Drug absorption from large intestine: Physicochemical factors governing drug absorption

T. Kimura, K. Sudo, Y. Kanzaki, K. Miki, Y. Takeichi, Yuji Kurosaki, T. Nakayama

Research output: Contribution to journalArticle

38 Citations (Scopus)

Abstract

Profiles of absorption versus drug molecular weight and absorption versus drug lipophilicity were investigated in both the small and large intestines of rats by an in situ loop method. The absorption-molecular weight profiles examined using different-sized polyethylene glycols (PEGs) were different between the small and large intestines; the large-intestinal absorption of PEGs with molecular weights larger than 300 was poor, while PEGs with molecular weights up to 600 were relatively well absorbed in the small intestine. It is suggested that the paracellular route for drug penetration in the large intestine is restricted more than in the small intestine. The absorption-lipophilicity profiles were also examined in various regions (loops of 6 cm) of rat intestine using three acylsalicylic acids, acetyl-, propionyl- and butyrylsalicylic acids. The absorption rates of the acylsalicylic acids were different in the intestinal regions: the jejunum > the ileum > the colon > the rectum. In each region, the absorption rate increased with the drug lipophilicity. However, it was shown that the absorption rates in the small intestine tended to reach a ceiling at the high lipophilicity. To confirm this tendency, the absorption rates of acetaminophen and indomethacin were compared in the four intestinal regions. The absorption rates of highly lipophilic indomethacin were similar in the large and small intestines, while intermediately lipophilic acetaminophen was more rapidly absorbed in the small intestine than in the large intestine. A thicker unstirred water layer adjacent to the small-intestinal mucosa would be one of the factors which cause such varying absorption-lipophilicity profiles.

Original languageEnglish
Pages (from-to)327-333
Number of pages7
JournalBiological and Pharmaceutical Bulletin
Volume17
Issue number2
Publication statusPublished - 1994

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Large Intestine
Small Intestine
Pharmaceutical Preparations
Molecular Weight
Acetaminophen
Indomethacin
Acids
Intestinal Absorption
Jejunum
Intestinal Mucosa
Ileum
Rectum
Intestines
Colon
Water

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology, Toxicology and Pharmaceutics(all)

Cite this

Kimura, T., Sudo, K., Kanzaki, Y., Miki, K., Takeichi, Y., Kurosaki, Y., & Nakayama, T. (1994). Drug absorption from large intestine: Physicochemical factors governing drug absorption. Biological and Pharmaceutical Bulletin, 17(2), 327-333.

Drug absorption from large intestine : Physicochemical factors governing drug absorption. / Kimura, T.; Sudo, K.; Kanzaki, Y.; Miki, K.; Takeichi, Y.; Kurosaki, Yuji; Nakayama, T.

In: Biological and Pharmaceutical Bulletin, Vol. 17, No. 2, 1994, p. 327-333.

Research output: Contribution to journalArticle

Kimura, T, Sudo, K, Kanzaki, Y, Miki, K, Takeichi, Y, Kurosaki, Y & Nakayama, T 1994, 'Drug absorption from large intestine: Physicochemical factors governing drug absorption', Biological and Pharmaceutical Bulletin, vol. 17, no. 2, pp. 327-333.
Kimura, T. ; Sudo, K. ; Kanzaki, Y. ; Miki, K. ; Takeichi, Y. ; Kurosaki, Yuji ; Nakayama, T. / Drug absorption from large intestine : Physicochemical factors governing drug absorption. In: Biological and Pharmaceutical Bulletin. 1994 ; Vol. 17, No. 2. pp. 327-333.
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