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      • KCI등재

        Comparative in vitro biotransformation of fipronil in domestic poultry using liver microsome

        Kraisiri Khidkhan,Saranya Poapolathep,Sittinee Kulprasertsri,Rattapong Sukkheewan,Paphatsara Khunlert,Mario Giorgi,Amnart Poapolathep 대한수의학회 2022 Journal of Veterinary Science Vol.23 No.6

        Domestic poultry are among the non-target species of exposure to fipronil, but limited information is available on the metabolic effects of fipronil exposure in avian. We investigated the comparative capacity of in vitro biotransformation of fipronil among chicken, duck, quail, goose, and rat. Interspecies differences in kinetic parameters were observed; the clearance rate calculations (Vmax/Km) indicated that chicken and duck are more efficient in the cytochrome P450-mediated metabolism of fipronil to sulfone than quail, goose and rat. The lower hepatic clearance of fipronil in quail, goose and rat, suggested that fipronil sulfone may serve as a biomarker to indicate fipronil exposure in these species.

      • KCI등재

        Elution profiles of metronidazole from calcium sulfate beads

        Burasarin Ithisariyanont,Saranya Poapolathep,Amnart Poapolathep,Pareeya Udomkusonsri 대한수의학회 2023 Journal of Veterinary Science Vol.24 No.6

        Background: Antibiotic beads are used to treat local bacterial infections by delivering high drug concentrations to infected tissue. Objectives: This study examined the elution characteristics of metronidazole from metronidazole-calcium sulfate (MCa) and metronidazole-calcium-potassium sulfate (MCaK) beads over 20 days and the antibacterial efficacy of the beads after storage. Methods: The MCa and MCaK beads were prepared by mixing 250 mg of metronidazole and 10 g of calcium sulfate hemihydrate with water and a 3% potassium sulfate solution, respectively. The beads were placed in phosphate-buffered saline for the elution study. The metronidazole eluents were determined using high-performance liquid chromatography. The microstructures were examined by scanning electron microscopy (SEM), and the antimicrobial activity was evaluated by a microbioassay. Results: For the 20-day study, the total amount of metronidazole released was greater in the MCa beads than in the MCaK beads by 6.61 ± 0.48 mg (89.11% ± 3.04%) and 4.65 ± 0.36 mg (73.11% ± 4.38%), respectively. The amounts of eluted drugs from the MCa and MCaK beads were higher than the minimum inhibitory concentration at 0.5 µg/mL against anaerobicbacteria at both 20 days and 14 days. SEM showed that calcium crystals on the outer surface had dissolved after elution, and thinner calcium crystals were prominent in the MCaK beads. The MCa and MCaK beads exhibited antibacterial activity after setting, followed by storage at room temperature or 4°C for 21 days. Conclusions: The MCa beads could release more drug than the MCaK beads, but all eluted metronidazole amounts were effective in controlling bacterial infections. Both metronidazole beads could be stored at ambient temperature or in a refrigerator.

      • SCIESCOPUSKCI등재

        Pharmacokinetics of thalidomide in dogs: can feeding affect it? A preliminary study

        Pierini, Alessio,Sartini, Irene,Giorgi, Mario,Lebkowska-Wieruszewska, Beata,Lisowski, Andrzej,Poapolathep, Amnart,Marchetti, Veronica The Korean Society of Veterinary Science 2020 JOURNAL OF VETERINARY SCIENCE Vol.21 No.2

        Background: Tumor-associated neoangiogenesis is a crucial target for antitumor therapies. Thalidomide (TAL) is a promising anti-neoangiogenetic drug that has recently been used in the treatment of several malignancies in dogs. Objectives: The aim of the study was to assess the pharmacokinetics of TAL after single oral administration in dogs. Additionally, the influence of feeding on the pharmacokinetic profile of TAL in dogs has been preliminarily investigated. Methods: Six healthy adult female Labradors were enrolled according to a randomized single-dose, 2-treatment, 2-phase, paired 2 × 2 cross-over study design. The dogs were administered a single 400 mg capsule of TAL in fasted and fed conditions. Blood was collected from 15 min to 48 h after dosing, and TAL quantified in plasma by a validated high-performance liquid chromatography method. The pharmacokinetics of TAL were analyzed using a non-compartmental approach. Results: TAL concentration was quantifiable up to 10 h and 24 h after fasted and fed conditions, respectively. C<sub>max</sub> (fasted, 1.34 ± 0.12 ㎍/mL; fed, 2.47 ± 0.19 ㎍/mL) and T<sub>max</sub> (fasted, 3 h; fed, 10 h) differed substantially between the 2 groups. AUC and t<sub>1/2</sub>λz were significantly higher in fed (42.46 ± 6.64 mg × h/L; 17.14 ± 4.68 h) compared to fasted (12.38 ± 1.13 mg × h/L; 6.55 ± 1.25 h) dogs. The relative oral bioavailability of TAL for the fasted group was low (36.92% ± 3.28%). Conclusions: Feeding affects the pharmacokinetics of oral TAL in dogs, showing a delayed, but higher absorption with different rate of elimination. These findings are of importance in clinical veterinary settings, and represent a starting point for further related studies.

      • KCI등재

        Pharmacokinetics of thalidomide in dogs: can feeding affect it? A preliminary study

        Alessio Pierini,Irene Sartini,Mario Giorgi,Beata Łebkowska-Wieruszewska,Andrzej Lisowski,Amnart Poapolathep,Veronica Marchetti 대한수의학회 2020 Journal of Veterinary Science Vol.21 No.5

        Background: Tumor-associated neoangiogenesis is a crucial target for antitumor therapies. Thalidomide (TAL) is a promising anti-neoangiogenetic drug that has recently been used in the treatment of several malignancies in dogs. Objectives: The aim of the study was to assess the pharmacokinetics of TAL after single oral administration in dogs. Additionally, the influence of feeding on the pharmacokinetic profile of TAL in dogs has been preliminarily investigated. Methods: Six healthy adult female Labradors were enrolled according to a randomized single-dose, 2-treatment, 2-phase, paired 2 × 2 cross-over study design. The dogs were administered a single 400 mg capsule of TAL in fasted and fed conditions. Blood was collected from 15 min to 48 h after dosing, and TAL quantified in plasma by a validated high-performance liquid chromatography method. The pharmacokinetics of TAL were analyzed using a non-compartmental approach. Results: TAL concentration was quantifiable up to 10 h and 24 h after fasted and fed conditions, respectively. Cmax (fasted, 1.34 ± 0.12 μg/mL; fed, 2.47 ± 0.19 μg/mL) and Tmax (fasted, 3 h; fed, 10 h) differed substantially between the 2 groups. AUC and t1/2λz were significantly higher in fed (42.46 ± 6.64 mg × h/L; 17.14 ± 4.68 h) compared to fasted (12.38 ± 1.13 mg × h/L; 6.55 ± 1.25 h) dogs. The relative oral bioavailability of TAL for the fasted group was low (36.92% ± 3.28%). Conclusions: Feeding affects the pharmacokinetics of oral TAL in dogs, showing a delayed, but higher absorption with different rate of elimination. These findings are of importance in clinical veterinary settings, and represent a starting point for further related studies.

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