[1]曹娅琪,王章阳,戴青.不同吸收促进剂对孟鲁司特钠家兔直肠吸收的促进作用[J].第三军医大学学报,2017,39(09):897-903.
 Cao Yaqi,Wang Zhangyang,Dai Qing.Effects of different absorption enhancers on intestinal absorption of montelukast sodium in rabbits[J].J Third Mil Med Univ,2017,39(09):897-903.
点击复制

不同吸收促进剂对孟鲁司特钠家兔直肠吸收的促进作用(/HTML )
分享到:

《第三军医大学学报》[ISSN:1000-5404/CN:51-1095/R]

卷:
39卷
期数:
2017年第09期
页码:
897-903
栏目:
基础医学
出版日期:
2017-05-15

文章信息/Info

Title:
Effects of different absorption enhancers on intestinal absorption of montelukast sodium in rabbits
作者:
曹娅琪王章阳戴青
第三军医大学西南医院药剂科
Author(s):
Cao Yaqi Wang Zhangyang Dai Qing

Department of Pharmacy, Southwest Hospital, Third Military Medical University, Chongqing, 400038, China

关键词:
孟鲁司特钠直肠吸收吸收促进剂HPLC
Keywords:
montelukast sodium rectal absorption absorption enhancers highperformance liquid chromatography
分类号:
R322.45; R969.1; R974.3
文献标志码:
A
摘要:

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。

Abstract:

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.

参考文献/References:

