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Development and Evaluation of Immediate Release Tablets of Dolutegravir Sodium by Solid Dispersion Technique

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The Dolutegravir Sodium is an antiretroviral drugs bear some significant drawbacks such as, low solubility, low bioavailability, and undesirable side effects. Efforts have been made to design immediate release drug delivery systems for anti-HIV agents to increase the solubility & bioavailability and decrease the degradation/metabolism in the gastrointestinal tract, and to deliver them to the target cells selectively with minimal side effects. The half-life of Dolutegravir is 15 hours. It gets metabolized mainly in the liver, dolutegravir is a BSC class-II drug, it has low solubility and high permeability, hence need to enhance the solubility of by using different solid dispersion techniques. Solid dispersion of dolutegravir is prepared by rotary solvent evaporation method. The purpose of this study was to develop   immediate release tablets of poorly water soluble dolutegravir. In this study dolutegravir immediate release tablet were prepared by direct compression method using superdisintegrants at a concentration range 0.5-5% .The tablet is based on interactive mixture of components, consisting of carrier particles covered by fine particles of dolutegravir. The tablets were evaluated for hardness, friability, DT, swelling index ratio and in-vitro drug release. FT-IR, XRD and physical compatibility study were conducted for drug excipient interactions.
Title: Development and Evaluation of Immediate Release Tablets of Dolutegravir Sodium by Solid Dispersion Technique
Description:
The Dolutegravir Sodium is an antiretroviral drugs bear some significant drawbacks such as, low solubility, low bioavailability, and undesirable side effects.
Efforts have been made to design immediate release drug delivery systems for anti-HIV agents to increase the solubility & bioavailability and decrease the degradation/metabolism in the gastrointestinal tract, and to deliver them to the target cells selectively with minimal side effects.
The half-life of Dolutegravir is 15 hours.
It gets metabolized mainly in the liver, dolutegravir is a BSC class-II drug, it has low solubility and high permeability, hence need to enhance the solubility of by using different solid dispersion techniques.
Solid dispersion of dolutegravir is prepared by rotary solvent evaporation method.
The purpose of this study was to develop   immediate release tablets of poorly water soluble dolutegravir.
In this study dolutegravir immediate release tablet were prepared by direct compression method using superdisintegrants at a concentration range 0.
5-5% .
The tablet is based on interactive mixture of components, consisting of carrier particles covered by fine particles of dolutegravir.
The tablets were evaluated for hardness, friability, DT, swelling index ratio and in-vitro drug release.
FT-IR, XRD and physical compatibility study were conducted for drug excipient interactions.

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