Wegiel Lindsay A, Mosquera-Giraldo Laura I, Mauer Lisa J, Edgar Kevin J, Taylor Lynne S
Department of Industrial and Physical Pharmacy, College of Pharmacy, Purdue University, West Lafayette, Indiana, 47907, USA.
Department of Food Sciences, Purdue University, West Lafayette, Indiana, 47907, USA.
Pharm Res. 2015 Oct;32(10):3324-37. doi: 10.1007/s11095-015-1709-z. Epub 2015 May 15.
To investigate the phase behavior of resveratrol amorphous solid dispersions upon addition to aqueous media.
Polymers with different crystallization inhibitor properties were used to form amorphous solid dispersions of resveratrol. Resveratrol crystallization in aqueous environments was monitored over time using Raman spectroscopy, and solution concentrations were determined by ultraviolet (UV) spectroscopy.
The crystallization behavior varied depending on the type and amount of polymer present in the dispersion. Polyvinylpyrrolidone (PVP) and Eudragit E100 (E100) dispersions did not crystallize for 24 h when slurried in pH 6.8 buffer at 37°C. Even though no crystallization occurred, a supersaturated solution was not achieved, most likely because of resveratrol-polymer complexation. Dispersions formed with cellulose derivatives crystallized rapidly, and the extent of crystallization varied depending on the amount of polymer in the dispersion. The solution concentration achieved in the slurries varied considerably between the various solid dispersions and depended on several factors including the extent of resveratrol crystallization, the nature of the resveratrol-polymer interactions, and the concentration of solid dispersion added to the slurry.
It was found that the extent of supersaturation was limited not only by crystallization, but also by soluble and insoluble complex formation between resveratrol and the polymer.
研究白藜芦醇无定形固体分散体加入水性介质后的相行为。
使用具有不同结晶抑制性能的聚合物形成白藜芦醇的无定形固体分散体。使用拉曼光谱随时间监测白藜芦醇在水性环境中的结晶情况，并通过紫外光谱测定溶液浓度。
结晶行为因分散体中聚合物的类型和含量而异。当在37°C的pH 6.8缓冲液中制成浆液时，聚乙烯吡咯烷酮（PVP）和丙烯酸树脂E100（E100）分散体在24小时内未结晶。尽管未发生结晶，但未形成过饱和溶液，这很可能是由于白藜芦醇与聚合物的络合作用。用纤维素衍生物形成的分散体迅速结晶，结晶程度因分散体中聚合物的含量而异。在各种固体分散体中，浆液中达到的溶液浓度差异很大，并且取决于几个因素，包括白藜芦醇的结晶程度、白藜芦醇与聚合物相互作用的性质以及加入浆液中的固体分散体的浓度。
发现过饱和程度不仅受结晶限制，还受白藜芦醇与聚合物之间可溶性和不溶性络合物形成的限制。
