The objective of this work was to systematically investigate the absorptive profile of chlorogenic acid (CGA) in rats and to increase its intestinal absorption using absorption enhancers. The rat in situ intestinal perfusion technique was used to examine absorptive rate and extent of CGA. In vitro enzymatic drug degradation study was carried out with rat intestinal washings. Various experimental conditions such as different concentrations, extraction purity, and different absorption enhancers such as sodium taurocholate (ST), sodium lauryl sulphate (SLS), carbomer, borneol were examined. Absorption rate constants were determined by the plot of log remaining amount of drug in perfusate vs. time. During the in vitro enzymatic degradation study, no measurable degradation was observed. It was found that CGA could be poorly absorbed by the gastrointestinal tract. The absorptive rate of CGA is independent of the drug concentration. Absorption processes fit first order processes. Extraction of high purity is benefit to the absorption of CGA. Drug absorption extent could be increased via absorption enhancers except SLS. ST appeared to be more effective for enhancing the intestinal absorption of CGA than the other absorption enhancers. In vivo studies were carried out to compare the pharmacokinetic parameters of solutions with and without ST. The order of increasing CGA absorption caused by the enhancers was ST > carbomer > borneol > SLS.
机构:
Sichuan Univ, W China Sch Pharm, Key Lab Drug Targeting, Chengdu 610041, Peoples R ChinaSichuan Univ, W China Sch Pharm, Key Lab Drug Targeting, Chengdu 610041, Peoples R China
Ren, Jing
Jiang, Xuehua
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Sichuan Univ, W China Sch Pharm, Key Lab Drug Targeting, Chengdu 610041, Peoples R ChinaSichuan Univ, W China Sch Pharm, Key Lab Drug Targeting, Chengdu 610041, Peoples R China
Jiang, Xuehua
Li, Chenrui
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Sichuan Univ, W China Sch Pharm, Key Lab Drug Targeting, Chengdu 610041, Peoples R ChinaSichuan Univ, W China Sch Pharm, Key Lab Drug Targeting, Chengdu 610041, Peoples R China
机构:
Hunan Univ Arts & Sci, Inst Phys Culture, Dept Human Movement Sci, Changde 415000, Peoples R ChinaHunan Univ Arts & Sci, Inst Phys Culture, Dept Human Movement Sci, Changde 415000, Peoples R China
Liu Xianchu
Cheng Changhao
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Hunan Univ Arts & Sci, Inst Phys Culture, Dept Human Movement Sci, Changde 415000, Peoples R ChinaHunan Univ Arts & Sci, Inst Phys Culture, Dept Human Movement Sci, Changde 415000, Peoples R China
Cheng Changhao
Deng Beiwang
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Hunan Univ Arts & Sci, Inst Phys Culture, Dept Human Movement Sci, Changde 415000, Peoples R ChinaHunan Univ Arts & Sci, Inst Phys Culture, Dept Human Movement Sci, Changde 415000, Peoples R China
Deng Beiwang
Peng Huan
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Xiangya Changde Hosp, Dept Hematol, Changde, Hunan 415000, Peoples R ChinaHunan Univ Arts & Sci, Inst Phys Culture, Dept Human Movement Sci, Changde 415000, Peoples R China
Peng Huan
Liu Ming
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Hunan Univ Arts & Sci, Coll Life & Environm Sci, Dept Biochem, Changde 415000, Peoples R ChinaHunan Univ Arts & Sci, Inst Phys Culture, Dept Human Movement Sci, Changde 415000, Peoples R China