Abstract

FORMULATION AND EVALUATION OF ARIPIPRAZOLE ORAL DISINTEGRATING TABLET RESEARCH ARTICLE

Shikha Kuksal* and Dr. G. Gnanarajan

ABSTRACT

Aripiprazole is an antipsychotic medication, works by changing the actions of chemicals in the brain. It is used to treat the symptoms of psychotic conditions such as schizophrenia and bipolar disorder (manic depression). In order to formulate a newer aripiprazole immediate release of strength 30mg we performed the drug characterization study for the active pharmaceutical ingredient. Morphological characteristics, melting point, angle of repose, bulk density, tapped density, carr’s index, hausner ratio, sieve analysis, water content and moisture pick up were determined. The results obtained were satisfactory and within the specified limits. The drug characterization study was found to be useful for formulation and development of aripiprazole immediate release tablet. The aim of this study was to design a novel carrier for enhancing the bioavailability of the poorly water-soluble drug, aripiprazole (ARP). Silicosan, the applied carrier, was obtained by chemical interaction between tetraethyl orthosilicate (TEOS) and chitosan HCl. Different ARP-loaded silicosan particles were successfully prepared in absence and presence of one of the following surfactants; Tween 80, Poloxamer 407 and cetyltrimethylammonium bromide (CTAB). The prepared ARP-loaded silicosan particles were thoroughly investigated for their structures using FTIR, XRD, and DSC analysis as well as their particle size, zeta potential, flowability, drug content, and in vitro drug release efficiencies. The prepared ARPloaded silicosan particles were characterized by amorphous structure, high drug entrapment efficiency and a remarkable improvement in the release of aripiprazole in simulated gastric fluid. SEM and EDX revealed that the morphology and silica atom content in the prepared ARP-loaded silicosan particles were affected by the used surfactant in their formulations. The selected ARP-loaded silicosan particles were subjected to in vivo study using rabbits. The obtained pharmacokinetic results showed that the relative bioavailability for orally administered ARP-loaded silicosan particles (SC-2-CTAB) was 66% higher relative to the oral suspension (AUC0-10h was 16.38 ± 3.21 and 27.23 ± 2.35 ng.h/mL for drug powder and SC-2-CTAB formulation, respectively). The obtained results suggested the uniquestructured silicosan particles to be used as successful vehicle for ARP.

Keywords: Aripiprazole, antipsychotics, schizophrenia, drug characterization, immediate release tablets.