Determination of tiamulin hydrogen fumarate in animal feeds using high-performance liquid chromatography

Howard, Deborah; Cowen, Todd

doi:10.1039/an9820700319

Cited by 8 publications

(4 citation statements)

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“…The absorption half‐life ( t 1 / 2kα ) in plasma was found to be shorter (1.29 and 0.44 h) after oral and intravenous administration, respectively, than that reported in dog (2.2 ± 0.19 h for subcutaneous administration of 25 mg/kg; 2.76 ± 0.13 h for subcutaneous route of 10 mg/kg tiamulin, and 2.23 ± 0.76 h for intramuscular administration of 10 mg/kg tiamulin). The difference may mainly be related to the pharmaceutical preparation of tiamulin, that is, TIF is the fumarate of tiamulin, which has a water‐soluble property (Howard & Cowen, 1982). By control, tiamulin is a poorly water‐soluble drug (i.e., 0.36008 mg/L; ChemSpider, 2020).…”

Section: Discussionmentioning

confidence: 99%

“…Tiamulin, [14‐deoxy‐14‐(2‐diethylaminoethyl) mercaptoacetoxy‐mutilin], is a semisynthetic derivative of the natural antibiotic pleuromutilin, produced by fungi Pleurotus mutilus or Clitopilus (Hanson et al, 2002; Witkamp et al, 1996). The fumarate of tiamulin (TIF; Figure 1) is an ideally chemical medicine and suitable for administration in feed, in drinking water, or by injection because of its stability and water‐soluble properties (Howard & Cowen, 1982). The activity of tiamulin against antibacterial depends on the inhibition of protein synthesis by binding to the 50S ribosomal subunit (Schlünzen et al, 2004) and blocking the substrate‐binding site for peptide formation (Hodgin & Högenauer, 1974; Long et al, 2006; Poulsen et al, 2001; Schlünzen et al, 2004).…”

Section: Introductionmentioning

confidence: 99%

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Pharmacokinetics, bioavailability, and tissue disposal profiles of Tiamulin fumarate in Nile tilapia (Oreochromis niloticus) following oral and intravenous administrations

Liu

Cao

Song

et al. 2021

Vet Pharm & Therapeutics

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Tiamulin fumarate (TIF) is a pleuromutilin antibiotic and has high activity against animal bacterial pathogens including aquatic bacterial pathogens. However, its pharmacokinetic profiles, tissue distribution characteristics and bioavailability in aquatic animals remain unknown. The objective of this study was to investigate the pharmacokinetics and tissue distribution regularities of TIF in tilapia (Oreochromis niloticus) following a single oral (PO) dose of 20 mg/kg body weight (bw) and a single intravenous (IV) dose of 5 mg/kg bw at 22 ± 1°C, respectively. TIF concentrations in tilapia plasma and tissues were determined using the isotope dilution HPLC‐HESI‐MS/MS procedure, which was validated according to the guidelines defined by US Food and Drug Administration. TIF was well distributed throughout the body compartments of tilapia judged by the apparent volume of distribution (Vd) >1 L/kg (6.69 L/kg PO and 1.78 L/kg IV). TIF had a short mean residence time (MRT; 22.82 h PO and 14.61 h IV) and quick total body clearance (CLb) (0.62 L kg−1 h−1 PO and 0.60 L kg−1 h−1 IV). The total area under the curve (AUCtot) of plasma were 32.25 μg h−1 ml−1 (PO) and 8.30 μg h−1 ml (IV), respectively, and the oral absolute bioavailability (F%) of TIF was calculated to be approximately 97.1%. For tissue distribution, high concentrations of TIF were found in kidney, and the longest MRT was recorded in bile. The withdrawal time (WT) of TIF in muscle, skin, liver, kidney, gill, and bile was 3.75 (4) and 1.79 (2), 1.77 (2) and 2.06 (3), 6.41 (7) and 1.97 (2), 6.95 (7) and 3.98 (4), 4.92 (5) and 2.36 (3), and 7.06 (8) and 6.16 (7) days after PO and IV administration, respectively. The present investigations indicated that TIF was quickly absorbed, well distributed, rapidly eliminated in tilapia, and it could serve as reference data for establishing use regimen and provide useful information for the further development of TIF in aquaculture.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Pharmacokinetics, bioavailability, and tissue disposal profiles of Tiamulin fumarate in Nile tilapia (Oreochromis niloticus) following oral and intravenous administrations

