| Improvement of intestinal peptide absorption by a synthetic bile acid derivative, cholylsarcosine. | |
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MedLine Citation:
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PMID: 10727879 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
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Authors:
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S Michael; M Thöle; R Dillmann; A Fahr; J Drewe; G Fricker |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't |
Journal Detail:
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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:
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Created Date: 2000-06-23 Completed Date: 2000-06-23 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 9317982 Medline TA: Eur J Pharm Sci Country: NETHERLANDS |
Other Details:
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Languages: eng Pagination: 133-40 Citation Subset: IM |
Affiliation:
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Institut für Pharmazeutische Technologie und Biopharmazie, Ruprecht-Karls-Universität Heidelberg, Heidelberg, Germany. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Area Under Curve Bile Acids and Salts / pharmacology Caco-2 Cells Cell Membrane Permeability / drug effects Cell Survival / drug effects Cholic Acids / pharmacology* Dextrans Electric Impedance Fluorescein-5-isothiocyanate / analogs & derivatives Fluorescent Dyes Humans Intestinal Absorption / drug effects* Male Membranes, Artificial Peptides / pharmacokinetics* Rats Rats, Wistar Sarcosine / analogs & derivatives*, pharmacology Stimulation, Chemical |
| Chemical | |
Reg. No./Substance:
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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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