Formulation and in vitro Evaluation of Fast Dissolving Tablets of Febuxostat Using Co-Processed Excipients.

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.

• Authors: Manpreet Kaur, Amit Mittal, Monica Gulati, Deepika Sharma, Rajesh Kumar
• Journal: Recent patents on drug delivery & formulation (Recent Pat Drug Deliv Formul) Vol. 14 Issue 1 Pg. 48-62 ( 2020) ISSN: 2212-4039 [Electronic] United Arab Emirates
• PMID: 31884935 (Publication Type: Journal Article)
• Copyright: Copyright© Bentham Science Publishers; For any queries, please email at [email protected].

Chemical References

• Excipients
• Gout Suppressants
• Tablets
• Febuxostat
• Cellulose
• Povidone
• microcrystalline cellulose

Topics

• Biological Availability
• Cellulose (chemistry)
• Chemistry, Pharmaceutical
• Drug Liberation
• Excipients (chemistry)
• Febuxostat (administration & dosage, chemistry)
• Gout Suppressants (administration & dosage, chemistry)
• Povidone (chemistry)
• Solubility
• Tablets