不同吸收促进剂对孟鲁司特钠家兔直肠吸收的促进作用

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.

Effects of different absorption enhancers on intestinal absorption of montelukast sodium in rabbits

Objective To investigate the rectal absorption profile of montelukast sodium in the rabbits and determine the effects of different absorption enhancers on the absorption.Methods A method of high-performance liquid chromatography (HPLC) was established to detect the blood concentrations of montelukast sodium in the rabbits.The blood concentration was measured in the rabbits after rectal administration in the presences of different absorption enhancers,including Tween-80,sodium caprate,sodium cholate,laurocapram,laurate sodium,L-arginine,chlorpromazine hydrochloride and EDTA-2Na.With he blood concentration after venous administration as control,the rectal absorption profile of montelukast sodium and the effects of different absorption enhancers were evaluated.Results Montelukast sodium was minimally absorbed in the rectum.All the absorption enhancers exerted promoting effects on its intestinal absorption in a concentration-dependent manner.The absorption enhancing effects of the absorption enhancers were as following order,10％ Tween-80 ＞ 1％ sodium caprate ＞ 0.2％ sodium cholate ＞ 4％ laurocapram ＞ 3％ laurate sodium ＞ 1.5％ L-arginine (P ＜ 0.05).The effect of 2％ chlorpromazine hydrochloride and 1％EDTA-2Na was similar,with mild effect.Conclusion The rectum is not a favorable absorption site for montelukast sodium.Absorption enhancers can promote its rectal absorption.10％ Tween-80 has the best enhancing effect on its absorption.