Pharmacokinetics after administration of an injectable experimental long-acting parenteral formulation of doxycycline hyclate in goats

Estrada, Dinorah Vargas; Gutiérrez, Lilia; Juárez, Iván; Gonzalez, Francisco; López, Héctor Sumano

doi:10.2460/ajvr.69.8.1085

Cited by 16 publications

(24 citation statements)

References 28 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Compared with other tetracyclines, doxycycline has better pharmacokinetics characteristics in mammals, including superior absorption rate following oral administration and the increased distribution to various body tissues (Aronson, ; Riond & Riviere, ). Pharmacokinetics of doxycycline in different species have been studied, such as in dogs (Gutierrez et al ., ), cats (Hartmann et al ., ), chicken (Yang et al ., ), pigs (Yang et al ., ), horses (Zozaya et al ., ), sheep (Castro Robles et al ., ), goats (Vargas et al ., ), and calves (Vargas‐Estrada et al ., ). However, pharmacokinetics profiles of doxycycline in fish species, especially its oral bioavailability, are very limited.…”

Section: Introductionmentioning

confidence: 99%

Pharmacokinetics of doxycycline in tilapia (Oreochromis aureus × Oreochromis niloticus) after intravenous and oral administration

Yang

et al. 2014

Vet Pharm & Therapeutics

View full text Add to dashboard Cite

The pharmacokinetics of doxycycline was studied in plasma after a single dose (20 mg/kg) of intravenous or oral administration to tilapia (Oreochromis aureus × Oreochromis niloticus) reared in fresh water at 24 °C. Plasma samples were collected from six fish per sampling point. Doxycycline concentrations were determined by high-performance liquid chromatography with a 0.005 μg/mL limit of detection, then were subjected to noncompartmental analysis. Following oral administration, the double-peak phenomenon was observed, and the first (Cmax1 ) and second (Cmax2) peaks were 1.99 ± 0.43 μg/mL at 2.0 h and 2.27 ± 0.38 μg/mL at 24.0 h, respectively. After the intravenous injection, a Cmax2 (12.12 ± 1.97 μg/mL) was also observed, and initial concentration of 45.76 μg/mL, apparent elimination rate constant (λz) of 0.018 per h, apparent elimination half-life (t1/2λz) of 39.0 h, systemic total body clearance (Cl) of 41.28 mL/h/kg, volume of distribution (Vz) of 2323.21 mL/kg, and volume of distribution at steady-state (Vss) of 1356.69 mL/kg were determined, respectively. While after oral administration, the λz, t1/2λz, and bioavailability of doxycycline were 0.009 per h, 77.2 h, and 23.41%, respectively. It was shown that doxycycline was relatively slowly and incompletely absorbed, extensively distributed, and slowly eliminated in tilapia, in addition, doxycycline might undergo enterohepatic recycling in tilapia.

show abstract

Section: Introductionmentioning

confidence: 99%

Pharmacokinetics of doxycycline in tilapia (Oreochromis aureus × Oreochromis niloticus) after intravenous and oral administration

Yang

et al. 2014

Vet Pharm & Therapeutics

View full text Add to dashboard Cite

show abstract

“…Injection of an aqueous preparation of DOX-hyclate is not an option because as it occurs with other tetracyclines, this drug is remarkably tissue-irritating [1,8,10], a fact that also explains the lack of an injectable long-acting (LA) preparation. A possible exception can be found in the poloxamer β-cyclodextrin-based matrix, long acting formulation of doxyclyne (DOX-h-LA) that has been proposed for cows [11] and goats [12]. In these trials both, favorable pharmacokinetics and a minimum irritation at the injection site were found.…”

