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| Granulated pellet-containing tablets (GPCT) were prepared via a novel granulation technique, which laid the excipients on coated pellets and then compressed into GCPT after mixing with the cushioning fillers. The pharmacokinetics of doxycycline hydrochloride GPCT were evaluated to confirm the integrity of the coating film after compaction, with the coated pellets as a reference, containing equivalent doxycycline hydrochloride in the two formulations. The study was performed on six healthy beagles by a randomized-sequence, open-label, single-dose, two-period, crossover design with a 2-week washout period. Blood samples were collected and analyzed to calculate several pharmacokinetics parameters. The mean maximum plasma concentration (Cmax) for the test formulation and reference formulation were 2.73±0.22 mg/L and 2.94±0.47 mg/L, the mean time to reach Cmax (Tmax) were 6.67±0.47 h and 6.33±0.42 h, the AUC0-t were 68.42±6.94 mgoh/L and 72.87±12.51 mgoh/L, and the mean residence time (MRT) were 15.62±0.53 h and 15.26±0.79 h respectively. The pharmacokinetics analysis suggested that there was no significant difference regarding drug release properties, and the granulated pellet-containing tablets met the regulatory criteria for bioequivalence to the reference formulation of coated pellets in the healthy fasting beagles, from which the novel granulation technique might be proposed as an effective approach to prepare pellet-containing tablets without compromising the integrity of coating films. |
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| Keywords:Coated pellets; Granulation technique; Granulated pellet-containing tablets (GPCT); Pharmacokinetics; Doxycycline hydrochloride; Beagles |
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