Formulation design and optimization of novel mouth dissolving tablets for venlafaxine hydrochloride using sublimation technique

Abstract

AimVenlafaxine hydrochloride, commonly used as antidepressant, has poor bioavailability due to extensive first pass metabolism. The objective of present study is to develop novel method of preparing compressed tablets for venlafaxine hydrochloride with high porosity which dissolves rapidly in mouth, using camphor as sublimating agent. MethodsA 32 factorial design was used to investigate effect of amount of camphor and superdisintegrant namely indion 234 as independent variable. Friability, disintegration time, percent drug release were taken as dependent variables. Different concentrations (3%, 4%, 5%)of superdisintegrant indion 234 and camphor (5%, 10%, 15%) were used respectively. Tablets were prepared by direct compression method. Pearlitol SD-200 was used as bulking agent. The compressed tablets were dried for 6 h to allow sublimation of camphor to increase the porosity of the tablets to improve their dissolution. The tablets were evaluated for hardness, thickness, friability, weight variation, porosity, wetting time, disintegration time, drug content and in-vitro drug release. Drug-excipient interaction was investigated by FTIR study. Optimized formulation was evaluated for stability as per ICH guideline. ResultsAll tablets had hardness 3–3.5 kg/cm2 and friability of all formulations was less than 1.08%. Weight variation and drug content were within USP limits. FTIR study revealed no drug-excipient interaction. SEM study showed the porous surface morphology of tablets. A stability study for optimized F3 formulation as per ICH guideline for 90 days showed no changes in drug content. ConclusionTherefore, it may be concluded that developed novel method of preparing compressed tablets for venlafaxine hydrochloride with high porosity which dissolve rapidly in mouth, could be industrially feasible.