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- W4285809733 abstract "In dissolution test, the surfactant sodium lauryl sulfate (SLS) is usually added to increase the dissolution of insoluble drugs and achieve the sink condition. However, the current study found that 0.1 % SLS would significantly decrease the dissolution of crystalline lurasidone hydrochloride (LH, a BCS Ⅱ drug). The aim of this study was to clarify the mechanism of this unexpected phenomenon and explore a strategy for mitigating the negative effect of SLS on the dissolution of LH. Sample characterizations (such as PLM, DSC, PXRD, IR and NMR) confirmed that the insoluble single-phase amorphous LH-SLS complex (with a single T g at 35.2 °C) formed during dissolution in 0.1 % SLS aqueous solution via electrostatic interaction, tetrel bond interaction, and hydrophobic effect. Due to the plasticization effect of water, the transition of amorphous LH-SLS from its glassy state to viscous supercooled liquid state led to the gel formation, and suppressd the dissolution of LH. Meanwhile, the solubility curve of LH in SLS aqueous solution at various concentrations exhibited an unusual V-shaped feature, with the CMC value of SLS serving as the inflection point, since the gel degree was attenuated due to the micelle solubilization of SLS. Additionally, an innovative strategy was developed to alleviate the inhibiting effect of SLS on LH dissolution based on the potential competitive interactions. This study not only enriches the internal mechanism of surfactant-inhibited drug dissolution but also informs an effective strategy to mitigate the gelation." @default.
- W4285809733 created "2022-07-19" @default.
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- W4285809733 date "2022-08-01" @default.
- W4285809733 modified "2023-10-18" @default.
- W4285809733 title "Effect of sodium lauryl sulfate-mediated gelation on the suppressed dissolution of crystalline lurasidone hydrochloride and a strategy to mitigate the gelation" @default.
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- W4285809733 doi "https://doi.org/10.1016/j.ijpharm.2022.122035" @default.
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