Decrease in ciprofloxacin absorption by polyvalent metal cations is not fully attributable to chelation or adsorption

Ayuko Imaoka; Michiko Hattori; Takeshi Akiyoshi; Hisakazu Ohtani

doi:10.2133/dmpk.DMPK-14-RG-001

Decrease in ciprofloxacin absorption by polyvalent metal cations is not fully attributable to chelation or adsorption

Ayuko Imaoka, Michiko Hattori, Takeshi Akiyoshi, Hisakazu Ohtani

Research output: Contribution to journal › Article › peer-review

4 Citations (Scopus)

Abstract

The drug interaction between new quinolone antibiotics (NQs) and polyvalent metal cation products, leading to a significant decrease in the absorption of NQ, is considered to be attributable to the formation of poorly absorbable chelate and physicochemical adsorption of NQs to cation products. To clarify the mechanisms of this drug interaction in detail, we investigated the effects of Al³⁺ or Mg²⁺ on the membrane permeation profile of ciprofloxacin (CPFX) across human colon carcinoma cell lines (Caco-2) in monolayer culture, and characterized the adsorption nature of CPFX to polyvalent metal cation products under physiological conditions. As a result, Al³⁺ or Mg²⁺ partially but not fully impaired the permeation of CPFX across Caco-2 monolayer up to 30% or 60% of control, respectively. Physicochemical adsorption of CPFX to cation products was not observed under physiological pH. In conclusion, two possible mechanisms investigated, the decrease in the permeability of CPFX by chelate formation and adsorption of CPFX to polyvalent metal cation products, may partially but not fully explain the extent of the drug interaction clinically observed.

Original language	English
Pages (from-to)	414-418
Number of pages	5
Journal	Drug Metabolism And Pharmacokinetics
Volume	29
Issue number	5
DOIs	https://doi.org/10.2133/dmpk.DMPK-14-RG-001
Publication status	Published - 2014

Keywords

Absorption
Adsorption
Aluminum
Caco-2 cells
Chelate
Drug interactions
Magnesium
New quinolones
Permeability

ASJC Scopus subject areas

Pharmacology
Pharmaceutical Science
Pharmacology (medical)

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10.2133/dmpk.DMPK-14-RG-001

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title = "Decrease in ciprofloxacin absorption by polyvalent metal cations is not fully attributable to chelation or adsorption",

abstract = "The drug interaction between new quinolone antibiotics (NQs) and polyvalent metal cation products, leading to a significant decrease in the absorption of NQ, is considered to be attributable to the formation of poorly absorbable chelate and physicochemical adsorption of NQs to cation products. To clarify the mechanisms of this drug interaction in detail, we investigated the effects of Al3+ or Mg2+ on the membrane permeation profile of ciprofloxacin (CPFX) across human colon carcinoma cell lines (Caco-2) in monolayer culture, and characterized the adsorption nature of CPFX to polyvalent metal cation products under physiological conditions. As a result, Al3+ or Mg2+ partially but not fully impaired the permeation of CPFX across Caco-2 monolayer up to 30% or 60% of control, respectively. Physicochemical adsorption of CPFX to cation products was not observed under physiological pH. In conclusion, two possible mechanisms investigated, the decrease in the permeability of CPFX by chelate formation and adsorption of CPFX to polyvalent metal cation products, may partially but not fully explain the extent of the drug interaction clinically observed.",

keywords = "Absorption, Adsorption, Aluminum, Caco-2 cells, Chelate, Drug interactions, Magnesium, New quinolones, Permeability",

author = "Ayuko Imaoka and Michiko Hattori and Takeshi Akiyoshi and Hisakazu Ohtani",

note = "Publisher Copyright: Copyright {\textcopyright} 2014 by the Japanese Society for the Study of Xenobiotics (JSSX).",

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doi = "10.2133/dmpk.DMPK-14-RG-001",

language = "English",

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AU - Akiyoshi, Takeshi

AU - Ohtani, Hisakazu

PY - 2014

Y1 - 2014

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AB - The drug interaction between new quinolone antibiotics (NQs) and polyvalent metal cation products, leading to a significant decrease in the absorption of NQ, is considered to be attributable to the formation of poorly absorbable chelate and physicochemical adsorption of NQs to cation products. To clarify the mechanisms of this drug interaction in detail, we investigated the effects of Al3+ or Mg2+ on the membrane permeation profile of ciprofloxacin (CPFX) across human colon carcinoma cell lines (Caco-2) in monolayer culture, and characterized the adsorption nature of CPFX to polyvalent metal cation products under physiological conditions. As a result, Al3+ or Mg2+ partially but not fully impaired the permeation of CPFX across Caco-2 monolayer up to 30% or 60% of control, respectively. Physicochemical adsorption of CPFX to cation products was not observed under physiological pH. In conclusion, two possible mechanisms investigated, the decrease in the permeability of CPFX by chelate formation and adsorption of CPFX to polyvalent metal cation products, may partially but not fully explain the extent of the drug interaction clinically observed.

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KW - New quinolones

KW - Permeability

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Decrease in ciprofloxacin absorption by polyvalent metal cations is not fully attributable to chelation or adsorption

Abstract

Keywords

ASJC Scopus subject areas

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