Pharmacokinetics of doxycycline and tissue concentrations of an experimental long-acting parenteral formulation of doxycycline in Wistar rats
Por:
Vargas-Estrada, D, Gutierrez, L, Juarez-Rodriguez, I, Sumano, H
Publicada:
1 ene 2008
Categoría:
Drug Discovery
Resumen:
Doxycycline hyclate (CAS 24390-14-5, doxycycline-h), an antibacterial with time-dependent action, was formulated as a non-irritating long-acting parenteral formulation based on a beta-cyclodextrin: poloxamer-based matrix (doxycycline-h-LA). Tissue and serum concentrations vs time profile were investigated after its subcutaneous injection to Wistar rats. Serum concentration profiles and key pharmacokinetic (PK) variables of doxycycline-h-LA were compared to the corresponding profiles and PK values obtained with an aqueous formulation of doxycycline-h administered either intramuscularly, orally or intravenously to Wistar rats. In all groups, the dose was 10 mg/kg. Doxycycline-h-LA showed outstanding bioavailability (951% or 477% if a correction formula is considered), as compared to the one obtained with an aqueous formulation (106-82%, respectively). Corresponding values for maximum serum concentration were 3.19 mu g/ml and 3.00 mu g/ml, respectively, and elimination half-lives were com
Filiaciones:
Vargas-Estrada, D:
Univ Nacl Autonoma Mexico, Fac Med Vet & Zootecnia, Dept Fisiol & Farmacol, Mexico City 04510, DF, Mexico
Gutierrez, L:
Univ Nacl Autonoma Mexico, Fac Med Vet & Zootecnia, Dept Fisiol & Farmacol, Mexico City 04510, DF, Mexico
Juarez-Rodriguez, I:
Univ Nacl Autonoma Mexico, Fac Med Vet & Zootecnia, Dept Fisiol & Farmacol, Mexico City 04510, DF, Mexico
Sumano, H:
Univ Nacl Autonoma Mexico, Fac Med Vet & Zootecnia, Dept Fisiol & Farmacol, Mexico City 04510, DF, Mexico
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