Development of Rebaudioside D Polymorphs with Improved Solubility

Abstract

Steviol glycosides are found in the leaves of Stevia rebaudiana Bertoni plants and have been used as natural, high-intensity sweeteners. Rebaudioside D (RebD) is a steviol glycoside derivative that has a similar sweetening profile to that of sugar; however, it is poorly soluble in water. Therefore, in this study, polymorphs of RebD showing greater solubility were investigated. We identified at least two novel polymorphs using differential scanning calorimetry (DSC) and X-ray diffractometry (XRD). We identified the transition to one polymorphic form of RebD (named "form α") by desolvation at about 50 ℃, and the other (named "form β") at about 70 ℃. Both forms exhibited greater water solubility compared to untreated RebD. This is the first report of RebD polymorphs with improved solubility, which may contribute to the production of RebD with both a sugar-like taste profile and high-solubility property.

Enhancement of Rebaudioside M Production by Structure-Guided Engineering of Glycosyltransferase UGT76G1

“…In order to resolve the problem of the low solubility of Reb D, , fed-batch feeding of Reb D was carried out for the scale preparation of Reb M using the preliminary optimization of reaction conditions. Reb D (100 μL 100 mM) was added at 0, 0.5, and 2 h time points.…”

Exploring Solid Form Landscape of Anticancer Drug Dimethylaminomicheliolide Fumarate: Crystal Structures Analysis, Phase Transformation Behavior, and Physicochemical Properties Characterization

“…Phase transitions including polymorph interconversion, hydrate formation, and solvate desolvation − may happen under different processes, such as crystallization, granulation, compaction, drying, storage, and transport. It will further affect the performance (stability, − particle size and shape, − flowability, hygroscopicity, − and solubility − ) of the active pharmaceutical ingredients . Consequently, a thorough characterization of all possible pharmaceutical polymorphs and investigation of the phase transformation process are crucial for selecting the optimal solid form for development. − Furthermore, mapping the solid form landscapes will increase the understanding of the physicochemical properties and crystallization behavior of crystal forms, which can contribute to product design and process development.…”