Abstract Layered double hydroxides (LDHs) are widely used as inorganic hosts for different applications, in particular for drug delivery. Piretanide, a poorly soluble diuretic drug, could benefit of the association with LDH for improving the dissolution rate and also for limiting the gastric irritation after its repeated administration thanks to natural antacid properties of LDH. In this paper, the hybrids compounds Piretanide-Mg3Al-LDH and Zn3Al-LDH were synthesized by co-precipitation method. The first proofs to demonstrate the successful intercalation came from X-ray powder diffraction (from hydroxide layers expansion with respect to LDH-carbonate), thermal analysis (from the absence of drug melting point in the hybrid compound) and infrared spectroscopy (from the absence of the carboxylic acid vibration in the hybrid). In addition, SEM microscopy/EDS microanalysis supported the formation of new entities. Both compounds showed a significant improvement of the drug dissolution rate, compared to the active alone, in biorelevant conditions simulating the oral administration.

中文翻译：

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Piretanide在层状双氢氧化物中的特殊溶解行为

摘要 层状双氢氧化物 (LDHs) 被广泛用作不同应用的无机主体，特别是用于药物递送。Piretanide 是一种难溶性利尿药，由于 LDH 的天然抗酸特性，它可以受益于与 LDH 的联合，以提高溶出率，并限制重复给药后的胃刺激。本文采用共沉淀法合成了杂化化合物吡咯他尼-Mg3Al-LDH和Zn3Al-LDH。证明成功嵌入的第一个证据来自 X 射线粉末衍射（来自氢氧化物层相对于 LDH-碳酸盐的膨胀）、热分析（来自混合化合物中没有药物熔点）和红外光谱（来自没有杂化物中的羧酸振动）。此外，SEM 显微镜/EDS 微量分析支持新实体的形成。在模拟口服给药的生物相关条件下，与单独的活性物质相比，这两种化合物都显示出药物溶出率的显着提高。