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Single-step coprecipitation and coating to prepare curcumin formulations by supercritical fluid technology
The Journal of Supercritical Fluids ( IF 3.4 ) Pub Date : 2020-01-18 , DOI: 10.1016/j.supflu.2020.104758
Ravenna L. Matos , Tiejun Lu , Gary Leeke , Valentina Prosapio , Christopher McConville , Andrew Ingram

Common strategies to improve the dissolution properties of hydrophobic drug compounds include the preparation of composites with hydrophilic excipients and/or size reduction. However, nanoparticles have poor flowability and difficult handling. Therefore, this work aims to demonstrate the single-step improvement of dissolution and flow properties of pharmaceutical formulations. Coprecipitates of curcumin and poly (vinyl pyrrolidone) (guest particles) are simultaneously produced and coated onto microcrystalline cellulose (MCC, 175 μm), corn starch (15 μm) and lactose (< 5 μm) (host particles), by combining the Supercritical Antisolvent process with two different configurations of fluidized bed (tapered bed and stirred vessel). Experiments were performed at 40 °C, 9−12 MPa, 2.5–30.0 % guest/host mass ratio and stirrer speed varying from 400 to 1200 rpm. SEM images demonstrated that nanoparticles of coprecipitates were obtained while DSC results showed that they were amorphous, explaining the remarkable improvement in dissolution achieved. Free-flowing powder was obtained when MCC was used.



中文翻译:

单步共沉淀和包衣通过超临界流体技术制备姜黄素制剂

改善疏水性药物化合物的溶解特性的常用策略包括制备具有亲水性赋形剂和/或减小尺寸的复合材料。但是,纳米颗粒的流动性差并且难以处理。因此,这项工作旨在证明一步一步改善药物制剂的溶出度和流动性。姜黄素和聚乙烯吡咯烷酮(客体颗粒)的共沉淀物可同时生产,并通过结合超临界混合物,涂覆在微晶纤维素(MCC,175μm),玉米淀粉(15μm)和乳糖(<5μm)(宿主颗粒)上具有两种不同配置的流化床(锥形床和搅拌容器)的抗溶剂工艺。实验是在40°C,9-12 MPa,2.5-30下进行的。0%的宾客/主机质量比和搅拌器速度从400到1200 rpm不等。SEM图像表明获得了共沉淀的纳米颗粒,而DSC结果表明它们为无定形的,这说明溶解度显着提高。当使用MCC时,获得自由流动的粉末。

更新日期:2020-01-18
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