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KMID : 0370220210650060487
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Yakhak Hoeji
2021 Volume.65 No. 6 p.487 ~ p.493
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Effect of Spray Drying Method on the Properties of Glimepiride-loaded Solid Dispersion
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Yang Hyun-Seok
Oh Yu-Rim
Kim Dong-Wuk
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Abstract
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Glimepiride (GLI) is a third-generation sulfonylurea class antidiabetic drug that has low aqueous solubility. Theobjective of this study was to evaluate the effect of solvents in the development of GLI-loaded solid dispersions (GLISD)using spray drying technique. Two GLI-SD were prepared by adding GLI, polyvinylpyrrolidone (PVP K30), andsodium lauryl sulfate (SLS) in an ethanol/water mixture (solvent evaporation, SE) and water only (surface attached, SA).
Intrinsic saturated solubilities and in-vitro dissolution were evaluated and compared to the GLI powder and physicalmixture (PM). In addition, physicochemical studies such as scanning electron microscopy, differential scanning calorimetry,and X-ray diffraction were also evaluated. We found that the solubility of GLI was significantly improved by both thepreparation methods. The SE method showed 4,960-fold improvement while the SA method displayed 2,900-foldenhancement, which is equivalent to the PM. The in-vitro dissolution studies showed that both methods had a higherrelease rate, about 1.3-fold for SE and 2-fold for SA, as compared to pure GLI powder. However, GLI release slightlydecreased with time for the SA method. Furthermore, solid-state characterizations also revealed that most of the crystallinedrug was transformed to the amorphous form in both GLI-SD. Thus, these results indicate that choice of the solventsystem plays an important role in the spray drying technique which affects the solubility, dissolution, and crystallinity ofpoorly soluble drugs such as GLI.
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KEYWORD
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Glimepiride, Polyvinyl pyrrolidone, Sodium lauryl sulfate, Solid dispersion, Solvent evaporation method, Surface attached method, Spray dryer
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