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《Journal of Changsha Medical University》 2015-01
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Absorption mechanism of SM-1:a procaspase-3-activated anti-tumor agent

TANG Jing;LUO Li-na;ZHANG Hai-long;ZHENG Zhi-nan;ZHANG Jie;LI Su;HE Hua;DING Jin-song;  
Objective:Aim To study absorption characteristics of SM-1,a novel anti- tumor agent,to provide a research basis for the druggability evaluation of SM-1 and formulation design. Methods:Caco-2 cell monolayer model and in situ singlepass intestinal perfusion rat model were used to study the absorption characteristics of SM-1,and the absorption of SM-1 in vivo was evaluated through absolute bioavailability study in rats. Results:The results of cell monolayer model showed that cumulative absorption and efflux of SM-1 increased linearly with concentration(10~40mg·L-1). There were no significant differences in Papp with different concentrations(P 0.05). SM-1 was absorbed mainly through passive diffusion. The intestinal perfusion results showed that Ka and Peff of SM-1 had no significant differences(P0.05),when the concentrations ranged from 25 to 100 mg·L-1. SM-1 entered the systemic circulation mainly via on passive diffusion,indicating it is a compound with high permeability. The absorption of SM-1 in duodenum was superior toother intestinal segments(P0.05),there were no significant differences in the jejunum,ileum and colon(P0.05). The absolute bioavailability of SM-1 in rats was 29.3%. Conclusion:The membrane permeability of SM-1 is high and it can be absorbed by intestine well. The absorption mechanism of SM-1 is passive diffusion,and it possibly escapes from the efflux transporter protein. The absolute bioavailability of SM-1 in rats is low.
【Fund】: 国家“十二五”重大科技专项(No2012ZX09103101-051)
【CateGory Index】: R966
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