Received:28 November 2016,
Published:15 May 2017
移动端阅览
Yaqi Cao, Zhangyang Wang, Qing Dai. Effects of different absorption enhancers on intestinal absorption of montelukast sodium in rabbits[J]. Journal of Third Military Medical University, 2017, 39(9): 897-903.
Yaqi Cao, Zhangyang Wang, Qing Dai. Effects of different absorption enhancers on intestinal absorption of montelukast sodium in rabbits[J]. Journal of Third Military Medical University, 2017, 39(9): 897-903. DOI: 10.16016/j.1000-5404.201611102.
Objective
2
To investigate the rectal absorption profile of montelukast sodium in the rabbits and determine the effects of different absorption enhancers on the absorption.
Methods
2
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
2
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
2
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.
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