Liu

Cao

Song

et al. 2021

Vet Pharm & Therapeutics

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“…According to the available scientific literature, the antibiotic undergoes an extensive metabolic pathway in swine [26,27], but some of the aspects of its clinical pharmacology have not been adequately elucidated so far. Even though the accessible peer-reviewed publications present detailed information about modern analytical methods (including high-performance liquid chromatography-HPLC) developed for monitoring the antibiotic in several biological matrices, such as animal tissues [3,26,28], cow milk [29], honey [30], premixes and medicated feeds [31][32][33], soil [34], liquid manure [35], and swine wastewater [36], these methods have not yet been fully utilised in order to shed light upon the matter of some missing links in modern academic knowledge. Indeed, tiamulin serum and tissue concentrations in pigs following oral and intramuscular administration have been established empirically [3,27,37]; nevertheless, to the best of our knowledge, there is a paucity of information from experimental data on the passage of the antibiotic in question into sow milk.…”

Section: Introductionmentioning

confidence: 99%

Determination of Tiamulin Concentration in Sow Milk and in Sera of Suckling Piglets

Cybulski,

Gajda,

Bilecka

et al. 2023

Molecules

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Although modern analytical methods developed for monitoring antibiotics in several biological matrices are easily available, none of them have been applied to evaluate the transfer of tiamulin into sow milk. Therefore, this work was intended to analyse the concentrations of tiamulin in milk samples collected from lactating sows during and after a treatment consisting of three consecutive intramuscular applications of the antibiotic. The second aim of this investigation was to determine tiamulin concentrations in serum samples obtained from suckling piglets ingesting milk contaminated with the compound. Ultra-high-performance liquid chromatography coupled with tandem mass spectrometry (UHPLC-MS/MS) was used to quantify the analyte in both matrices. Our investigation proved tiamulin was transmitted into the milk of lactating sows. The mean concentration of the antibiotic among samples collected 3 h after administration was 1043 μg/L. The mean level of tiamulin on days 1 and 2 was 876 μg/L and 902 μg/L, respectively. The highest mean concentration of the antibiotic (1061 μg/L) was observed in samples collected on day 3. The mean concentration of the antibiotic in serum samples collected from 3-day-old piglets was 22.2 μg/L. The association between their body weight and serum tiamulin concentration was not statistically significant (p = 0.456).

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“…Because of its stability, crystalline structure, and water-soluble properties, this chemotherapeutic agent is ideally suited for administration to swine in feed, in drinking water, or by injection. Tiamulin in medicated formulations is quantitatively determined by reverse-phase liquid chromatography; the literature contains little information about this antibiotic [16,17].…”

Section: Introductionmentioning

confidence: 99%

Quantitative analysis of colistin and tiamulin in liquid and solid medicated premixes by HPLC with diode-array detection

et al. 2001

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SummaryCoJistin (COL) and tiamuJin (TML) are antibiotics used in veterinary practice. Diseases in animals are usually treated by adding the drug (liquid and/or sohd medicated premix) to animal feed. Two simple, inexpensive, and rapid methods have been developed for quantification of COL and TML in liquid and solid medicated premixes by HPLC with diode-array detection, on the basis of scanning in the UV range 200-380 nm. The wavelengths 206 and 208 nm were used for quantification of COL and TML, respectively. The total elution time was less than 15 min. When the applicability of the optimized method was tested by analysis of commercial feed premixes there was no interference from the matrix.

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Determination of tiamulin hydrogen fumarate in animal feeds using high-performance liquid chromatography

Cited by 8 publications

References 0 publications

Pharmacokinetics, bioavailability, and tissue disposal profiles of Tiamulin fumarate in Nile tilapia (Oreochromis niloticus) following oral and intravenous administrations

Pharmacokinetics, bioavailability, and tissue disposal profiles of Tiamulin fumarate in Nile tilapia (Oreochromis niloticus) following oral and intravenous administrations

Determination of Tiamulin Concentration in Sow Milk and in Sera of Suckling Piglets

Quantitative analysis of colistin and tiamulin in liquid and solid medicated premixes by HPLC with diode-array detection

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