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Preparation, characterization, and pharmacokinetics in swine of a florfenicol enteric formulation prepared using hot‐melt extrusion technology

Xu, Y., Wen, X., Feng, X., Liang, Z., Ye, X., Nie, H., Liao, X., Li, J., Zeng, Y., Tang, S., He, J.
Journal of veterinary pharmacology and therapeutics 2018 v.41 no.4 pp. 572-580
Fourier transform infrared spectroscopy, acetates, bioavailability, commercialization, differential scanning calorimetry, extrusion, florfenicol, manufacturing, pharmacokinetics, phosphates, polymers, succinic acid, swine, thermogravimetry
The objective of this work was to manufacture an enteric formulation of florfenicol (FF) using hot‐melt extrusion (HME) technology and to evaluate its in vitro dissolution and in vivo pharmacokinetics. For the HME process, hypromellose acetate succinate LG (HPMCAS‐LG) was the enteric polymer mixed with FF, and the two components were extruded with a standard screw configuration at a speed of 50 rpm. Differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), powder X‐ray diffraction (PXRD), and Fourier transform infrared spectroscopy (FT‐IR) were performed to characterize the HME extrudate. The release percentage of the enteric formulation in the acidic stage was <10% of the loaded FF, whereas that in the phosphate buffer stage was >80%. Pharmacokinetic evaluations in swine revealed that the enteric formulation had a longer t₁/₂λ and MRT than commercially available FF powder (FULAIKA®), indicating that the novel formulation exhibited enteric and sustained release properties. Compared with the commercial product, the relative bioavailability of the enteric formulation reached up to 117.2%. This study suggests that this formulation may have potential for future commercialization.