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Triboelectrification and dissolution property enhancements of solid dispersions

机译:固体分散体的摩擦起电和溶解性能增强

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The use of solid dispersion techniques to modify physicochemical properties and improve solubility and dissolution rate may result in alteration to electrostatic properties of particles. Particle triboelectrification plays an important part in powder processing, affecting end product quality due to particle deposition and powder loss. This study investigates the use of glucosamine hydrochloride (GLU) in solid dispersions with indomethacin. Solvents selected for the preparation of the dispersions were acetone, acetone-water, ethanol and ethanol-water. Solid state characterizations (DSC, FTIR and XRPD) and dissolution were conducted. Dispersions were subjected to charge using a custom built device based on a shaking concept, consisting of a Faraday cup connected to an electrometer. All dispersions improved the dissolution rate of indomethacin. Analysis showed the method of preparation of the dispersion induced polymorphic forms of the drug. Indomethacin had a high propensity for charging (-411 nC/g). GLU had a very low charge (-1 nC/g). All dispersions had low charges (-1 to 14 nC/g). Acetone as a solvent, or in combination with water, produced samples with an electronegative charge in polarity. The same approach with ethanol produced electropositive charging. The results show the selection of solvents can influence powder charge thereby improving powder handling as well as dissolution properties. (C) 2015 Elsevier B.V. All rights reserved.
机译:使用固体分散技术来改变物理化学性质并提高溶解度和溶解速度可能会导致颗粒的静电性质改变。颗粒摩擦起电在粉末加工中起重要作用,由于颗粒沉积和粉末损失,影响最终产品质量。这项研究调查了葡萄糖胺盐酸盐(GLU)在消炎痛固体分散液中的使用。选择用于制备分散体的溶剂是丙酮,丙酮-水,乙醇和乙醇-水。进行了固态表征(DSC,FTIR和XRPD)和溶解。使用基于振动概念的定制设备对分散液进行充电,该设备由连接到静电计的法拉第杯组成。所有分散体均提高了消炎痛的溶出度。分析显示了分散诱导的药物多晶型形式的制备方法。消炎痛具有很高的充电倾向(-411 nC / g)。 GLU的电荷很低(-1 nC / g)。所有分散体均具有低电荷(-1至14 nC / g)。丙酮作为溶剂,或与水混合,可制得极性带负电电荷的样品。使用乙醇的相同方法产生正电。结果表明,溶剂的选择会影响粉末电荷,从而改善粉末处理以及溶解性能。 (C)2015 Elsevier B.V.保留所有权利。

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