Title:Formulation and in vitro Evaluation of Fast Dissolving Tablets of Febuxostat Using Co-Processed Excipients
VOLUME: 14 ISSUE: 1
Author(s):Manpreet Kaur, Amit Mittal, Monica Gulati, Deepika Sharma and Rajesh Kumar*
Affiliation:Department of Pharmacy, Rayat Bahra Institute of Pharmacy, V. Bohan, Hoshiarpur, Punjab 146004, Department of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab 144411, Department of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab 144411, Department of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab 144411, Department of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab 144411
Keywords:Bioavailability, co-processed excipients, crospovidone, fast dissolving tablets, febuxostat, gout, microcrystalline
cellulose.
Abstract:
Background: Febuxostat is a novel, orally-administered, powerful, non-purine, xanthine
oxidase inhibitor used for treating gout and ceaseless tophaceous gout. The drug exhibits low bioavailability
(about 49%) which is ascribed to its dissolution rate-limited absorption.
Objective: The current work is aimed to provide a novel strategy to improve the dissolution profile and
thus, the bioavailability of Febuxostat.
Methods: Formulation of Fast Dissolving Tablets (FDT) is anticipated to provide immediate release of
the drug, which in turn, will improve its dissolution profile to provide the initial surge in plasma concentration
required in an acute gout attack. Incorporation of co-processed excipients in a tablet is
known to improve the compressibility and disintegration characteristics of the tablets, which, in turn,
result in enhanced in vitro drug release and improved bioavailability. A combination of crospovidone
(it rapidly wicks saliva into the tablet to create the volume development and hydrostatic weight important
to give quick disintegration) and microcrystalline cellulose (a highly compressible ingredient with
good wicking and absorbing capacity) was, therefore, used as co-processed excipients.
Results: The tablets were prepared by direct compression technique with the application of a 32 randomized
full factorial design. The prepared tablets were able to release more than 80% of the drug
within 10 minutes of the start of dissolution testing and were able to show a better drug release profile
in comparison to available marketed formulation.
Conclusion: So, it can be concluded that the developed fast release formulation was found to exhibit
convincing in vitro results and may prove a boon in the treatment of acute gout attack after establishing
in vivo potential.
