Importance of bile acids for novel oral absorption system containing polyamines to improve intestinal absorption

The synergetic improving effect of bile acids with spermine (SPM), a major polyamine, on the absorption of rebamipide, a poorly soluble and poorly absorbable drug (BCS Class IV), was evaluated in rats and beagle dogs. Although the absorption of rebamipide was improved by the addition of polyamines a...

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Veröffentlicht in:Journal of controlled release 2006-10, Vol.115 (2), p.130-133
Hauptverfasser: Miyake, Masateru, Minami, Takanori, Toguchi, Hajime, Odomi, Masaaki, Ogawara, Ken-ichi, Higaki, Kazutaka, Kimura, Toshikiro
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container_end_page 133
container_issue 2
container_start_page 130
container_title Journal of controlled release
container_volume 115
creator Miyake, Masateru
Minami, Takanori
Toguchi, Hajime
Odomi, Masaaki
Ogawara, Ken-ichi
Higaki, Kazutaka
Kimura, Toshikiro
description The synergetic improving effect of bile acids with spermine (SPM), a major polyamine, on the absorption of rebamipide, a poorly soluble and poorly absorbable drug (BCS Class IV), was evaluated in rats and beagle dogs. Although the absorption of rebamipide was improved by the addition of polyamines alone in normal rats, it was not improved in bile duct ligated (BDL) rats. The combinatorial use of sodium taurocholate (STC), a bile acid, with SPM improved the absorption of rebamipide even in BDL rats. In the beagle dogs, the oral administration of SPM alone did not enhance the absorption of rebamipide, but the combinatorial use of STC with SPM improved the absorption as well as in the BDL rats. These results indicate that bile acids are indispensable for the novel formulation containing SPM to improve the absorption of rebamipide after oral administration.
doi_str_mv 10.1016/j.jconrel.2006.07.015
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Pharmaceutical industry</subject><subject>Pharmacology. 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Pharmaceutical industry</topic><topic>Pharmacology. 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Although the absorption of rebamipide was improved by the addition of polyamines alone in normal rats, it was not improved in bile duct ligated (BDL) rats. The combinatorial use of sodium taurocholate (STC), a bile acid, with SPM improved the absorption of rebamipide even in BDL rats. In the beagle dogs, the oral administration of SPM alone did not enhance the absorption of rebamipide, but the combinatorial use of STC with SPM improved the absorption as well as in the BDL rats. These results indicate that bile acids are indispensable for the novel formulation containing SPM to improve the absorption of rebamipide after oral administration.</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>16973235</pmid><doi>10.1016/j.jconrel.2006.07.015</doi><tpages>4</tpages></addata></record>
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subjects Alanine - administration & dosage
Alanine - analogs & derivatives
Alanine - pharmacokinetics
Animals
Area Under Curve
Beagle dog
Bile acid
Bile Acids and Salts - pharmacology
Bile duct ligated rat
Bile Ducts - physiology
Biogenic Polyamines - pharmacology
Biological and medical sciences
Dogs
General pharmacology
Intestinal absorption
Intestinal Absorption - drug effects
Ligation
Male
Medical sciences
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Polyamine
Quinolones - administration & dosage
Quinolones - pharmacokinetics
Rats
Rats, Sprague-Dawley
Spermine - pharmacology
Taurocholic Acid - pharmacology
title Importance of bile acids for novel oral absorption system containing polyamines to improve intestinal absorption
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