首页> 外文期刊>International Journal of Pharmaceutics >Influence of temperature on the solubilization of thiabendazole by combined action of solid dispersions and co-solvents.
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Influence of temperature on the solubilization of thiabendazole by combined action of solid dispersions and co-solvents.

机译:温度对固体分散体和助溶剂共同作用下噻菌灵增溶的影响。

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摘要

Co-solvents and solid dispersions with polyvinyl pyrrolidone were tested to increase solubility of thiabendazole. Solid dispersions were prepared by the solvent method and analyzed by differential scanning calorimetry. The solubility was measured at 15-35 degrees C in aqueous (ethanol-water) and non-aqueous (ethanol-ethyl acetate) mixtures. Combination of solid dispersions with cosolvents increased the water solubility of thiabendazole in a larger extent that each method separately. The effect of the solid dispersions is greatest in water and it decreases nonlinearly as the volume fraction of ethanol-in water increases. The solubility enhancement is smaller in ethanol-ethyl acetate and is uncorrelated with co-solvent concentration. Solubility parameters delta were used to predict drug/carrier compatibility and related to solubility profiles. Thiabendazole shows an intermediate behaviour between solubility curves with two peaks (more polar drugs with larger delta values) and a single peak (less polar drugs with lower delta values). The solid dispersions increase the solubility parameter of thiabendazole from delta=24 to delta=25.7 MPa(1/2). The model of Bustamante et al. allowed solubility prediction including jointly both mixtures whereas the equation of Jouyban et al. was able to predict the solubility at several temperatures in each binary mixture separately, using a few experiments.
机译:测试了与聚乙烯吡咯烷酮的助溶剂和固体分散体,以提高噻菌灵的溶解度。通过溶剂法制备固体分散体,并通过差示扫描量热法进行分析。在15-35℃下在水性(乙醇-水)和非水性(乙醇-乙酸乙酯)混合物中测量溶解度。与每种方法分别相比,固体分散体与助溶剂的组合在更大程度上提高了噻菌灵的水溶性。固体分散体在水中的影响最大,并且随着乙醇在水中体积分数的增加而非线性降低。在乙醇-乙酸乙酯中的溶解度提高较小,并且与助溶剂浓度无关。溶解度参数delta用于预测药物/载体的相容性,并与溶解度曲线有关。噻苯达唑显示了在具有两个峰(极性值较大的极性较大的药物)和单个峰(δ值较小的极性较小的药物)的溶解度曲线之间的中间行为。固体分散体将噻菌灵的溶解度参数从delta = 24增加到delta = 25.7 MPa(1/2)。 Bustamante等人的模型。允许同时包括两种混合物的溶解度预测,而Jouyban等人的方程式。通过一些实验,我们能够分别预测每种二元混合物在几个温度下的溶解度。

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