Section: Introductionmentioning

confidence: 99%

Pharmacokinetics of an injectable long-acting formulation of doxycycline hyclate in dogs

et al. 2012

Self Cite

View full text Add to dashboard Cite

Based on its PK/PD ratios, doxycycline hyclate (DOX-h), a time-dependant antibacterial, is ideally expected to achieve both sustained plasma drug concentrations at or slightly above the MIC level for as long as possible between dosing intervals. Pursuing this end, a poloxamer-based matrix was used to produce a long-acting injectable preparation (DOX-h-LA) and its serum concentrations vs. time profile investigated after its SC injection to dogs (≤ 0.3 mL per injection site), and results compared with the oral (PO) and IV pharmacokinetics of DOX-h, prepared as tablet or as freshly made solution. A crossover (4 x 4 x 4) study design was employed with 12 Mongrel dogs, with washout periods of 21 days, and at dose of 10 mg/kg in all cases. DOX-h-LA showed the greatest values for bioavailability (199.48%); maximum serum concentration (Cmax) value was 2.8 ± 0.3 with a time to reach Cmax (Tmax) of 2.11 ± 0.12 h and an elimination half-life of 133.61 ± 6.32 h. Considering minimum effective serum concentration of 0.5 μg/mL, a dose-interval of at least 1 week h can be achieved for DOX-h-LA, and only 48 h and 24 h after the IV or PO administration of DOX-h as a solution or as tablets, respectively. A non-painful small bulge, apparently non-inflammatory could be distinguished at injection sites. These lumps dissipated completely in 30 days in all cases.

show abstract

“…The agar diffusion technique used here to determine serum and tissue concentrations of doxycycline is a dependable method, allowing pharmacokinetic data to be extrapolated to antibacterial activity with certainty (Santos et al, 1996;Vargas et al, 2008).…”

Section: Discussionmentioning

confidence: 99%

Bio-equivalence study of two oral doxycycline formulations (doxycycline kela 75%Â® and mebcodox 75%Â®) in broiler Chickens

Elkomy¹,

Aboubakr²

2020

IJPT

View full text Add to dashboard Cite

The present study was designed to assess the comparative bio-equivalence of Doxycycline Kela 75%® and Mebcodox 75%® in healthy broiler chickens after oral administration of both products in a dose of 20 mg doxycycline base/kg.b.wt. Twenty four broiler chickens were divided into two groups. The first group was designed to study the pharmacokinetics of Doxycycline Kela 75%®, while the 2nd group was designed to study the pharmacokinetics of Mebcodox 75%®. Each broiler chickens in both groups were orally administered with 20 mg doxycycline base/kg.b.wt. Blood samples were obtained from the wing vein and collected immediately before and at 0.08, 0.16, 0.25, 0.5, 1, 2, 4, 6, 8, 12 and 24 hours after a single oral administration The disposition kinetics of Doxycycline Kela 75%® and Mebcodox 75%® following oral administration of 20 mg doxycycline base/kg.b.wt. revealed that the maximum blood concentration [Cmax] were 3.35 and 3.28 μg/ml and attained at [tmax] of 0.97 and 0.99 hours, respectively.In conclusion: Mebcodox 75%® is bioequivalent to Doxycycline Kela 75%® since the ratios of Cmax, AUC0-24 and AUC0-∞ (T/R) was 0.97, 0.95 and 0.94 respectively. These are within the bioequivalence acceptance range. Mebcodox 75%® and Doxycycline Kela 75%® are therefore bioequivalent and interchangeable.

show abstract

Pharmacokinetics after administration of an injectable experimental long-acting parenteral formulation of doxycycline hyclate in goats

Cited by 16 publications

References 28 publications

Pharmacokinetics of doxycycline in tilapia (Oreochromis aureus × Oreochromis niloticus) after intravenous and oral administration

Pharmacokinetics of doxycycline in tilapia (Oreochromis aureus × Oreochromis niloticus) after intravenous and oral administration

Pharmacokinetics of an injectable long-acting formulation of doxycycline hyclate in dogs

Bio-equivalence study of two oral doxycycline formulations (doxycycline kela 75%Â® and mebcodox 75%Â®) in broiler Chickens

Contact Info

Product

Resources

About