离心熔融纺丝技术提高伊曲康唑的溶解度

Q4 Pharmacology, Toxicology and Pharmaceutics
Rodge PJ, Shirolkar SV
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引用次数: 0

摘要

伊曲康唑是一种水溶性差、生物利用度有限的抗真菌药物,难以实现有效的治疗应用。采用离心熔融纺丝技术提高伊曲康唑的溶解度。在这个过程中,伊曲康唑在熔化时受到离心力的作用,形成无定形的固体分散体。以蔗糖为载体,采用离心熔融纺丝法制备了负载10% w/w伊曲康唑的微纤维。扫描电镜结果表明,成功制备了形貌均匀、平均直径为14.27±2.90 μm的itz -蔗糖微纤维。XRD和DSC测试证实了纺丝微纤维的无定形性质。与普通伊曲康唑相比,伊曲康唑蔗糖微纤维的溶解度显著提高了17倍。溶出度实验表明,负载ITZ的蔗糖微纤维在10分钟内的释放率为94.96±1.47%,与普通药物相比有显著提高。研究表明,利用离心熔融纺丝技术成功制备了伊曲康唑的无定形固体分散体,大大提高了药物的溶解度。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Solubility Enhancement of Itraconazole by Centrifugal Melt Spinning Technique
Itraconazole is an antifungal drug with poor water solubility and limited bioavailability, presenting difficulties in achieving effective therapeutic applications. This study aimed to employ centrifugal melt spinning, an innovative method, to improve the solubility of itraconazole. In this process, itraconazole was subjected to centrifugal forces while melting, forming amorphous solid dispersions. Microfibers loaded with 10% w/w itraconazole were prepared through centrifugal melt spinning, employing sucrose as a carrier. ITZ-sucrose microfibers with uniform morphology and an average diameter of 14.27 ± 2.90 μm were successfully fabricated, as evidenced by the scanning electron microscopy results. XRD and DSC measurements confirmed the amorphous nature of the spun microfibers. The solubility of Itraconazole sucrose microfibers was significantly enhanced by 17-fold compared to plain itraconazole. The dissolution experiments demonstrated that sucrose microfibers loaded with ITZ achieved a significant release of 94.96 ± 1.47% within 10 minutes, representing a substantial enhancement compared to plain drugs. The study indicated that utilizing the centrifugal melt spinning technique successfully generated amorphous solid dispersions of itraconazole, leading to a considerable improvement in the drug’s solubility.
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来源期刊
International Journal of Drug Delivery Technology
International Journal of Drug Delivery Technology Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
0.70
自引率
0.00%
发文量
0
期刊介绍: International Journal of Drug Delivery Technology (IJDDT) provides the forum for reporting innovations, production methods, technologies, initiatives and the application of scientific knowledge to the aspects of pharmaceutics, including controlled drug release systems, drug targeting etc. in the form of expert forums, reviews, full research papers, and short communications.
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