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Research ArticleBasic Science Investigation

PET Imaging of the Gastrointestinal Absorption of Orally Administered Drugs in Conscious and Anesthetized Rats

Shinji Yamashita, Tadayuki Takashima, Makoto Kataoka, Hiroyuki Oh, Shinji Sakuma, Masayuki Takahashi, Norio Suzuki, Emi Hayashinaka, Yasuhiro Wada, Yilong Cui and Yasuyoshi Watanabe
Journal of Nuclear Medicine February 2011, 52 (2) 249-256; DOI: https://doi.org/10.2967/jnumed.110.081539
Shinji Yamashita
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Tadayuki Takashima
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Makoto Kataoka
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Hiroyuki Oh
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Shinji Sakuma
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Masayuki Takahashi
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Norio Suzuki
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Emi Hayashinaka
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Yasuhiro Wada
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Yilong Cui
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Yasuyoshi Watanabe
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  • FIGURE 1.
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    FIGURE 1.

    Coronal maximum-intensity-projection whole-body PET images after oral administration of 18F-FDG to conscious and anesthetized rats: 40 min (A) and 85 min (B).

  • FIGURE 2.
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    FIGURE 2.

    Coronal maximum-intensity-projection abdominal PET images obtained serially after oral administration of 18F-FDG to conscious rat (A) and rats anesthetized with isoflurane (B) or propofol (C).

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    FIGURE 3.

    Time courses of radioactivity in stomach (A) and small intestine (B) after oral administration of 18F-FDG to conscious rats (○) and rats anesthetized with isoflurane (□) or propofol (▵). Data are mean ± SD of 3 experiments.

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    FIGURE 4.

    Compartment model for gastric emptying and intestinal absorption. D (X0) represents dose of 18F-FDG. Xs and Xi represent amount of 18F-FDG in stomach and intestine, respectively, at time t.

  • FIGURE 5.
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    FIGURE 5.

    Time courses of radioactivity in whole blood after oral administration of 18F-FDG to conscious rats (○) and rats anesthetized with isoflurane (▵) or propofol (□). Data are mean ± SD of 3 experiments.

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    FIGURE 6.

    Intestinal permeability of d-glucose and 2-FDG in absence or presence of glucose transporter inhibitors. As inhibitor, phlorizin (1.0 mM, gray bar) or d-glucose (20 mM, black bar) was added in luminal solution with [UL-13C6]-d-glucose or 2-FDG (0.1 mM, white bar). Data are mean ± SD of 3 experiments. *P < 0.05 compared with respective inhibitor-free experiment by unpaired Student t test.

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    TABLE 1.

    Parameters of Gastric Emptying and Intestinal Absorption

    Gastric emptyingIntestinal absorption
    State of ratskGE (min−1)T1/2 (min)kIT (min−1)T1/2 (min)Tmax (min)
    Conscious0.217 ± 0.0893.71 ± 1.890.057 ± 0.02714.19 ± 6.796.96 ± 2.35
    Anesthesia with isoflurane0.014 ± 0.001*50.32 ± 2.37*0.033 ± 0.00821.72 ± 4.8641.83 ± 14.36
    Anesthesia with propofol0.022 ± 0.011*36.46 ± 14.62*0.034 ± 0.00420.29 ± 2.4818.17 ± 6.43
    • ↵* P < 0.005 compared with conscious rat group by ANOVA.

    • T1/2 = Half-life of radioactivity in stomach or intestine.

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    TABLE 2.

    Pharmacokinetic Parameters from Blood Profile after Oral Administration of 18F-FDG to Rats

    State of ratsCmax (% of dose/mL)Tmax (min)Area under curve from 0 to 90 min (% of dose·min/mL)ka (min−1)
    Conscious0.554 ± 0.04523.3 ± 5.7729.39 ± 2.320.076 ± 0.019
    Anesthesia with isoflurane0.327 ± 0.091*50.0 ± 8.66*20.29 ± 3.23*0.016 ± 0.005*
    Anesthesia with propofol0.410 ± 0.13550.0 ± 8.66*28.07 ± 7.660.020 ± 0.009*
    • ↵* P < 0.005 compared with conscious rat group by ANOVA.

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Journal of Nuclear Medicine: 52 (2)
Journal of Nuclear Medicine
Vol. 52, Issue 2
February 1, 2011
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PET Imaging of the Gastrointestinal Absorption of Orally Administered Drugs in Conscious and Anesthetized Rats
Shinji Yamashita, Tadayuki Takashima, Makoto Kataoka, Hiroyuki Oh, Shinji Sakuma, Masayuki Takahashi, Norio Suzuki, Emi Hayashinaka, Yasuhiro Wada, Yilong Cui, Yasuyoshi Watanabe
Journal of Nuclear Medicine Feb 2011, 52 (2) 249-256; DOI: 10.2967/jnumed.110.081539

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PET Imaging of the Gastrointestinal Absorption of Orally Administered Drugs in Conscious and Anesthetized Rats
Shinji Yamashita, Tadayuki Takashima, Makoto Kataoka, Hiroyuki Oh, Shinji Sakuma, Masayuki Takahashi, Norio Suzuki, Emi Hayashinaka, Yasuhiro Wada, Yilong Cui, Yasuyoshi Watanabe
Journal of Nuclear Medicine Feb 2011, 52 (2) 249-256; DOI: 10.2967/jnumed.110.081539
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