Formulation and Evaluation of Floating Sustain Release Pellets of Anti Gout Drug

Hiteshkumar A Patel,Upasana J Patel

doi:10.9734/jpri/2021/v33i60b34952

Abstract

Objective: The objective of this investigation was to formulate and evaluate effervescent pellets of febuxostat to achieve sustain release effect. Place and Duration of Study: APMC College of Pharmaceutical education and research, Department of Pharmaceutics, Himatnagar-383001, between June 2019 and July 2021. Materials and Methods: The gastro retentive effervescent pellets of febuxostat were formulated using Sodium CMC and HPMC K4M and HPMCK15M as a sustain release polymer. Pellets were prepared by extrusion- spheronization technique using microcrystalline cellulose as spheronizing agent and sodium bicarbonate and citric acid as a gas forming agent for effervescent pellets. The pellets were characterized with respect to their floating lag time, total buoyancy time and % cumulative drug release. Results and Discussion: DSC study showed that there was no change in the melting endotherm of the drug and drug-polymers mixture which means drug and polymers were compatible with each other. The optimized formulation B14 exhibits a floating lag time 4.00±0.004 sec. and cumulative % drug release at 12th hour 99.58±0.02. Scanning electron microscopy photomicrograph revealed that the surface was rough and pellets were spherical shaped in nature. Conclusion: Febuxostat sustain release pellets was successfully formulated and evaluated as effervescent pellets with gas former agents and sustain release polymer HPMC K15.

Highlights

Due to considerable therapeutic advantages such as patient compliance, simplicity of patient administration, and formulation flexibility, oral dosage forms have been created throughout the last four decades [1]
Carbon dioxide gas production occurs due to the reaction of bicarbonates and acid present in pellets, formed gas is entrapped in the polymers, which allows the systems to remain buoyant
The time between the introduction of the pellets into the medium and its buoyancy to the upper one third of the dissolution vessel and the time for which the formulation constantly floated on the surface of the medium were measured simultaneously

Summary

Introduction

Due to considerable therapeutic advantages such as patient compliance, simplicity of patient administration, and formulation flexibility, oral dosage forms have been created throughout the last four decades [1]. The Oral dosage forms have been developed from the past four decades due to their significant therapeutic advantages such as patient compliance, ease of patient administration and flexibility in formulation articulate floating drug delivery system (FDDS) was preferred over a single-unit system due to minimum inter and intrasubject variability in drug absorption and lower possibility of dose dumping [6]. FDDS are low density systems, which allows them to remain buoyant in the stomach for a prolonged period. Carbon dioxide gas production occurs due to the reaction of bicarbonates and acid present in pellets, formed gas is entrapped in the polymers, which allows the systems to remain buoyant. The FDDS are efficiently used to design sustained drug delivery systems and improve the oral bioavailability of drugs [7,8,9]

Methods

Results

Conclusion