Martynek Dominik, Ridvan Luděk, Sivén Mia, Šoóš Miroslav
Department of Chemical Engineering, University of Chemistry and Technology Prague, Technická 5, 166 28 Prague 6, Dejvice, Czech Republic; Zentiva, k.s., Ukabelovny 130, 10237 Prague 10, Czech Republic.
Zentiva, k.s., Ukabelovny 130, 10237 Prague 10, Czech Republic.
Int J Pharm. 2025 Mar 15;672:125331. doi: 10.1016/j.ijpharm.2025.125331. Epub 2025 Feb 9.
Spray drying and hot-melt extrusion are among the most prevalent preparation techniques used in the pharmaceutical industry to produce amorphous solid dispersions (ASDs). This study advances previous research by integrating sample production, comprehensive analytical characterization, intrinsic dissolution rate measurements, and assessments of the behavior of ASDs under elevated temperature and humidity conditions. The study focuses on indomethacin, a widely used model for poorly soluble drugs, processed with PVP K30 or HPMC E5, both commonly used polymers. The findings demonstrate that hot-melt extruded samples exhibit superior stability against recrystallization, whereas spray dried samples achieve higher intrinsic dissolution rates. Furthermore, PVP K30 significantly outperforms HPMC E5 in the co-processing of indomethacin, enhancing both the intrinsic dissolution rate and the stability.
喷雾干燥和热熔挤出是制药行业中用于生产无定形固体分散体（ASD）的最普遍的制备技术。本研究通过整合样品制备、全面的分析表征、固有溶解速率测量以及对ASD在高温高湿条件下行为的评估，推进了先前的研究。该研究聚焦于吲哚美辛，一种广泛用于难溶性药物的模型，与常用聚合物PVP K30或HPMC E5一起加工。研究结果表明，热熔挤出样品在抗重结晶方面表现出卓越的稳定性，而喷雾干燥样品则具有更高的固有溶解速率。此外，在与吲哚美辛的共加工中，PVP K30显著优于HPMC E5，提高了固有溶解速率和稳定性。
