利用喷雾干燥技术改善柚皮苷-盐酸喹哪啶的物理化学和机械性能,从实验室到中试规模的柚皮苷-盐酸喹哪啶共晶制剂升级

IF 4.5 2区 工程技术 Q2 ENGINEERING, CHEMICAL Powder Technology Pub Date : 2024-11-17 DOI:10.1016/j.powtec.2024.120458
Lasya Priya Katukam, Amruta Prabhakar Padakanti, Naveen Chella
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引用次数: 0

摘要

目前的工作重点是通过配制一种共晶体系来改善柚皮苷(NRN)和盐酸喹哪啶(QDH)较差的物理化学和机械性能,在这种体系中,两种药物的性能相互补充。此外,还尝试评估喷雾干燥法在放大实验室规模工艺(如旋转蒸发)生产的稳定共晶制剂方面的有效性。包括 PXRD、DSC、SEM 和 FT-IR 光谱在内的分析过程证实了 NRN-QDH 的非晶化以及二者之间的分子相互作用。在 FaSSGF 和 FaSSIF 中,NRN 的溶解度明显提高,溶解速率提高了 10 和 19 倍。经微观力学和 Heckel 分析证实,QDH 的流动特性和压缩行为在由此产生的共晶制剂中得到了改善。这些积极的结果鼓励我们进一步开展临床前研究,以证明这种组合的药代动力学和动态优势,并将其成功应用于临床。
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Upscaling co-amorphous formulation of naringin-quinacrine dihydrochloride translating from laboratory to pilot scale using spray drying for improved physicochemical and mechanical properties
The current work focuses on improving the poor physicochemical and mechanical properties of naringin (NRN) and quinacrine dihydrochloride (QDH) by formulating a co-amorphous system where the properties of individual drugs complement each other. Additionally, an attempt was made to evaluate the effectiveness of spray-drying in scaling up the stable co-amorphous formulations produced by lab-scale process like rotary evaporation. Analytical processes including PXRD, DSC, SEM, and FT-IR spectroscopy confirmed the amorphization of NRN-QDH and molecular interactions between two. A significant enhancement in the NRN solubility along with 10 &19-folds improvement in dissolution rate was observed in FaSSGF & FaSSIF. The flow properties and compression behaviour of QDH were improved in the resultant co-amorphous formulation as confirmed by the micromeritics and Heckel analysis. These positive results encourage further investigation of the preclinical studies to prove the pharmacokinetic and dynamic benefits of this combination and their successful transfer to clinical applications.
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来源期刊
Powder Technology
Powder Technology 工程技术-工程:化工
CiteScore
9.90
自引率
15.40%
发文量
1047
审稿时长
46 days
期刊介绍: Powder Technology is an International Journal on the Science and Technology of Wet and Dry Particulate Systems. Powder Technology publishes papers on all aspects of the formation of particles and their characterisation and on the study of systems containing particulate solids. No limitation is imposed on the size of the particles, which may range from nanometre scale, as in pigments or aerosols, to that of mined or quarried materials. The following list of topics is not intended to be comprehensive, but rather to indicate typical subjects which fall within the scope of the journal's interests: Formation and synthesis of particles by precipitation and other methods. Modification of particles by agglomeration, coating, comminution and attrition. Characterisation of the size, shape, surface area, pore structure and strength of particles and agglomerates (including the origins and effects of inter particle forces). Packing, failure, flow and permeability of assemblies of particles. Particle-particle interactions and suspension rheology. Handling and processing operations such as slurry flow, fluidization, pneumatic conveying. Interactions between particles and their environment, including delivery of particulate products to the body. Applications of particle technology in production of pharmaceuticals, chemicals, foods, pigments, structural, and functional materials and in environmental and energy related matters. For materials-oriented contributions we are looking for articles revealing the effect of particle/powder characteristics (size, morphology and composition, in that order) on material performance or functionality and, ideally, comparison to any industrial standard.
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