FORMULATION DEVELOPMENT AND EVALUATION OF FAST DISSOLVING TABLETS OF PREGABALIN

Jitendra Singh*, Neelesh Choubey, Hemant Kumar Sharma, Prabhakar Budholiya, Geeta Parkhe

Sri Satya Sai University of Technology and medical Science, Sehore, Madhya Pradesh, India

ABSTRACT

Pregabalin (PRE) is a structural analogue of γ-amino butyric acid, which is used to treat refractory partial seizures, diabetic neuropathy, post-therapeutic neuralgia, and social anxiety disorders. Its main site of action appears to be the α2-δ subunit of the voltage-dependent calcium channels that are widely distributed throughout the peripheral and central nervous system. The concept of formulating fast dissolving tablets containing PRE offers a suitable and practical approach in serving desired objective of faster disintegration and dissolution characteristics with increased bioavailability. Fast dissolving tablets of PRE were prepared by direct compression methods and blend was evaluated for the pre-compression parameters such as bulk density, compressibility, angle of repose etc. The tablets were prepared by using Croscarmellose sodium, Crospovidone and sodium starch glycolate, as superdisintegrants in different concentration along with microcrystalline cellulose. Total six formulations were prepared and evaluated for hardness, friability, weight variation, content uniformity, wetting time, water absorption ratio, disintegration time and invitro drug release. In-vitro dissolution studies are performed by using phosphate buffer pH 6.8 at 75 rpm by paddle method. Overall, the formulation F4containing of Croscarmellose sodium was found to be promising and has shown a disintegration time 45 sec. The stability studies were performed for two months (accelerated studies) as per ICH guidelines. The optimized formulation (F4) showed no significant variations for the tablets parameters and it was stable for the specified time period. Thus results conclusively demonstrated successful masking of taste and fastest disintegration of the formulated tablets in oral cavity.

Keywords:

Pregabalin, fast dissolving tablets, γ-amino butyric acid, Super-Disintegrant, Pre-compression