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目的研究孟鲁司特钠经家兔直肠吸收的程度及不同吸收促进剂对其吸收的影响。方法建立孟鲁司特钠在家兔体内血药浓度的HPLC测定法,测定孟鲁司特钠经家兔直肠给药及在不同吸收促进剂(吐温-80、癸酸钠、胆酸钠、月桂氮卓酮、月桂酸钠、L-精氨酸、EDTA-2Na及盐酸氯丙嗪)作用下的血药浓度,并以静脉给药为对照,对孟鲁司特钠的直肠吸收情况及吸收促进剂作用进行评价。结果孟鲁司特钠本身经直肠吸收极少,所用促进剂对其在肠道的吸收均有影响,并与其使用浓度有关,促进作用为10%吐温-80>1%癸酸钠>0.2%胆酸钠>4%月桂氮卓酮>3%月桂酸钠>1.5%L-精氨酸(P<0.05),2%盐酸氯丙嗪与1%EDTA-2Na效果相近,促进作用均较低。结论直肠不是孟鲁司特钠的良好吸收部位,利用吸收促进剂可促进其在直肠的吸收,10%吐温-80促吸收效果最好。
Objective To study the degree of rectal absorption of montelukast sodium by rabbits and the effect of different absorption enhancers on their absorption. Methods HPLC method was established to determine the plasma concentration of montelukast sodium in rabbits. The montelukast sodium was administered rectally in rabbits and tested in different absorption promoters (Tween-80, sodium caprate, sodium cholate , Laurocapram, sodium laurate, L-arginine, EDTA-2Na and chlorpromazine hydrochloride), and the intravenous administration as the control, the rectal absorption of montelukast sodium And the role of absorption enhancer evaluation. Results Montelukast sodium absorbed little through the rectum, and the accelerant used had an effect on its absorption in the intestine and was related to the concentration used. Its promotion effect was that 10% Tween-80> 1% sodium caprate> 0.2 % Sodium cholate> 4% laurodeazone> 3% sodium laurate> 1.5% L-arginine (P <0.05). The effect of 2% chlorpromazine and 1% EDTA-2Na was similar low. Conclusion The rectum is not a good absorption site of montelukast sodium. The absorption enhancer can promote the rectal absorption in the rectum. The best absorption rate is 10% Tween-80.