Determination of pharmacokinetic parameters and tissue distribution characters of enrofloxacin and its metabolite ciprofloxacin in Procambarus clarkii after two routes of administration

Liu, Yongtao; Zhang, Guodong; Sun, Ruyu; Zhou, Shu Feng; Dong, Jing; Yang, Yibin; Yang, Qiuhong; Xu, Ning; Ai, Xiaohui

doi:10.1016/j.aqrep.2021.100939

Cited by 5 publications

(4 citation statements)

References 25 publications

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“…Among 4 antibiotic classes, the FQs were detected in the samples with the highest detection frequency of 16.3%. This observation was consistent with previous investigations that the FQs were frequently detected in cultured aquatic products, indicating their common occurrence in the commercial fish ( He et al., 2016 ; Liu et al., 2022 ). Consideration of the ciprofloxacin as the main metabolite of enrofloxacin ( Xu et al., 2006 ; Elezz et al., 2019 ), the sum of the detection frequency for ciprofloxacin and enrofloxacin was calculated to evaluate the sample.…”

Section: Resultssupporting

confidence: 93%

Occurrence and human health risk assessment of antibiotics in cultured fish from 19 provinces in China

Tang

Lou

Yang

et al. 2022

Front. Cell. Infect. Microbiol.

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The occurrence of antibiotics and potential health risk of 300 cultured fish samples from 19 provinces in China were investigated. The levels of 28 antibiotics (15 fluoroquinolones, 4 tetracyclines, 8 macrolides and rifampin) in 8 fish species were measured through liquid chromatography electrospray tandem mass spectrometry. As a result, 10 antibiotics were detected with an overall detection frequency of 24.3%, and the individual detection frequency of antibiotics ranged from 0.33 to 16.7%. The extremely high concentrations (above 100 µg/kg) of doxycycline and erythromycin were found in the samples. Antibiotics with high detection frequency was noticed in largemouth bass (41.2%), followed by snakehead (34.4%) and bream (31.2%). Specifically, Heilongjiang, Xinjiang, Qinghai and Gansu presented high detection frequency values of more than 60%. Moreover, the highest mean concentration was observed in Shandong, and the concentration covered from 34.8 µg/kg to 410 µg/kg. Despite the high detection frequency and levels of antibiotics were found in samples, ingestion of cultured fish was not significantly related to human health risks in China, according to the calculated estimated daily intakes and hazard quotients. These results provided us the actual levels of antibiotics in cultured fish and human health risk assessment of consuming fishery products.

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Section: Resultssupporting

confidence: 93%

Occurrence and human health risk assessment of antibiotics in cultured fish from 19 provinces in China

Tang

Lou

Yang

et al. 2022

Front. Cell. Infect. Microbiol.

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“…Enrofloxacin is a third-generation fluoroquinolone antibacterial drug [4,5] which is often used to treat bacterial infections in crab breeding operations in China because of its wide antibacterial spectrum and high potency [6,7]. Although enrofloxacin is approved for aquaculture in China [8], when used in large quantities, the antimicrobial remains in the aquaculture water and sediment accumulates in aquatic animals. Pharmacokinetic 2 of 14 studies on enrofloxacin in crustaceans, including the Eriocheir sinensis [9][10][11], Atlantic horseshoe crab [12], and giant mud crab [13], have been reported.…”

Section: Introductionmentioning

confidence: 99%

Transcriptomics Analysis of the Toxicological Impact of Enrofloxacin in an Aquatic Environment on the Chinese Mitten Crab (Eriocheir sinensis)

Wang

et al. 2023

IJERPH

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Enrofloxacin is an important antimicrobial drug that is widely used in aquaculture. Enrofloxacin residues can have negative effects on aquatic environments and animals. The toxicological effects of different concentrations of enrofloxacin residues in cultured water on Chinese mitten crabs (Eriocheir sinensis) were compared. A histological analysis of the E. sinensis hepatopancreas demonstrated that the hepatopancreas was damaged by the different enrofloxacin residue concentrations. The hepatopancreas transcriptome results revealed that 1245 genes were upregulated and that 1298 genes were downregulated in the low-concentration enrofloxacin residue group. In the high-concentration enrofloxacin residue group, 380 genes were upregulated, and 529 genes were downregulated. The enrofloxacin residues led to differentially expressed genes related to the immune system and metabolic processes in the hepatopancreas of the Chinese mitten crab, such as the genes for alkaline phosphatase, NF-kappa B inhibitor alpha, alpha-amylase, and beta-galactosidase-like. The gene ontology terms “biological process” and “molecular function” were enriched in the carboxylic acid metabolic process, DNA replication, the synthesis of RNA primers, the transmembrane transporter activity, the hydrolase activity, and the oxidoreductase activity. A Kyoto Encyclopedia of Genes and Genomes pathway analysis determined that the immune and metabolic signal transduction pathways were significantly enriched. Furthermore, the nonspecific immune enzyme (alkaline phosphatase) and the metabolic enzyme system played a role in the enrofloxacin metabolism in the E. sinensis hepatopancreas. These findings helped us to further understand the basis of the toxicological effects of enrofloxacin residues on river crabs and provided valuable information for the better utilization of enrofloxacin in aquatic water environments.

