Abstract

Objective: The aim of the present investigation was to design and evaluate fast dissolving tablet (FDT) for the oral delivery containing solid dispersion of meclizine (MCZ) hydrochloride, an antiemetic drug.Methods: The solubility of meclizine was increased by preparing solid dispersions using mannitol as a carrier by fusion method. The prepared solid dispersion, was subjected for in vitro drug release, percent practical yield, drug content, infrared spectroscopy (IR), differential scanning calorimetry (DSC), scanning electron microscopy (SEM). Optimized solid dispersion was incorporated to prepare fast dissolving tablets. Preformulation studies were carried out on tablet blends. The prepared solid dispersion, as well as pure drug fast dissolving tablets, was evaluated for drug content, weight variation, hardness, friability, in vitro drug release, wetting time, disintegration time, water absorption ratio, in vitro dispersion time.Results: Meclizine pure drug, solid dispersions formulations SD1, SD3 and SD5 showed 12.8, 31.68, 38.92 and 53.28% cumulative drug release in phosphate buffer pH 6.8 after 60 min, respectively. Thus faster dissolution rate was exhibited by the solid dispersion containing 1:5 (w/w) ratio of meclizine: mannitol. Percent cumulative drug release for control and solid dispersion tablets after 60 min in phosphate buffer pH 6.8 was 92.04 and 98.2% respectively. The release of drug meclizine from best formulation SD5 FDT was found to be faster than pure drug FDT.Conclusion: Fast dissolving tablet of optimized solid dispersion showed better in vitro dissolution result then FDT of pure drug at the end of one hour.

Highlights

  • Solubility is an important physicochemical factor affecting absorption of the drug and its therapeutic effectiveness

  • Solubility measurements of meclizine pure drug and its solid dispersions are tabulated in table 2

  • From the solubility studies of the prepared solid dispersions in different media, it was found that as the increase in pH of the media increased the solubility i.e. meclizine showed superior solubility in phosphate buffer pH 6.8 when compared with others

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Summary

Introduction

Solubility is an important physicochemical factor affecting absorption of the drug and its therapeutic effectiveness. Formulation development scientists are focusing on the development of oral dosage forms of poor aqueous solubility drugs through various solubility enhancing approaches. Among these approaches, preparation of solid dispersion is one of the widely used approaches to enhance the solubility and dissolution rate of poorly watersoluble drugs. Solid dispersions of fenofibrate were prepared using PEG 6000, poloxamer 407 and a mixture of polyethylene glycol 6000 (PEG 6000) and poloxamer 407 [3]. The solid dispersion of terbinafine HCl was prepared with PEG 6000 and mannitol to increase water solubility [4]. Solid dispersions of carvedilol with polyvinyl pyrrolidone (PVP K30) were prepared to improve solubility [5]

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