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. 2021 Sep 16;26(18):5633.
doi: 10.3390/molecules26185633.

Absorption and Distribution of Toltrazuril and Toltrazuril Sulfone in Plasma, Intestinal Tissues and Content of Piglets after Oral or Intramuscular Administration

Hamadi Karembe  1 , Daniel Sperling  1 , Nathalie Varinot  1 , Reynald Magnier  1 , Mathieu Peyrou  1 , Nicolas Guerra  1 , Jiří Smola  2 , Jan Vasek  2 , Barbara Hinney  3 , Anja Joachim  3
Affiliations

Absorption and Distribution of Toltrazuril and Toltrazuril Sulfone in Plasma, Intestinal Tissues and Content of Piglets after Oral or Intramuscular Administration

Hamadi Karembe et al. Molecules. .

Abstract

Piglet coccidiosis due to Cystoisospora suis is a major cause of diarrhea and poor growth worldwide. It can effectively be controlled by application of toltrazuril (TZ), and oral formulations have been licensed for many years. Recently, the first parenteral formulation containing TZ in combination with iron (gleptoferron) was registered in the EU for the prevention of coccidiosis and iron deficiency anemia, conditions in suckling piglets requiring routine preventive measures. This study evaluated the absorption and distribution of TZ and its main metabolite, toltrazuril sulfone (TZ-SO2), in blood and intestinal tissues after single oral (20 mg/kg) or single intramuscular (45 mg/piglet) application of TZ. Fifty-six piglets were randomly allocated to the two treatment groups. Animals were sacrificed 1-, 5-, 13-, and 24-days post-treatment and TZ and TZ-SO2 levels were determined in blood, jejunal tissue, ileal tissue, and mixed jejunal and ileal content (IC) by high performance liquid chromatography (HPLC). Intramuscular application resulted in significantly higher and more sustained concentrations of both compounds in plasma, intestinal tissue, and IC. Higher concentrations after oral dosing were only observed one day after application of TZ in jejunum and IC. Toltrazuril was quickly metabolized to TZ-SO2 with maximum concentrations on day 13 for both applications. Remarkably, TZ and TZ-SO2 accumulated in the jejunum, the primary predilection site of C. suis, independently of the administration route, which is key to their antiparasitic effect.

Keywords: Isospora suis; anticoccidials; coccidiosis; pharmacokinetics; prevention; swine; tissue distribution.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Plasma concentrations of toltrazuril (TZ) and toltrazuril sulfone (TZ-SO2) (mean ± SD) following single oral (Baycox 5%) or intramuscular (Forceris) administration to piglets.
Figure 2
Figure 2
Concentrations of toltrazuril and toltrazuril sulfone (mean ± SD) in jejunal tissue following single oral (Baycox 5%) or intramuscular (Forceris) administration to piglets.
Figure 3
Figure 3
Concentrations of toltrazuril and toltrazuril sulfone (mean ± SD) in the ileum following single oral (Baycox 5%) or intramuscular (Forceris) administration to piglets.
Figure 4
Figure 4
Concentrations of toltrazuril and toltrazuril sulfone (mean ± SD) in the intestinal content following single oral (Baycox 5%) or intramuscular (Forceris) administration to piglets.
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