Document Detail

Absorption enhancement study of astragaloside IV based on its transport mechanism in caco-2 cells.
MedLine Citation:
PMID:  16715776     Owner:  NLM     Status:  MEDLINE    
The purpose of this study was to investigate the transport characteristics and mechanisms for discovering the possible causes of the low bioavailability of astragaloside IV and to develop an absorption enhancement strategy. Caco-2 cells used as the in vitro model. Results showed a low permeability coefficient (3.7 x 10(-8)cm/s for transport from the AP to BL direction), which remained unchanged throughout the concentration range studied, indicating that the transport of astragaloside IV was predominantly via a passive route. The AP to BL transport of astragaloside IV was found to be highly sensitive to the extracellular Ca2+ concentration, which suggested that its transport may be via a paracellular route. Both chitosan and sodium deoxycholate can increase the permeation efficiency of astragaloside IV. This study indicated that astragaloside IV having a low fraction dose absorbed in humans mainly due to its poor intestinal permeability, high molecular weight, low lipophilicity as well as its paracelluar transport may directly result in the low permeability through its passive transport. Meanwhile, chitosan and sodium deoxycholate can be used as absorption enhancers based on its transport mechanism.
C R Huang; G J Wang; X L Wu; H Li; H T Xie; H Lv; J G Sun
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  European journal of drug metabolism and pharmacokinetics     Volume:  31     ISSN:  0378-7966     ISO Abbreviation:  Eur J Drug Metab Pharmacokinet     Publication Date:    2006 Jan-Mar
Date Detail:
Created Date:  2006-05-23     Completed Date:  2006-07-25     Revised Date:  2011-02-02    
Medline Journal Info:
Nlm Unique ID:  7608491     Medline TA:  Eur J Drug Metab Pharmacokinet     Country:  Switzerland    
Other Details:
Languages:  eng     Pagination:  5-10     Citation Subset:  IM    
Drug Metabolism and Pharmacokinetic Research Center, China Pharmaceutical University, Nanjing, People's Republic of China.
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MeSH Terms
Biological Availability
Biological Transport / drug effects
Caco-2 Cells
Chelating Agents / pharmacology
Chitosan / pharmacology
Chromatography, Liquid
Data Interpretation, Statistical
Deoxycholic Acid / pharmacology
Edetic Acid / pharmacology
Intestinal Absorption / drug effects*
Saponins / metabolism,  pharmacology*
Spectrometry, Mass, Electrospray Ionization
Stimulation, Chemical
Triterpenes / metabolism,  pharmacology*
Reg. No./Substance:
0/Chelating Agents; 0/Saponins; 0/Triterpenes; 60-00-4/Edetic Acid; 83-44-3/Deoxycholic Acid; 83207-58-3/astragaloside A; 9012-76-4/Chitosan

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