Oral sustained-release suspension based on a novel taste-masked and mucoadhesive carrier-ion-exchange fiber

The purpose of this study was to evaluate the feasibility of ion-exchange fiber ZB-1 as a novel carrier in oral taste-masked mucoadhesive sustained-release suspensions. Propranolol (PPN) hydrochloride was selected as a model drug with good water solubility, short half life and bitter taste. The PPN-fiber complexes (PF) were prepared by a batch process and coated with Eudragit® RS100. Gamma scintigraphy was performed on fasted volunteers revealed about 30% ZB-1 and more than 50% coated ZB-1 were still remaining in the stomach at 6 h. In vitro results showed the releases of PF and coated PPN-fiber complexes (C-PF) were sustained. The release, drug content and particle size of C-PF were influenced by coat to core ratio, concentration of coating material and rotation rate. The suspension was stable after standing for 30 days in 0.5% Carbopol® with no release rate and taste changed. The administration of C-PF suspension to rats resulted a significant different (P < 0.05) improvement of the plasma drug level and prolongation of the release. However, because of the burst effect, the Cmax values of PF suspension didn't differ from drug solution (P > 0.05). Furthermore, a linear relationship between in vitro dissolution and in vivo absorption was observed.

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