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Study of the Preparation of Amorphous Itraconazole Formulations

机译：非晶态伊曲康唑制剂的制备研究

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The formulation of poorly water soluble active pharmaceutical, ingredients (APIs) has been widely studied in the last few decades to :overcome the limited bioavailability imposed by these pharmaceutical ingredients. In this work, supercritical fluid extraction of emulsions has been applied Using two different types of excipients, i.e., poly(vihyl alcohol) (PVA) and glycyrrhizic acid (GA), to address the precipitation of itraconazole (ITZ) as an amorphous :solid: The delivery profiles of the in vitro dissolution tests of the ITZ-GA particles confirmed the advantage of the Manufactured amorphous material in terms of apparent solubility in comparison to the raw ITZ. Furthermore, the stability of an amorphous glassy product and its potential to recrystallize in the presence of Water have been experimentally determined using both excipients and interpreted applying molecular dynamics (MD) simulations. Results show that recrystallization of the amorphous ITZ particles starts at their surface, corroborating that the better adsorption of GA into the surface of the particles inhibits the crystallization and provides long-term stability products. This study Shows the importance of the selection of the excipient in the preparation of amorphous formulations of APIs, as well as their effect on the stability to recrystallize over storage or dosing in the presence of water.
机译：在过去的几十年中，水溶性差的活性药物成分（API）的配方得到了广泛的研究，以：克服这些药物成分带来的有限的生物利用度。在这项工作中，已使用两种不同类型的赋形剂，即聚（乙烯醇）（PVA）和甘草酸（GA），对乳液进行超临界流体萃取，以解决伊曲康唑（ITZ）作为无定形固体的沉淀问题。 ：ITZ-GA颗粒体外溶出度测试的输送曲线证实了与原始ITZ相比，人造无定形材料在表观溶解度方面的优势。此外，已使用两种赋形剂通过实验确定了无定形玻璃态产品的稳定性及其在水存在下重结晶的潜力，并通过分子动力学（MD）模拟进行了解释。结果表明，非晶态ITZ颗粒的重结晶始于其表面，这证实了GA更好地吸附到颗粒表面会抑制结晶并提供长期稳定性的产物。这项研究表明，在制备无定形的API原料中选择赋形剂很重要，并且它们对在储存或加水存在下重结晶的稳定性也有影响。

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