Kim Do-Hyun, Kim Young-Woo, Tin Yee-Yee, Soe Mya-Thet-Paing, Ko Byoung-Hyen, Park Sun-Jae, Lee Jaeh-Wi
College of Pharmacy, Chung-Ang University, Seoul 06974, Korea.
CAU-Myanmar Pacific Pharmaceutical Research Center, Chung-Ang University, Seoul 06974, Korea.
Pharmaceutics. 2021 Aug 23;13(8):1318. doi: 10.3390/pharmaceutics13081318.
Amorphization technology has been the subject of continuous attention in the pharmaceutical industry, as a means to enhance the solubility of poorly water-soluble drugs. Being in a high energy state, amorphous formulations generally display significantly increased apparent solubility as compared to their crystalline counterparts, which may allow them to generate a supersaturated state in the gastrointestinal tract and in turn, improve the bioavailability. Conventionally, hydrophilic polymers have been used as carriers, in which the amorphous drugs were dispersed and stabilized to form polymeric amorphous solid dispersions. However, the technique had its limitations, some of which include the need for a large number of carriers, the tendency to recrystallize during storage, and the possibility of thermal decomposition of the drug during preparation. Therefore, emerging amorphization technologies have focused on the investigation of novel amorphous-stabilizing carriers and preparation methods that can improve the drug loading and the degree of amorphization. This review highlights the recent pharmaceutical approaches utilizing drug amorphization, such as co-amorphous systems, mesoporous particle-based techniques, and in situ amorphization. Recent updates on these technologies in the last five years are discussed with a focus on their characteristics and commercial potential.
非晶化技术一直是制药行业持续关注的课题，作为提高难溶性药物溶解度的一种手段。处于高能状态的无定形制剂通常比其结晶对应物表现出显著提高的表观溶解度，这可能使它们在胃肠道中产生过饱和状态，进而提高生物利用度。传统上，亲水性聚合物被用作载体，无定形药物分散并稳定在其中以形成聚合物无定形固体分散体。然而，该技术有其局限性，其中一些包括需要大量载体、储存期间重结晶的倾向以及药物在制备过程中热分解的可能性。因此，新兴的非晶化技术专注于研究能够提高药物载量和非晶化程度的新型非晶态稳定载体和制备方法。本综述重点介绍了最近利用药物非晶化的制药方法，如共无定形系统、介孔颗粒技术和原位非晶化。讨论了这些技术在过去五年中的最新进展，重点是它们的特点和商业潜力。
