration of 4 mg rebamipide chitosan capsule or its gelatin capsule or its CMC - Na solution, the C of rebamipide in the colon tissue were 5 963.9, 2 190.7 and 1 185.8 ng· g^-1 respectively versus 252.7, 949.0 and 1 023.3 ng ·mL^-1 respectively in plasma. CONCLUSIONS： The established HPLC gradient elution in the study can be used to determine quantitatively the rebamipide level in plasma or colon tissue for the development of its colon specific delivery preparations.