The Effect of Relative Humidity on the Physical Properties of Two Melibiose Monohydrate batches with Differing Particle Size Distributions and Surface Properties

• Published in: Journal of pharmaceutical sciences Vol. 102; no. 1; pp. 195 - 203
• Main Authors: Heljo, Ville P., Sainio, Janne, Shevchenko, Anna, Kivikero, Niina, Lakio, Satu, Juppo, Anne M.
• Format: Journal Article
• Language: English
• Published: Hoboken Elsevier Inc 01.01.2013; Wiley Subscription Services, Inc., A Wiley Company; Elsevier Limited
• Subjects: Chemistry, Pharmaceutical; Crystallization; Crystallography, X-Ray; Drug Storage; excipients; Excipients - chemistry; excipients; solid state stability; Humidity; hygroscopicity; Melibiose - chemistry; Models, Molecular; Molecular Structure; Particle Size; Porosity; Powder Diffraction; pseudopolymorphism; solid state stability; spectroscopy; Spectroscopy, Fourier Transform Infrared; Spectrum Analysis, Raman; Surface Properties; Technology, Pharmaceutical - methods; Transition Temperature; Water - chemistry; Wettability; X‐ray powder diffractometry; pseudopolymorphism; solid state stability; X‐ray powder diffractometry; excipients; hygroscopicity; spectroscopy
• ISSN: 0022-3549; 1520-6017
• DOI: 10.1002/jps.23366

Melibiose monohydrate has shown promise when employed as a pharmaceutical excipient, but its physical properties have not been adequately characterized. Therefore, two different melibiose monohydrate batches were analyzed as received or after storage under different relative humidity (RH) atmospheres. The particle size distributions and specific surface areas of the two batches were shown to differ considerably, which also had an effect on their water sorption tendencies and on the intermolecular structure of melibiose after storage. The relatively large primary particles that were more abundant in one of the batches were shown to possess a porous surface structure, and water evaporation from them occurred in two phases when heated. Furthermore, storing the batch with smaller mean particle size under dry conditions affected the crystal structure and molecular vibrations of the sample more than in the case of the batch with larger mean particle size. It was concluded that the physical properties of melibiose monohydrate after storage at different RH atmospheres is largely governed by the primary particle size and porosity.