[1]林琳,马忠英,乔逸,等.孟鲁司特钠分散片的人体生物等效性研究[J].解放军药学学报,2011,27(4);334-336.DOI: 10.3969/j.issn.10089926.2011.04.016.
Lin L,Ma Z Y,Qiao Y,et al.Bioequivalence of montelukast dispersible tablets in healthy volunteers[J].Pharm J Chin PLA,2011,27(4):334-336. DOI: 10.3969/j.issn.1008-9926. 2011.04.016.
[2]Junginger H E. Excipients as Absorption Enhancers[M]//Krishna R, Yu L. Biopharmaceutics Applications in Drug Development.New York:Springer US, 2008:139-174.DOI: 10.1007/9780387-72379-2.
[3]Sharma P, Varma M V, Chawla H P, et al. Absorption enhancement, mechanistic and toxicity studies of medium chain fatty acids, cyclodextrins and bile salts as peroral absorption enhancers[J].Farmaco,2005,60(11/12):884-893. DOI:10.1016/j.farmac.2005.08.008.
[4]Rege B D,Yu L X,Hussain A S,et al.Effect of common excipients on Caco-2 transport of lowpermeability drugs[J].J Pharm Sci,2001,90(11):1776-1786.
[5]李文淑,刘树红,孙斌,等.孟鲁斯特钠咀嚼片在健康人体内药动学和生物等效性[J].现代生物医学进展,2012,12(2):337-340.DOI: 10.13241/j.cnki.pmb. 2012.02.061.
Li W S,Liu S H,Sun B,et al.Study on bioavailability of montelukast sodium chewable tablets[J].Progress in Modern Biomedicine,2012,12(2):337-340. DOI: 10.13241/j.cnki.pmb.2012.02.061.
[6]Alsarra I,Khalil N Y,Sultan M,et al.Spectrofluorometric determination of momtelukast in dosage forms and spiked human plasma[J].Pharmazie,2005,60(11):823-826.
[7]杨振华,偶志红,徐丹丹.不同吸收促进剂对氯唑西林钠栓溶出度和家兔血药浓度的比较[J].中国医院药学杂志,1998,18(1):5-8.DOI: 10.3321/j.issn:1001-5213. 1998.01.002.
Yang Z H, Ou Z H, Xu D D. Different absorption promoter of cloxacillin sodium suppository dissolution and the comparison of rabbit plasma concentration[J].Chinese Journal of Hospital Pharmacy,1998,18(1):5-8.DOI:10.3321/j.issn:1001-5213.1998.01.002.
[8]侯雪梅,李国栋,李卫华.化学促渗剂及其机理的探讨[J].上海医药,2008,29(5):231-235.DOI: 10.3969/j.issn.1006-1533.2008.05.016.
Hou X M, Li G D, Li W H. The discussion of chemical enhancers mechanism[J].Shanghai Medical & Pharma J,2008,29(5):231-235.DOI: 10.3969/j.issn.1006-1533. 2008.05.016.
[9]李国锋,黄蓓蓓,腊蕾,等.几种表面活性剂对Pgp底物罗丹明123经肠黏膜透过性的影响[J].中国药学杂志,2008,43(16):1252-1256.DOI: 10.3321/j.issn:1001-2494. 2008.16.012.
Li G F,Huang B B,La L,et al.Effect of some surfactants on permeabilities of rhodamine 123 , a Pgp substrate through the rat intestinal membranes in vitro[J].Chin Pharm,2008,43(16):1252-1256. DOI: 10.3321/j.issn:1001-2494.2008.16.012.
[10]张明令,张海燕,丛英,等.吐温-80在水溶液中的表面活性研究[J].中成药,2010,32(1):55-58.DOI: 10.3969/j.issn.1001-1528.2010.01.016.
Zhang M L,Zhang H Y,Cong Y,et al.Research on Tween-80 surfactant in aqueous solution[J].Chin Trad Pat Med,2010,32(1):55-58.DOI:10.3969/j.issn.1001-1528.2010.01.016.
[11]Lindmark T, Kimura Y, Artursson P. A bsorption enhancement through intracellular regulation of tight junction permeability by medium chain fatty acids in Caco-2 cells [J].J Pharmacol Exp Ther,1998,284(1):362-369.
[12]Coyne C B,Kelly M M,Boucher R C,et al.Enhanced epithelial gene transfer by modulation of tight junctions with sodium caprate[J].Am J Respir Cell Mol Biol,2000,23(5):602-609.DOI:10.1165/ajrcmb.23.5.4164.
[13]Suqibayashi K,Onuki Y,Takayama K.Displacement of tight junction proteins from detergentresistant membrane domains by treatment with sodium caprate[J].Eur J Pharm Sci,2009,36(2/3):246-253.DOI:10.1016/j.ejps.2008.09.011.
[14]Imai T,Sakai M,Ohtake H,et al.Absorption-enhancing effect of glycyrrhizin induced in the presence of capric acid[J]. Int J Pharm,2005,294(1/2):11-21.DOI: 10.1016/j.ijpharm. 2004.12.029.
[15]Miyake M, Kamada N, Oka Y,et al.Development of suppository formulation safely improving rectal absorption of rebamipide, a poorly absorbable drug, by utilizing sodium laurate and taurine[J].J Control Release,2004,99(1):63-71.DOI:10.1016/j.jconrel.2004.06.007.
[16]Emori H,Yokohama S,Nishihata T.Small intestinal absorption of bropirimine in rats and effect of bile salt on the absorption[J].J Pharm Pharmacol,1995,47(6):487-492.
[17]Mukaizawa F, Taniguchi K, Miyake M,et al.Novel oral absorption system containing polyamines and bile salts enhances drug transport via both transcellular and paracellular pathways across Caco-2 cell monolayers[J].Int J Pharm,2009, 367(1/2):103-108.DOI:10.1016/j.ijpharm. 2008.09.027.
[18]黄波,陈畅.一氧化氮的功能及其作用机制(Ⅰ)——性质与功能[J].生物物理学报,2012,28(3):173-184.DOI: 10.3724/SP.J.1260.2012.20007.
Huang B,Chen C.Function and mechanism of nitric oxide(Ⅰ)character and function[J].ACTA BIOPHYSICA SINICA,2012,28(3):173-184.DOI: 10.3724/SP.J.1260.2012.20007.
[19]Aungst B J.Intestinal permeation enhancers[J].J Pharm Sci,2000,89(4):429-442.DOI:10.1002/(SICI)15206017(200004)89:4<429::AID-JPS1>3.0.CO;2J.
[20]Wisniewska A,Wolnicka-Glubisz A.ESR studies on the effect of cho1esterol on chlorpromazine interaction with saturated and unsaturated liposome membranes[J].Biophys Chem,2004,111(1):43-52.DOI: 10.1016/j.bpc.2004.04.001.
[21]杨丹,王章阳,陈勇川,等.盐酸氯丙嗪促进药物直肠吸收机制研究[J].第三军医大学学报,2009,31(10):926-930.DOI:10.3321/j.issn:1000-5404.2009.10.014.
Yang D,Wang Z Y,Chen Y C,et al. In vitro mechanisms of drug absorption in rectum promoted by chlorpromazine hydrochloride[J].J Third Mil Med Univ,2009,31(10):926-930.DOI:10.3321/j.issn:10005404.2009.10.014.

相似文献/References:

[1]杨丹,王章阳,陈勇川,等.盐酸氯丙嗪促进药物直肠吸收机制研究[J].第三军医大学学报,2009,31(10):926.
 YANG Dan,WANG Zhang-yang,CHEN Yong-chuan,et al.In vitro mechanisms of drug absorption in rectum promoted by chlorpromazine hydrochloride[J].J Third Mil Med Univ,2009,31(09):926.

更新日期/Last Update: 2017-05-08