Department of Applied Physics, Aalto University School of Science, P.O. Box 15100, FI-00076 AALTO, Espoo, Finland.
AAPS PharmSciTech. 2012 Jun;13(2):707-12. doi: 10.1208/s12249-012-9789-0. Epub 2012 May 5.
L-Leucine formed different crystalline coatings on salbutamol sulphate aerosol particles depending on the saturation conditions of L-leucine. The work emphasizes a careful characterization of powders where structural compartments such as crystal size and particle coating may affect the performance of drug when administered. The sublimation of L-leucine from the aerosol particles took place 90°C lower temperature than the bulk L-leucine which was attributed to result from the sublimation of L-leucine from nano-sized crystalline domains. The dissolution slowed down and initial dissolution rate decreased with increasing L-leucine content. Decreasing crystalline domains to nano-scale improve heat and mass transfer which was observed as the lowered decomposition temperature of the drug salbutamol sulphate and the sublimation temperature of surface material L-leucine as well as the altered dissolution characteristics of the drug. The structure of the coated drug particles was studied by means of thermal analysis techniques (DSC and TG), and the dissolution of salbutamol sulphate was studied as an on-line measurement in a diffusion cell.
L-亮氨酸会根据 L-亮氨酸的饱和度在硫酸沙丁胺醇气溶胶颗粒上形成不同的晶型涂层。这项工作强调了对粉末的仔细表征,其中结构隔室(如晶体尺寸和颗粒涂层)可能会影响药物给药时的性能。L-亮氨酸从气溶胶颗粒中的升华发生在比大块 L-亮氨酸低 90°C 的温度下,这归因于纳米级晶区的 L-亮氨酸升华所致。随着 L-亮氨酸含量的增加,溶解速度减慢,初始溶解速率降低。将结晶域减小到纳米尺度可改善热传递和质量传递,这表现为药物硫酸沙丁胺醇的分解温度降低,表面材料 L-亮氨酸的升华温度降低,以及药物的溶解特性发生变化。通过热分析技术(DSC 和 TG)研究了包衣药物颗粒的结构,并在扩散池中进行了在线测量以研究硫酸沙丁胺醇的溶解。