Increased bioavailability of tylosin phosphate as in-feed medication formulated for long-action pellets in broiler chickens

Gutiérrez, Lilia; Alcalá, Yazmín; Bernad, María Josefa Bernad; López, Héctor Sumano

doi:10.3382/japr/pfx035

Cited by 5 publications

(8 citation statements)

References 14 publications

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“…The pharmacokinetic parameters obtained for the reference florfenicol as premix were very similar to what was achieved in other studies with soluble florfenicol. Minor differences can be attributed to the use of different bloodlines of chicken, different ages, feeding, and housing peculiarities ( 22 , 23 ). More efficient absorption of florfenicol, when prepared as FOLA pellets, was anticipated as sustained-release formulations tend to achieve better bioavailability values ( 20 , 24 ), and such behavior has already been obtained with FOLAs for doxycycline and tylosin in poultry ( 19 , 23 ).…”

Section: Discussionmentioning

confidence: 99%

Oral pharmacokinetics of a pharmaceutical preparation of florfenicol in broiler chickens

Gutierrez,

Guzman-Flores,

Monroy-Barreto

et al. 2023

Front. Vet. Sci.

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IntroductionThe use of florfenicol must follow particular pharmacokinetic/pharmacodynamic (PK/PD) ratios, i.e., it requires achieving serum concentrations at or slightly above the pathogen's minimum inhibitory concentration (MIC) during the dosing interval and that the ratio of area under the concentration vs. time curve (AUC)/MIC should be as high as possible (still undetermined for poultry). As an alternative to the standard soluble florfenicol that is administered to the flock through drinking water, florfenicol premix is often recommended as feed medication in Latin America. However, no particular pharmaceutical design has been proposed.MethodsThis study compared the PK of two preparations of florfenicol in broiler chickens and pondered the possibility of each covering the referred PK-PD ratios as predictors of clinical efficacy. The preparations comprise a pharmaceutical form as FOLA pellets (F = bioavailability; O = optimum; and LA = long-acting) and the premix formulation. The former are small colored pellets with vehicles and absorption enhancers of florfenicol designed for long action, and the latter is the reference premix of the antibiotic. First, these two pharmaceutical forms of florfenicol were administered as oral boluses (30 mg/kg), aided by a probe. In a second trial of the dosing form, both pharmaceutical preparations of florfenicol were administered in feed and ad libitum (110 ppm; ~30 mg/kg).ResultsIn both cases, FOLA-florfenicol presented much higher relative bioavailability (3.27 times higher) and mean better residence time than florfenicol premix (two times high when forced as bolus dose). Consequently, FOLA-florfenicol possesses better PK/PD ratios than less sensitive pathogens, i.e., E. coli. It is proposed that if a metaphylactic treatment of a bacterial outbreak in poultry is implemented with florfenicol prepared as FOLA, better PK/PD ratios will be obtained than those of standard florfenicol premix.DiscussionClinicians must confirm that feed consumption in the flock has not been affected by the particular disease if FOLA pellets of florfenicol are used.

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Section: Discussionmentioning

confidence: 99%

Oral pharmacokinetics of a pharmaceutical preparation of florfenicol in broiler chickens

Gutierrez,

Guzman-Flores,

Monroy-Barreto

et al. 2023

Front. Vet. Sci.

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“…For TYL, an alternation of decrease and increase of concentrations was observed. TYL absorption is relatively poor orally ( Gutiérrez et al, 2018 ), which would explain why high concentrations were detected on the first sampling point (d 5 post-treatment). Then, there was a decreasing trend in concentration on the second and third sampling points and then a slight increase on the fourth sampling point.…”

Section: Discussionmentioning

confidence: 99%

Determination of five antimicrobial families in droppings of therapeutically treated broiler chicken by high-performance liquid chromatography-tandem mass spectrometry

et al. 2021

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Antimicrobials are currently used in poultry for disease treatment. However, their excretion in bird feces may contaminate the environment. Considering this, the objective of this work was to quantify antimicrobials residues concentrations in therapeutically treated broiler chicken droppings throughout the post-treatment period. For this aim a multiresidue method using high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) was validated. Forty-eight male broiler chickens were distributed and treated with commercial formulations of 5 different antimicrobials. Results showed that oxytetracycline and 4-epi-oxytetracycline, presented the highest concentrations during all sampling period, detecting concentrations of 1471.41 µg kg −1 at the last sampling point (day 22 post-treatment). Florfenicol, tylosin, enrofloxacin, and ciprofloxacin were eliminated and detected in treated chicken droppings until d 18 post-treatment. Sulfachloropyridazine decrease gradually during post-treatment period until day 30. Results demonstrate that studied antimicrobials in treated chicken droppings were eliminated for prolonged periods, therefore becoming a significant route of residues dissemination into the environment.

