DEVELOPMENT AND EVALUATION OF IMMEDIATE RELEASE TABLETS OF TENOFOVIR DISOPROXIL FUMARATE

The main aim of the present study was to develop and evaluate Tenofovir Disoproxil Fumarate (300mg) film coated tablets and to compare with the marketed product. A successful immediate release drug delivery system of Tenofovir disoproxil fumarate was prepared with immediate release mechanism that gives immediate onset of action and compared with that of innovator product VIREAD. Tenofovir disoproxil fumarate belongs to BCS class III drug possesing longer half life; hence it was good candidate for immediate release drug delivery system. Compatibility studies for drug and excipients mixture was done by performing DSC study. Preformulation studies such as Organoleptic characteristics (white to off white crystalline powder), solubility, Loss on drying (2.76), melting point (115.2C) were performed. Flow properties such as bulk density (0.431-0.478gm/cc), tapped density (0.57-0.61gm/cc), Compressibility index (10-29%), Hausner’s ratio (1.2-1.57) and angle of repose (25-50) were evaluated. F1 and F2 formulations failed in precompression parameters for the lubricated blend and F3 to F7 formulations passed the precompression parameters and possess good flow properties. Compared to dry granulation and direct compression, wet granulation was found to be suitable for the formulation of immediate release Tenofovir Disoproxil Fumarate tablets. Formulations were prepared by wet granulation and composed of Crospovidone, Croscarmellose sodium and calcium carboxy methyl cellulose as disintegrants with other excipients like lactose as diluents, povidone K-30, HPC and Pregelatinised starch as binder, Magnesium stearate as a lubricant. The tablets were coated with Opadry blue II suspension in a conventional coater. All the tablet formulations were evaluated for the appearance( blue coloured oval shaped coated), dimension(6.04-6.12mm), hardness(5-6kg/cm2), percentage friability(0.09-0.12%), weight variation(1.29-1.35%), drug content(98.75-101.2%) and In-vitro drug released profile. On the performance with respect to disintegration time and the drug release characteristics, the formulation F5 was selected as the best formulation as compared with innovator product. This formulation showed immediate released rate that showed 97.45% release within 45 min. The study revealed that by interchanging the disintegrant, drug release rate from tablets depends upon type of disintegrant.