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使用超临界流体技术对难溶性药物进行颗粒设计。

Particle design of poorly water-soluble drug substances using supercritical fluid technologies.

作者信息

Yasuji Takehiko, Takeuchi Hirofumi, Kawashima Yoshiaki

机构信息

Pharmaceutical Research and Technology Labs, Astellas Pharma Inc., 180 Ozumi, Yaizu, Shizuoka 425-0072, Japan.

出版信息

Adv Drug Deliv Rev. 2008 Feb 14;60(3):388-98. doi: 10.1016/j.addr.2007.03.025. Epub 2007 Oct 11.

Abstract

In order to improve the dissolution properties of poorly water-soluble drugs, some drugs were subjected to micronization or prepared as composite particles using supercritical fluid (SCF) technology with carbon dioxide (CO(2)). Solubility in CO(2) is the key when using this method. Solubility affects the supersaturation of the materials in the solvent as well as the mass transfer of that solvent, which are both critical to the micronization of the materials and the formation of the composite particles. Some useful techniques that can be used to avoid the problems posed by the characteristics of the drug itself are combining SC-CO(2) with other technologies, such as the formation of coacervates or emulsions, and other equipment types, such as milling or ultrasound fields. Another advantage of SCF technology is that it is considered to be green chemistry. SC-CO(2) can improve the solubility of poorly water-soluble drug substances using few or no organic solvents and with little or no heating.

摘要

为了改善难溶性药物的溶解性能,一些药物进行了微粉化处理,或采用超临界流体(SCF)技术与二氧化碳(CO₂)制备成复合颗粒。使用该方法时,在CO₂中的溶解度是关键。溶解度会影响材料在溶剂中的过饱和度以及该溶剂的传质,这两者对于材料的微粉化和复合颗粒的形成都至关重要。一些可用于避免药物自身特性带来问题的有用技术包括将超临界CO₂与其他技术(如凝聚层或乳液的形成)以及其他设备类型(如研磨或超声场)相结合。超临界流体技术的另一个优点是它被认为是绿色化学。超临界CO₂可以在使用很少或不使用有机溶剂且几乎不加热或不加热的情况下提高难溶性药物的溶解度。

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