Preparation and in vitro Characterisation of Solid Dispersion Floating Tablet by Effervescent Control Release Technique with Improved Floating Capabilities

Peeush Singhal,Vijay Jyoti Kumar,Rajneesh Dutt Kaushik

doi:10.5772/intechopen.92187

Peeush Singhal, Vijay Jyoti Kumar + Show 1 more

Open Access

https://doi.org/10.5772/intechopen.92187

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Abstract

In this Research, an effort has been done for the development of effervescent controlled release floating tablet (ECRFT) from solid dispersions (SDs) of diclofenac sodium (DS) for upsurge the solubility and dissolution rate. ECRFT of DS was prepared by using SDs of DS and its SDs prepared with PEG as carrier using thermal method (Simple fusion). SDs of DS were formulated in many ratio (1:1, 1:2, 1:3 and 1:4). Prepared SDs was optimized for its solubility, % drug content and % dissolution studies. Tablets were formulated by using optimized SDs products and all formulation was evaluated for various parameters. A clear rise in dissolution rate was detected with entirely SD, amid that the optimized SD (SD4) was considered for ECRFT. Among all the tablet formulations, its F3 formulation was better in all the terms of pre compression and post compression parameters. It had all the qualities of a good ECRFT, based on this F3 formulation was selected as the best formulation. Data of in vitro release was fitted in several kinetics models to explain release mechanism. The F3 formulation shows zero order release. From this study we can concluded that ECRFT containing SDs of DS can be successfully used for achieving better therapeutic objective.

Highlights

Diclofenac sodium (DS) is an effective NSAID with high affinity for both COX-1 and COX-2 receptors and it is one and only maximum frequently recommended drugs in India for the cure of pain, inflammation and joint stiffness caused by arthritis
When the spectra were compared it was found that there was no shifting of functional peaks and no overlapping of characteristic peaks and there was no appearance of new peaks
The prepared SDs and physical mixtures (PM) of DS were evaluated for saturation solubility, pH dependent solubility; percent drug content and in vitro dissolution studies

Summary

Introduction

Diclofenac sodium (DS) is an effective NSAID with high affinity for both COX-1 and COX-2 receptors and it is one and only maximum frequently recommended drugs in India for the cure of pain, inflammation and joint stiffness caused by arthritis. The pharmacokinetic profile of DS showed that the half-life is about $1.2–2 h and there is a requirement of frequent dosing (3–4 tablets daily) [5] but this requirement of frequent dose is very dangerous for patients because due to this frequent dosing fluctuation in plasma drug level in body and need constant monitoring of patient for adjustment of dose regimen. That is why this reason may support faster absorption of drug in stomach with higher concentrations for bioavailability improvement. The emphasis of the current research was to increase the release rate and bioavailability of DS through preparing ECRFT (effervescent control release floating tablets) with dual approach [9] using solid dispersion product of DS in order to regulate the drug release and make available security from first pass metabolism

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