ABSTRACT
The objective of the work was to formulate and evaluate anti-epileptic tablets of
Gabapentin using various super disintegrants in different ratios. Tablets were prepared by direct
compression method using Mannitol, Menthol, Sodium saccharin, Magnesium stearate and talc.
The drug-polymer incompatibility was ruled out by FTIR studies. Evaluation studies like drug
content, in-vitro drug release, disintegration time, hardness, friability, wetting time and weight
variation for formulations were performed. From the FTIR studies, the drug-polymer
compatibility was confirmed, that, the polymer did not interfere with the drug used. In-vitro drug
released varied from 95-99.64 %. The disintegration time was found to be in range of to 2.1-2.8
min. The hardness and friability was found to be in range 3.2-3.8 kg/cm2 & 0.32-0.69%
respectively. The formulation F12 since it showed good In vitro drug release of 99.64 % release
at the end of 30 min. From this study it could be concluded that the formulated Gabapentin
tablets by using various super disintegrates showed good and effective release with maximum
concentration of polymer.
Orally disintegrating tablets (ODTs) is uncoated tablets intended to be placed in the mouth
where they disintegrate within 3 min and disperse rapidly before being swallowed.6161 The
benefits of ODTs is to improve patients compliance, rapid onset of action, good stability and
increased bioavailability which make these tablets popular as a dosage form of choice in the
current market.6161
The basic approach in development of FDT is the use of superdisintegrants like MCC,
SSG, CP and CC etc, which provide instantaneous disintegration of tablet after putting on
tongue, their by release the drug in saliva1.
Gabapentin interacts with cortical neurons at auxillary subunits of voltage-sensitive
calcium channels. Gabapentin increases the synaptic concentration of GABA, enhances GABA
responses at non-synaptic sites in neuronal tissues, and reduces the release of mono-amine
neurotransmitters. One of the mechanisms implicated in this effect of gabapentin is the reduction
of the axon excitability measured as an amplitude change of the presynaptic fibre volley (FV) in
the CA1 area of the hippocampus. This is mediated through its binding to presynaptic NMDA
receptors. Other studies have shown that the antihyperalgesic and antiallodynic effects of
gabapentin are mediated by the descending noradrenergic system, resulting in the activation of
spinal alpha2-adrenergic receptors. Gabapentin has also been shown to bind and activate the
adenosine A1 receptor2. MATERIALS AND METHODS: FORMULATION AND EVALUATION OF GABAPENTIN TABLETS: Formulation of Gabapentin tablets:
For the preparation of the Gabapentin as tablet, various super disintegrants were used such
as MCC, SSG, CP, CC and other excipients such as menthol as flavoring agent, sodium
saccharine, methyl paraben and mannitol. The composition of tablet formulation containing
Gabapentin is given in table 1 and 2. Direct Compression