Publications (2)1.24 Total impact
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ABSTRACT: The pharmacokinetics and residues elimination of hydrochloric acid albendazole sulfoxide (ABZSO) and its metabolites were studied in healthy crucian carp (Carassius auratus, 250 ± 30 g) kept at water temperatures of 10 °C and 25 °C. The concentrations of ABZSO and its metabolites concentration in plasma and tissues were determined using high-performance liquid chromatography (HPLC) using an ultraviolet detector. The results revealed that the plasma concentration of ABZSO in plasma was significantly higher than that of albendazole sulfone (ABZSO(2)), whereas albendazole-2-aminosulfone (ABZ-SO(2)NH(2)) was not detected. The plasma concentrations of ABZSO and its main metabolite ABZSO(2) concentration-time data were fitted using a single-compartment model at 10 °C and 25 °C. The absorption half-life (t₁/₂ka) of ABZSO was 3.86 h at 10 °C and 1.29 h at 25 °C, whereas the elimination half-life (t₁/₂ke) was 16.34 h at 10 °C and 6.72 h at 25 °C; the maximum plasma concentration (C(max)) and the time-point of maximum plasma concentration (T(p)) were calculated as 3.20 μg mL(-1) and 10.58 h at 10 °C, 4.39 μg mL(-1) and 3.80 h at 25 °C. The distribution volume (V(d)/F) of ABZSO was estimated to be 1.99 L kg(-1) at 10 °C and 1.53 L kg(-1) at 25 °C; the total body clearance (CL(b)) of ABZSO were computed as 0.08 and 0.19 L/(h kg) at 10 and 25 °C, respectively; the areas under the concentration-time curve (AUC) was 118.22 μg mL(-1)h at 10 °C and 63.12 μg mL(-1)h at 25 °C. The [Formula: see text] of ABZSO(2) was found to be 6.39 °C at 10 °C and 3.73 h at 25 °C, whereas the [Formula: see text] was 12.86 h at 10 °C and 6.56 h at 25 °C; the C(max) and T(p) of ABZSO(2) was calculated as 0.78 μg mL(-1) and 12.82 h at 10 °C, 1.03 μg mL(-1) and 7.04 h at 25 °C, respectively; the V(d)/F of ABZSO(2) were estimated to be 6.43 L kg(-1) at 10 °C and 4.61 Lkg(-1) at 25 °C; the CL(b) of ABZSO(2) were computed as 0.34 and 0.49 L/(h kg) at 10 °C and 25 °C, respectively; the AUC of ABZSO(2) were 28.86 μg mL(-1)h at 10 °C and 20.52 μg mL(-1)h at 25 °C. It was demonstrated that ABZSO(2) was the main metabolite of ABZSO. The concentrations of ABZSO and its main metabolite (ABZSO(2)) were detected in muscle, skin, liver and kidney, whereas ABZ-SO(2)NH(2) was only detected in liver and kidney. The ABZSO and it metabolite (ABZSO(2)) could still be detected at 4 d time-point after administration at both temperatures in all tissues. The results revealed that the depletion of ABZSO and its metabolite (ABZSO(2)) in crucian carp was slower with a long half-life time, especially at lower water temperature.
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ABSTRACT: Danofloxacin mesylate gelatin microspheres (DFM-GMS) were prepared by an emulsion chemical crosslinking technique. Distribution of particle size, morphologic characteristics, drug content, and drug stability were evaluated. In-vitro study showed that the release of danofloxacin mesylate (DFM) from microspheres was much slower than from the raw material (DFM) in the release medium. Pharmacokinetic characteristics were evaluated following intramuscular injection of DFM-GMS or DFM in pigs at dosage of 2.5 mg/kg body weight. Elimination half-life (t(1/2β)) of the drug was 24.32 h for DFM-GMS, and 6.61 h for DFM (P < 0.01). Overall, DFM-GMS could be applied as a long-acting and lung targeting dosage form of DFM for clinical application.
Huazhong Agricultural University
Wu-han-shih, Hubei, China
- College of Veterinary Medicine