Absorption mechanism of silybin in human intestinal Caco-2 cells

被引：0
|
作者：
Hu Lin [1 ]
Tong Huan [1 ]
Ding Ru [1 ]
Wang Zhanbo [2 ]
You Linjun [2 ]
Yang Jin [1 ]
机构：
[1] China Pharmaceut Univ, Ctr Drug Metab & Pharmacokinet, Nanjing 210009, Jiangsu, Peoples R China
[2] China Pharmaceut Univ, Ctr New Drug Safety & Evaluat & Res, Nanjing 211198, Jiangsu, Peoples R China
来源：
JOURNAL OF CHINA PHARMACEUTICAL UNIVERSITY | 2018年 / 49卷 / 02期
关键词：
Caco-2; monolayer; Permeability; Silybin; Silybin-IV-meglumine;
D O I：
10.11665/j.issn.1000-5048.20180210
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
The aim of this paper was to investigate the absorption mechanism of silybin (SLB) in Caco-2 cells. Concentrations of samples in the study were determined by developing LC/MS/MS method of SLB, propranolol and atenolol in HBSS buffer to calculate apparent permeability coefficient (app ) . When Caco-2 cells were cultured to the 21st day, the TEER were above 350 Omega center dot cm(2) . The P-app of Lucifer yellow was far less than 1 x 10(-7) cm/s. As the positive control drugs, The P-app of atenolol and propranolol were similar to those reported in the literature, indicating that the Caco-2 monolayer model was successfully established in this experiment. The P(app )APBL) of SLB at 5, 20, and 50 mu g/mL were all more than 2 x 10(-6) cm/s, which showed that SLB was a moderately permeable drug. The efflux ratio was greater than 2 indicating the efflux transporter may be involved in the absorption process of SLB. The P(app )of silybin-N-meglumine was similar to that of SLB, suggesting that salt formation did not alter the membrane permeability of SLB. In conclusion, the membrane permeability of SLB is good, and its solubility is low. SLB is a BCS class 2 drug. The release of SLB in the gastrointestinal tract is an important factor in its absorption process.
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页码：202 / 208
页数：7
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