Purpose: Hydrophobic drugs are facing a major challenge in dissolution rate enhancement and\nsolubility in aqueous solutions; therefore, a variety of methods have been used to improve dissolution\nrate and/or solubility of bendroflumethiazide as a model hydrophobic drug. Methods: In this study,\ntwo main methods (physical mixing and lyophilisation) were used with gluconolactone, hydroxyl propyl\n�³-ccyclodextrin, and trehalose to explore this challenge. Bendroflumethiazide, practically insoluble\nin water, was mixed with one of the three excipients gluconolactone, hydroxyl propyl �³-cyclodextrin,\nand trehalose in three different ratios 1:1, 1:2, 1:5. To the best of our knowledge, the dissolution of the\ndrug has not been previously enhanced by using either these methods or any of the used excipients.\nSamples containing drug and each of the excipients were characterized via dissolution testing,\nFourier Transform infra-red spectroscopy, differential scanning calorimetry, and scanning electron\nmicroscopy. Results: The used methods showed a significant enhancement in dug dissolution\nrate; physical mixing significantly, p < 0.05, increased the percentage of the drug released with\ntime; for example, bendroflumethiazide dissolution in distilled water was improved from less than\n20% to 99.79% within 90 min for physically mixed drug-cyclodextrin 1:5. The lyophilisation process\nwas enhanced and the drug dissolution rate and the highest drug dissolution was achieved for\n(drug-gluconolactone 1:1) with 98.98% drug release within 90 min. Conclusions: the physical mixing\nand freeze drying processes significantly increased the percentage of drug release with time.
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