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“…The pharmaceutical preparation of FOLA pellets tested here incorporate these features. The composition of FOLA pellets is designed to stay longer in the GI tract for better calcium absorption-particularly at night-time (13,14) while the addition of capsicum-oleoresin improves bioavailability. Capsicum-oleoresin contains a group of substrates known as capsaicinoids that are responsible for the pungent taste of chili peppers (Capsicum annuum and Capsicum frutescens).…”

Section: Discussionmentioning

confidence: 99%

“…It has been postulated that capsaicin molecules activate the secretion of substance P from nearby nerve terminals, and the capsaicins are inserted into the double lipid layer of cell membranes to modify the selective permeability of the ion channels (30). The blockage of the P-glycoprotein-mediated expulsion pumps in the GI tract cells has also been proposed as a mechanism of action (13,14); capsaicinoids are known to activate anandamide receptors at the intestinal level thus increasing glucose absorption (31). Capsicum-oleoresin has an antibacterial activity and decreases the fecal release of Salmonella sp.…”

Section: Discussionmentioning

confidence: 99%

“…Based on these issues, various modified-release feed preparations have been designed to increase the bioavailability of drugs and nutrients (Patent No.MX/a/2012/01,3222 and PCT/MX2013/000137; National Autonomous University of Mexico), and they are collectively referred to as FOLA (F = bioavailability; O = optimum; L = long; A = action) (13,14). They are small calcium-containing pellets and designed to remain in the GI tract for a longer time to enhance nighttime release of calcium and consequently F. In addition, capsicum-oleoresin can be added to FOLAs to increase the F. Capsicum-oleoresin increases in a concentration-dependant manner, and the amount of divalent and monovalent ions entering the cells containing the VR1 receptor (vanilloid receptor) in intestinal epithelial cells, and there is evidence that the oral administration of capsicum-oleoresin promotes the F of some drugs such as enrofloxacin in poultry (15) and fexofenadine in rats (16).…”

Section: Introductionmentioning

confidence: 99%

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Higher Bioavailability of Calcium in Chickens With a Novel In-Feed Pharmaceutical Formulation

et al. 2020

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Egg production and egg shell quality decrease toward the end of the first laying cycle in hens (approximately by week 80). Even so, farmers often choose to work a second cycle with them. Defective egg shell production has been mainly linked to a decrease in gastrointestinal absorption of calcium. Here we studied pharmaceutically-designed modified-release small pellets (FOLAs) containing calcium to improve calcium bioavailability (F). The influence of FOLA alone or with capsicum-oleoresin was studied in a total of 400 Bovans-White hens randomly divided into four groups of 20 laying hens each and with five replicates per group (n = 100) as follows: (1) control group (GC) receiving a diet containing basal levels of 4.1% of calcium-carbonate; (2) group GF treated as GC but with the same dose of calcium-carbonate in FOLA; (3) group GFc5 was treated as GF but with 6 ppm of capsicum-oleoresin (500,000 Scoville Heat Units [SHU]); and (4) group GFc10 treated as GFc5 but with 1,000,000 SHU capsicum-oleoresin. Plasma concentrations of calcium were determined during 5 days at predetermined times sampling more often on days 1 and 5 for blood plasma kinetics of calcium. Relative bioavailability (Fr) values based on the area under the serum calcium concentration vs. time curve (AUC) were obtained and compared to GC. The AUC was statistically different among all groups (P < 0.5), but the GFc10 had the greatest Fr (194%), with serum calcium concentrations ranging from 25.37 to 31.2 µg/dL. Calcium residence time (RT) between GC and GF showed no statistical differences while GFc5 and GFc10 had statistically superior RT values. Simultaneously, the number of shell-less eggs per group and their thickness was evaluated by utilizing the same groups but with 150 hens per group on 6 days. Shell-less eggs decreased to zero in Group GFc10 and produced eggs with the greatest shell thickness from day 2 onwards. The inclusion of calcium-carbonate in the pharmaceutical form FOLA induced higher serum calcium concentrations (GF, GFc5, and GFc10) particularly during the night-phase of the hen's cycle-this coincides with the time at which egg shell formation occurs.

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Increased bioavailability of tylosin phosphate as in-feed medication formulated for long-action pellets in broiler chickens

Cited by 5 publications

References 14 publications

Oral pharmacokinetics of a pharmaceutical preparation of florfenicol in broiler chickens

Oral pharmacokinetics of a pharmaceutical preparation of florfenicol in broiler chickens

Determination of five antimicrobial families in droppings of therapeutically treated broiler chicken by high-performance liquid chromatography-tandem mass spectrometry

Higher Bioavailability of Calcium in Chickens With a Novel In-Feed Pharmaceutical Formulation

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