Patel Nirali G, Banella Sabrina, Serajuddin Abu T M
Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, 8000 Utopia Parkway, Queens, NY 11439, USA.
Department of Pharmaceutical Sciences, College of Pharmacy and Health Sciences, St. John's University, 8000 Utopia Parkway, Queens, NY 11439, USA.
Int J Pharm. 2023 Apr 5;636:122745. doi: 10.1016/j.ijpharm.2023.122745. Epub 2023 Feb 21.
Moisture sorption by polymeric carriers used in amorphous solid dispersion (ASD) plays a critical role in the physical stability of the dispersed drug as it can increase molecular mobility of drug in ASD by decreasing the glass transition temperatures (T) of the drug-polymer system, leading to drug crystallization. The present report describes Part III of a systematic investigation of moisture sorption by different polymers used in ASDs, where the results for four chemically different methacrylic acid-methyl methacrylate and related copolymers, namely, Eudragit® EPO, Eudragit® L100-55, Eudragit® L100, and Eudragit® S100, as the function of relative humidity (RH) are presented. Effects of moisture sorption on T of the polymers were also determined. Among the polymers, Eudragit® EPO is the least hygroscopic, having absorbed, for example, 1.3% w/w moisture at 25 °C/60% RH, while the three other polymers absorbed 4.7-7.5% w/w moisture at the same condition. The moisture sorption was relatively lower at 40 °C than that at 25 °C. The apparent T of polymers decreased with the increase in moisture content; however, T values remained higher than the usual storage temperature of ASD (25 °C) even at high RH, indicating that the effect of moisture sorption on the physical stability of ASD could be minimal when these polymers are used in ASDs.
用于无定形固体分散体（ASD）的聚合物载体的吸湿作用在分散药物的物理稳定性中起着关键作用，因为它可以通过降低药物 - 聚合物体系的玻璃化转变温度（T）来增加药物在ASD中的分子流动性，从而导致药物结晶。本报告描述了对ASD中使用的不同聚合物吸湿作用进行系统研究的第三部分，其中给出了四种化学性质不同的甲基丙烯酸 - 甲基丙烯酸甲酯及相关共聚物，即尤特奇®EPO、尤特奇®L100 - 55、尤特奇®L100和尤特奇®S100，作为相对湿度（RH）函数的吸湿结果。还测定了吸湿对聚合物T的影响。在这些聚合物中，尤特奇®EPO吸湿性最低，例如在25°C/60%RH条件下吸湿1.3%w/w，而其他三种聚合物在相同条件下吸湿4.7 - 7.5%w/w。40°C时的吸湿量比25°C时相对较低。聚合物的表观T随着水分含量的增加而降低；然而，即使在高RH下，T值仍高于ASD通常的储存温度（25°C），这表明当这些聚合物用于ASD时，吸湿对ASD物理稳定性的影响可能最小。
