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

摘要

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 T max compared with the tablets; and the relative bioavailability of SR pellets to IR tablets was 119.6%.