Abstract

FORMULATION DEVELOPMENT AND EVALUATION OF BILAYER TABLETS OF SOFOSBUVIR FOR EFFECTIVE TREATMENT OF CHRONIC HEPATITIS C USING NATURAL POLYMERS

Madankumar Daulatrao Kadwe*, Hemant Kumar Sharma, Prabhakar Budholiya

College of Pharmacy, Sri Satya Sai University of Technology and Medical Sciences, Bhopal (M.P)

ABSTRACT

Formulation development is an important part of drug design and development. Bioavailability and bioequivalence are totally dependent on formulation development. Now-a-days formulation development is done by following QbD (Quality by Design). The purpose of this work is to develop bilayer tablets of Sofosbuvir by using natural polymers, which is an anti-viral drug. It is used to treat Hepatitis C. As it is a fatal disease which damages the liver to an extent that one may die suffering from this disease. So development of a lifesaving drug was very much necessary for this disease. Hence a new approach is tried that gives one immediate release dose and a sustained release dose in single dosage form call bilayer tablets. Immediate release layer delivers the initial dose, it contains superdisintegrant which increase drug release rate whereas sustained release layer gastro retentive by using natural polymers and releases drug at sustained manner for prolonged period. A direct compression method was used to formulate 8 batches. Superdisintegrants like sodium starch glycolate, croscarmellose sodium, crospovidone sodium was used for immediate release layer and xanthan gum, gaur gum, karaya gum, PVP K30 like natural polymers were used in gastro retentive sustained release layer. The powders were evaluated for their flow properties and the finished tablets were evaluated for their physical parameters. A simple visible spectrophotometric method was employed for the estimation of Sofosbuvir at 264 nm and Beer’s law is obeyed in the concentration range of 5-25 µg/ml. The prepared gastro retentive tablets were evaluated for general appearance, thickness and diameter, drug content, hardness, friability, uniformity of weight and in vitro dissolution studies. Successful formulation was developed having disintegration Time 100±4 sec and drug release was sustained up to 12 hrs. A biphasic drug release can be obtained by using bilayer tabletting technology which involved compression of immediate and sustained release layer together. Bilayered floating tablets with release characteristics offer critical advantages such as, site specificity with improved absorption and efficacy. This technology can be inculcated to various medicaments which have stomach as the major site of absorption.

Keywords: Bilayer floating tablets, Sofosbuvir, Biphasic drug release, Bioavailability, Xanthan gum, Gaur gum, Karaya gum.