ENHANCEMENT OF THE SOLUBILITY AND THE DISSOLUTION RATE OF TAMOXIFEN CITRATE SOLID DISPERSION USING SOLUPLUS BY SOLVENT EVAPORATION TECHNIQUE
Objective: The aim of the present study was the enhancement in the solubility of tamoxifen citrate using solid dispersion which is considered as a great solution to overcome the poor water solubility behavior of tamoxifen citrate (TMX) by solvent evaporation technique using SoluplusÂ® as a novel carrier then formulate it as an orodispersible tablet.
Method: A total of 24 formulas were prepared as a solid dispersion by solvent evaporation method using SoluplusÂ® as a polymeric solubilizer in the ratio of 1:1, 1:3, 1:5, 1:7, and 1:10 then formulated as orodispersible tablets by incorporating three types of superdisintegrants; croscarmellose, crospovidone, and sodium starch glycolate (SSG) with the solid dispersion. Characterization of the formulation was done using differential scanning colorimetry, Fourier transforms infrared spectroscopy, X-ray diffraction, and scanning electron microscope and the best formula was selected according to the disintegration and dissolution tests.
Results and Discussion: Formula 22 were selected as the best formula which contains mixed types of superdisintegrants; croscarmellose and SSG with the fastest complete disintegration of 6.5 s and complete dissolution with <2 min.
Conclusion: Accordingly, TMX was successfully enhanced its water solubility by converting its crystalline structure into the amorphous state through solid dispersion with SoluplusÂ® and formulated as an orodispersible tablet to improve its oral absorption.
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