Document Detail

Improvement of intestinal peptide absorption by a synthetic bile acid derivative, cholylsarcosine.
MedLine Citation:
PMID:  10727879     Owner:  NLM     Status:  MEDLINE    
The potential of the nontoxic bile salt derivative, cholylsarcosine, to enhance the intestinal absorption of peptides was investigated in vitro and in situ. The permeation of the two model peptides octreotide and vasopressin-[arg(8)CT>/=CS, whereas ursodeoxycholic acid exhibited no absorption enhancement. Determination of the cytotoxic potential of the bile salts revealed the same rank order. In rats, octreotide and desmopressin were absorbed from the gastrointestinal-tract with moderate absorption efficiency. Coadministration of bile salts resulted in an increased absorption efficiency. The effect of CS was similar to that of CT. In conclusion, CS shows absorption enhancement properties and a relatively low cytotoxicity. It offers an alternative as absorption enhancer as compared to conventional bile acids which may have a potential cocarcinogenic risk.
S Michael; M Thöle; R Dillmann; A Fahr; J Drewe; G Fricker
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences     Volume:  10     ISSN:  0928-0987     ISO Abbreviation:  Eur J Pharm Sci     Publication Date:  2000 Apr 
Date Detail:
Created Date:  2000-06-23     Completed Date:  2000-06-23     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  9317982     Medline TA:  Eur J Pharm Sci     Country:  NETHERLANDS    
Other Details:
Languages:  eng     Pagination:  133-40     Citation Subset:  IM    
Institut für Pharmazeutische Technologie und Biopharmazie, Ruprecht-Karls-Universität Heidelberg, Heidelberg, Germany.
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MeSH Terms
Area Under Curve
Bile Acids and Salts / pharmacology
Caco-2 Cells
Cell Membrane Permeability / drug effects
Cell Survival / drug effects
Cholic Acids / pharmacology*
Electric Impedance
Fluorescein-5-isothiocyanate / analogs & derivatives
Fluorescent Dyes
Intestinal Absorption / drug effects*
Membranes, Artificial
Peptides / pharmacokinetics*
Rats, Wistar
Sarcosine / analogs & derivatives*,  pharmacology
Stimulation, Chemical
Reg. No./Substance:
0/Bile Acids and Salts; 0/Cholic Acids; 0/Fluorescent Dyes; 0/Membranes, Artificial; 0/Peptides; 0/fluorescein isothiocyanate dextran; 107-97-1/Sarcosine; 3326-32-7/Fluorescein-5-isothiocyanate; 9004-54-0/Dextrans; 93790-70-6/cholylsarcosine

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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