Document Detail

Combinatorial use of sodium laurate with taurine or L-glutamine enhances colonic absorption of rebamipide, poorly absorbable antiulcer drug, without any serious histopathological mucosal damages.
MedLine Citation:
PMID:  12661076     Owner:  NLM     Status:  MEDLINE    
We previously reported that the combinatorial use of sodium laurate (C12) with several amino acids such as taurine (Tau) and L-glutamine (L-Gln) enhanced the colonic absorption of phenol red with attenuating the local toxicity caused by C12. However, even these amino acids could not protect epithelial cells from being damaged if the mucosal damage got worse to the coagulation necrosis by an excessive dose of C12. Comparing C12 with sodium caprate (C10), used in drug products marketed, 100 micromol C10 was needed to exert the similar absorption-enhancement of rebamipide, a poorly absorbable antiulcer drug, to that by 10 micromol C12, and 100 micromol C10 was obviously more toxic to the mucosa than 10 micromol C12. The combinatorial use of C12 with Tau or L-Gln enhanced the colonic absorption of rebamipide four to nine times larger in AUC than the control. Histopathologic studies clearly showed that Tau and L-Gln exerted the cytoprotective action on epithelial cells suffering from slight damages such as shrinkage and exfoliation, more articulately at 6 h than at 1.5 h after dosing. In conclusion, the combinatorial use of C12 with Tau or L-Gln could lead to a novel formulation improving the bioavailability of poorly absorbable drugs without any serious local damages.
Masateru Miyake; Yoshikazu Oka; Takanori Minami; Hajime Toguchi; Masaaki Odomi; Ken-Ichi Ogawara; Kazutaka Higaki; Toshikiro Kimura
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Publication Detail:
Type:  Comparative Study; Journal Article    
Journal Detail:
Title:  Journal of pharmaceutical sciences     Volume:  92     ISSN:  0022-3549     ISO Abbreviation:  J Pharm Sci     Publication Date:  2003 Apr 
Date Detail:
Created Date:  2003-03-27     Completed Date:  2003-11-20     Revised Date:  2006-11-15    
Medline Journal Info:
Nlm Unique ID:  2985195R     Medline TA:  J Pharm Sci     Country:  United States    
Other Details:
Languages:  eng     Pagination:  911-21     Citation Subset:  IM    
Copyright Information:
Copyright 2003 Wiley-Liss, Inc. and the American Pharmaceutical Association J Pharm Sci 92: 911-921, 2003
Department of Pharmaceutics, Faculty of Pharmaceutical Sciences, Okayama University, 1-1-1 Tsushima-naka Okayama 700-8530, Japan.
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MeSH Terms
Adjuvants, Pharmaceutic / adverse effects,  pharmacology*
Administration, Oral
Alanine / analogs & derivatives*,  pharmacokinetics*
Amino Acids / adverse effects,  pharmacology*
Anti-Ulcer Agents / pharmacokinetics
Biological Availability
Colon / drug effects,  metabolism
Glutamine / adverse effects,  pharmacology
Intestinal Absorption / drug effects*
Intestinal Mucosa / drug effects*,  metabolism,  pathology
Lauric Acids / adverse effects,  pharmacology*
Quinolones / pharmacokinetics*
Rats, Sprague-Dawley
Taurine / adverse effects,  pharmacology
Reg. No./Substance:
0/Adjuvants, Pharmaceutic; 0/Amino Acids; 0/Anti-Ulcer Agents; 0/Lauric Acids; 0/Quinolones; 107-35-7/Taurine; 111911-87-6/rebamipide; 143-07-7/lauric acid; 56-41-7/Alanine; 56-85-9/Glutamine

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

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