ISSN : 2663-2187

Preparation and in vitro evaluation itraconazole SD using hot melt and solvent evaporation method

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Gamal Osman Elhassan, R.A.M. Jainaf Nachiya, Gangadevi Nataraja, Jiyauddin Khan, Jamal Moideen Muthu Mohamed
» doi: 10.33472/AFJBS.6.6.2024.7135-7142

Abstract

Infections of the fingernails and toenails caused by fungi are frequently treated with itraconazole (ITR). ITR has a poor aqueous solubility and may exhibit restricted absorption upon dissolution. Polyethele glycol (PEG 5000), gelucire (GLR 44/14), and β-cyclodextrin (βCD) were the polymers used to prepare the solid dispersion (SD) of ITR by physical mixing (PM), hot melt and solvent evaporation method, which were 1:1, 1:3, and 1:5 respectively. The physical characteristics, solubility, in vitro dissolution tests, and Fourier Transform Infrared (FT-IR) Spectroscopy of the SD were all studies. All formulations were determined to have a high and evenly distributed ITR content. The USP paddle (type II) dissolving apparatus was used for the in vitro dissolution investigations. The prepared SD exhibited a significantly higher ITR dissolving rate than the pure ITR. While comparing the aqueous solubility (0.9745 ± 0.029), drug content (94.55 ± 2.89), and dissolution rate (96.17 ± 3.89 %) of GLR 44/14 (1:5) by fusion technique to other dispersions prepared by physical mixing (PM) and fusion method using PEG 5000 and βCD (1:3 and 1:5), the latter revealed a slower rate of dissolution and the out of the three carriers, the ITR dissolved more readily in GLR 44/14 based SDs. It was concluded that the SD may improve the ITR's dissolution and that SDs based on PEG6000 were more successful in doing so.

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