A simple and novel method for preparing the taste masking levofloxacin microsphere suspension

摘要

A taste masking levofloxacin resinate microsphere suspension was prepared. At first, levofloxacin-resinates were prepared by?both?bath and column methods in?HCl solution (0.01 mol/L)?before they were?used as cores to prepare?the?suspension. The drug loading amount in the drug resinates made by bath method and column method was 33.2 ± 0.8 and 45.7 ± 0.6% (n = 6),?respectively. The average diameter of the drug resinates was 120 μm. The scanning electron microscopy (SEM) results showed?that there?was?no drug crystallization on the surface of the drug resinates. The?in vitro?drug release results showed that the drug resinates did not release levofloxacin in water, and?the drug released faster?with the increase of ion concentration in the dissolution mediums. The taste masking evaluation of the suspension was carried out?among?6 volunteers; taste evaluation revealed that the suspension masked the bitter taste of the drug completely.?Lastly,?in vivo?pharmacokinetics evaluation was carried out in beagle dogs. The?in vivo?pharmacokinetics test showed that the suspension and reference (levofloxacin tablets) had no significant differences for?Cmax?and?AUC0-36h, but indicated?a?significant difference for?Tmax.?The?Tmax?decreased from 1.83 h (reference) to 1 h (test), indicating a faster release property?in vivo.