Abstract

Objective: The study aims for the design and evaluation of floating tablets of emtricitabine (EMT), post oral administration to sustain the release and enhance gastric residence time (GRT).
 Methods: EMT is a nucleoside reverse-transcriptase inhibitor for the prevention and treatment of human immunodeficiency virus (HIV) infection. The investigation was considered to formulate a floating tablet of EMT with various agents. The formulation included with various concentrations of hydroxypropyl methylcellulose (HPMC) k4m, ethylcellulose, microcrystalline cellulose, polyvinylpyrrolidone (PVP) by wet granulation method. Various parameters for the prepared formulations were evaluated for weight variation, thickness, hardness, friability, floating lag time (FLT), total floating time (TFT), swelling index, in vitro drug release, and fourier-transform infrared spectroscopy (FTIR) studies.
 Results: The best formulation F1 exhibited 88.28% release in 24 h duration, with a floating lag time of 7 min and swelling index of 52.1% and drug content was determined to be 98.27%. The release mechanism was determined to be first order with higuchi release kinetics displaying diffusion along with the dissolution of the EMT from the tablet by non fickian mechanism.
 Conclusion: EMT tablets showed an increased GRT with a sustained release for 24 h thereby allowing a better window for absorption consequently improve the therapeutic effect of the drug.

Highlights

  • Sustained drug delivery system yields a perpetual oral delivery of drugs at conceivable and reproducible kinetics for a preordained period throughout the course of gastrointestinal (GI) transit [1]

  • Conventional oral dosage forms agonize from mainly two predicaments the short gastric residence time (GRT) and unpredictable gastric emptying time

  • EMT and hydroxypropyl methylcellulose (HPMC) k4m were procured from yarrow chem products (Mumbai, India), ethylcellulose and magnesium stearate were procured from loba chemie pvt. ltd. (Mumbai, India), microcrystalline cellulose, PVP and talc, were purchased from molychem (Mumbai, India), sodium hydrogen carbonate was procured from finar chemicals pvt

Read more

Summary

Introduction

Sustained drug delivery system yields a perpetual oral delivery of drugs at conceivable and reproducible kinetics for a preordained period throughout the course of gastrointestinal (GI) transit [1]. Conventional oral dosage forms agonize from mainly two predicaments the short GRT and unpredictable gastric emptying time. A relatively short GI transit time of most drug products hinder the formulation of single daily dosage forms. Altering the gastric emptying can overwhelm these problems. It is desirable, to formulate a sustained release dosage form that gives an extended GI residence time. One of the most workable approaches for achieving a sustained and predictable drug delivery profiles in the GI tract is to control the GRT using gastro retentive dosage forms that offer a novel and better option for drug delivery [2]

Methods
Results
Conclusion
Full Text
Published version (Free)

Talk to us

Join us for a 30 min session where you can share your feedback and ask us any queries you have

Schedule a call