Dissolution rate enhancement of irbesartan and development of fast-dissolving tablets

Authors

Abstract

Objective
The objective of the present investigation was to enhance the solubility and dissolution rate of poorly soluble drug irbesartan by preparing it as solid dispersions and formulating it as fast-dissolving tablets (FDTs) using various excipients.
Background
Irbesartan is poorly soluble in water, and this low aqueous solubility in addition to its poor wettability leads to poor bioavailability of the drug.
Materials and methods
Solid dispersions were prepared using Soluplus, PEG 6000, and Kollidon as carriers. The dispersions were prepared using the solvent evaporation and kneading methods in a 1:1 ratio of drug and carrier. These formulations were characterized for solid state properties using X-ray powder diffraction and Fourier transform infrared spectroscopy spectral studies. Formulations were further evaluated for dissolution.
Results
The aqueous solubility of irbesartan in solid dispersions was improved by the presence of polymer Soluplus when compared with other carriers. Solid state characterization indicated that irbesartan was present as amorphous material in the formulation with carrier. This was due to efficient entrapment of the drug in polymer matrix. Thus, the solid dispersion prepared with Soluplus would be useful for delivering poorly soluble irbesartan with enhanced solubility and dissolution rate. Furthermore, the solid dispersions that were formulated as FDTs using superdisintegrants showed faster drug release with increased dissolution rate.
Conclusion
FDTs containing irbesartan solid dispersions prepared using the solvent evaporation method and croscarmellose sodium as superdisintegrant showed faster disintegration and increased dissolution rate.

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