Abstract
Objective: The rationale of the current research work was to formulate and evaluate fast-dissolving tablets of doxazosin mesylate with minimum disintegration time and improved dissolution efficiency using solid dispersion method.Methods: Solid dispersions of doxazosin mesylate and polyethylene glycol 8000 in different ratios were prepared using the kneading method. The prepared solid dispersions were subjected to drug interaction and dissolution studies to select the effective solid dispersion for the formulation of fast-dissolving tablets. Fast dissolving tablets containing drug-polyethylene glycol 8000 solid dispersion (1:3) were prepared using various super-disintegrants such as crospovidone, croscarmellose sodium, mixture and coprocessed crospovidone and croscarmellose sodium in concentration range of 2% and 5% by direct compression technique. The prepared formulations (F1–F16) were evaluated for post compression parameters; hardness, thickness, friability, wetting time, disintegration time, and in–vitro drug release.Results: Drug doxazosin mesylate showed enhanced aqueous solubility of 13.3µg/ml in the presence of polyethylene glycol 8000. Differential scanning calorimetery and Fourier transform infrared spectroscopy studies confirmed no interaction between drug and polyethylene glycol 8000and, drug-polyethylene glycol 8000 solid dispersion showed cumulative drug release of 44.48% in 60 min. Formulated FDT of drug-polyethylene glycol 8000 solid dispersion, containing coprocessed mixture of crospovidone and croscarmellose sodium (5%) exhibited disintegration time of 14.5s with percentage cumulative release of 92.46% in 60 min.Conclusion: The work reasonably concludes that for the formulated doxazosin mesylate-fast dissolving tablets, disintegration time was effectively reduced by the presence of coprocessed mixture of crospovidone and croscarmellose sodium and dissolution efficiency was improved by preparation of solid dispersion with polyethylene glycol 8000.
Highlights
To overcome constraints of oral route for geriatric, pediatric, and travelling patients, modern advances in the pharmaceutical technology have prompted scientists to develop fast dissolving tablets (FDT) with improved patient compliance and convenience.FDT are the most extensively employed commercial product and become a promptly growing field in the pharmaceutical industry
The work reasonably concludes that for the formulated doxazosin mesylate-fast dissolving tablets, disintegration time was effectively reduced by the presence of coprocessed mixture of crospovidone and croscarmellose sodium and dissolution efficiency was improved by preparation of solid dispersion with polyethylene glycol 8000
The spectra are shown in fig. 2 for pure Doxazosin mesylate (DM), polyethylene glycol (PEG) 8000 and DM-PEG 8000 solid dispersion respectively
Summary
FDT are the most extensively employed commercial product and become a promptly growing field in the pharmaceutical industry. They are the oral solid dosage form, which dissipate instantaneously in the oral cavity when placed upon the tongue and swallowed without the aid of water. Solid dispersion is one of the accepted approaches for dissolution enhancement They are molecular mixtures of poor water soluble drugs with hydrophilic carriers prepared by solvent evaporation and melting method. They provide better wettability and dispersibility as the drug is in its supersaturated state due to forced solubilisation in the hydrophilic carriers. Literature supports many successful commercial products based on solid dispersion techniques. [9, 10]
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