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“…5 Furthermore, ENR can treat bacterial diseases and mycoplasma infections in aquaculture. 6,7 ENR easily dissolves in methylene chloride, sodium hydroxide solution, and acetonitrile; is slightly soluble in methanol; and is poorly soluble in water. Its lower water solubility results in low bioavailability, thus limiting the study of ENR in vitro and in vivo.…”

Section: Introductionmentioning

confidence: 99%

“…Enrofloxacin (ENR) is a key third-generation fluoroquinolone antibiotic agent widely used for veterinary purposes. , ENR inhibits the main enzymes of the microbial cell, deoxyribonucleic acid (DNA) gyrase, in a selective manner (type II topoisomerase) and DNA topoisomerase IV, thus killing bacteria. , ENR can also treat urinary tract infections, respiratory tract infections, intestine tract infections, and skin and tissue infections in poultry, pigs, and cattle . Furthermore, ENR can treat bacterial diseases and mycoplasma infections in aquaculture. , ENR easily dissolves in methylene chloride, sodium hydroxide solution, and acetonitrile; is slightly soluble in methanol; and is poorly soluble in water. Its lower water solubility results in low bioavailability, thus limiting the study of ENR in vitro and in vivo .…”

Section: Introductionmentioning

confidence: 99%

Enhancing the Bioavailability of a Novel Enrofloxacin Salt by Inhibiting Precipitation via a Crystallization Inhibitor

Mao,

Wang,

Liu

et al. 2024

Crystal Growth & Design

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Highly soluble cocrystals can improve the bioavailability of poorly soluble drugs by inducing supersaturation when absorption is limited by drug dissolution. Enrofloxacin (ENR) is a concentration-dependent fluoroquinolone antibacterial with poor solubility. In this study, two new ENR salts, 3,5-dihydroxybenzoic acid (ENR-3,5-DHBA) and 2,6-dihydroxybenzoic acid (ENR-2,6-DHBA•1/2H 2 O), were prepared, and their physicochemical properties were evaluated for suitability in formulation development.Results showed that the solubility of the two new salts enhanced. Although ENR-3,5-DHBA had a much higher solubility than ENR, it underwent rapid precipitation during dissolution, forming the poorly soluble ENR•6H 2 O in aqueous form. This negated the potential high-solubility advantage of the new salt, which might have enhanced its dissolution rate and in vivo bioavailability. To solve this problem, we systematically evaluated suitable crystallization inhibitors that could maintain the supersaturation generated by cocrystal/salt dissolution for a prolonged period. At 37 °C, the solubility and mean AUC 0−24h of ENR-3,5-DHBA increased by about 4.7 and 1.5 times, respectively (compared with ENR), when ENR-3,5-DHBA was dosed with 2.0 mg/mL methacrylic acidethyl acrylate copolymer (ME) solution instead of an active pharmaceutical ingredient. This study demonstrates that using a highly soluble salt and an appropriate crystallization inhibitor is a potentially effective formulation strategy for improving the oral bioavailability of poorly soluble drugs.

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Determination of pharmacokinetic parameters and tissue distribution characters of enrofloxacin and its metabolite ciprofloxacin in Procambarus clarkii after two routes of administration

Cited by 5 publications

References 25 publications

Occurrence and human health risk assessment of antibiotics in cultured fish from 19 provinces in China

Occurrence and human health risk assessment of antibiotics in cultured fish from 19 provinces in China

Transcriptomics Analysis of the Toxicological Impact of Enrofloxacin in an Aquatic Environment on the Chinese Mitten Crab (Eriocheir sinensis)

Enhancing the Bioavailability of a Novel Enrofloxacin Salt by Inhibiting Precipitation via a Crystallization Inhibitor

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