In vitro and in vivo évaluation of naringin sustained-release pellets compared with immediate-release tablets

Naringin, which is widely present in foods of plant origin and traditional Chinese medicines, has been reported to possess various biological and pharmacological properties. Unfortunately, its short half-life (t1/2) restricts its use as an oral dosage form. In this study, immediate-release (IR) tablet and sustained-release (SR) pellet forms of naringin were prepared to solve this problem. Low-substituted hydroxypropyl cellulose (L- HPC) was chosen as a disintegrant in the IR tablets. In the SR pellets, microcrystalline cellulose (MCC) acts as a matrix former in wet extrusion processes. Sodium dodecyl sulfate (SDS) and sodium chloride (NaCl) increased the drug release rate. In vitro, pellets sustained a release effect for 12 h while the tablets released completely during the first half hour. In vivo, pellets showed a 2.7-fold higher t1/2, a lower Cmax and an equal Tmax compared with the tablets; and the relative bioavailability of SR pellets to IR tablets was 119.6%.