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二氧化碳在 Soluplus 中有显著的溶解度,这使得使用超临界流体技术浸渍布洛芬成为可能。

Significant solubility of carbon dioxide in Soluplus facilitates impregnation of ibuprofen using supercritical fluid technology.

机构信息

a Pharmaceutical Technology , Jordan University of Science and Technology , Irbid , Jordan.

b German Jordanian University , Amman , Jordan.

出版信息

Pharm Dev Technol. 2018 Sep;23(7):697-705. doi: 10.1080/10837450.2017.1315135. Epub 2017 Apr 13.

DOI:10.1080/10837450.2017.1315135
PMID:28375669
Abstract

Treatment of Soluplus with supercritical carbon dioxide allows promising applications in preparing dispersions of amorphous solids. Several characterization techniques were employed to reveal this effect, including CO gas sorption under high pressure and physicochemical characterizations techniques. A gravimetric method was used to determine the solubility of carbon dioxide in the polymer at elevated pressure. The following physicochemical characterizations were used: thermal analysis, X-ray diffraction, Fourier transform, infrared spectroscopy and scanning electron microscopy. Drug loading of the polymer with ibuprofen as a model drug was also investigated. The proposed treatment with supercritical carbon dioxide allows to prepare solid solutions of Soluplus in less than two hours at temperatures that do not exceed 45 °C, which is a great advantage to be used for thermolabile drugs. The advantages of using this technology for Soluplus formulations lies behind the high sorption capability of carbon dioxide inside the polymer. This will ensure rapid diffusion of the dissolved/dispersed drug inside the polymer under process conditions and rapid precipitation of the drug in the amorphous form during depressurization accompanied by foaming of the polymer.

摘要

使用超临界二氧化碳处理 Soluplus 可在制备无定形固体分散体方面提供有前景的应用。采用了几种表征技术来揭示这种效果,包括高压下的 CO 气体吸附和物理化学特性技术。重量法用于确定聚合物在高压下对二氧化碳的溶解度。以下是使用的物理化学特性:热分析、X 射线衍射、傅里叶变换、红外光谱和扫描电子显微镜。还研究了聚合物与布洛芬作为模型药物的药物负载。用超临界二氧化碳进行的这种处理可在温度不超过 45°C 的情况下,在不到两小时的时间内制备 Soluplus 的固溶体,这对于热敏药物来说是一个很大的优势。使用这种技术用于 Soluplus 制剂的优点在于二氧化碳在聚合物内部的高吸附能力。这将确保在工艺条件下溶解/分散的药物在聚合物内部快速扩散,并在减压过程中伴随着聚合物起泡,迅速将药物沉淀为无定形形式。

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