In this study, we designed amorphous solid dispersions based on Eudragit E/HCl (neutralized Eudragit E using hydrochloric acid) to maximize the dissolution of trans-resveratrol. Solid-state characterization of amorphous solid dispersions of trans-resveratrol was performed using powder X-ray diffraction, scanning electron microscopy, and particle size measurements. In addition, an in vitro dissolution study and an in vivo pharmacokinetic study in rats were carried out. Among the tested polymers, Eudragit E/HCl was the most effective solid dispersion for the solubilization of trans-resveratrol. Eudragit E/HCl significantly inhibited the precipitation of trans-resveratrol in a pH 1.2 dissolution medium in a dose-dependent manner. The amorphous Eudragit E/HCl solid dispersion at a trans-resveratrol/polymer ratio of 10/90 exhibited a high degree of supersaturation without trans-resveratrol precipitation for at least 48 h by the formation of Eudragit E/HCl micelles. In rats, the absolute oral bioavailability (F%) of trans-resveratrol from Eudragit E/HCl solid dispersion (10/90) was estimated to be 40%. Therefore, trans-resveratrol-loaded Eudragit E/HCl solid dispersions prepared by spray drying offer a promising formulation strategy with high oral bioavailability for developing high-quality health supplements, nutraceutical, and pharmaceutical products.

中文翻译：

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通过喷雾干燥制备的中和Eudragit E固体分散体提高白藜芦醇的口服生物利用度

在这项研究中，我们设计了基于Eudragit E / HCl（使用盐酸中和的Eudragit E）的无定形固体分散体，以最大程度地提高反式白藜芦醇的溶解度。反式白藜芦醇的非晶态固体分散体的固态表征使用粉末X射线衍射，扫描电子显微镜和粒径测量进行。另外，在大鼠中进行了体外溶出研究和体内药代动力学研究。在测试的聚合物中，Eudragit E / HCl是反式白藜芦醇增溶最有效的固体分散体。Eudragit E / HCl显着抑制反式沉淀-白藜芦醇在pH 1.2溶出介质中的剂量依赖性。反式白藜芦醇/聚合物比率为10/90的无定形Eudragit E / HCl固体分散体通过形成Eudragit E / HCl胶束在至少48 h内表现出高的过饱和度，而没有反式白藜芦醇沉淀。在大鼠中，Eudragit E / HCl固体分散体（10/90）中反式白藜芦醇的绝对口服生物利用度（F％）估计为40％。因此，通过喷雾干燥制备的反式白藜芦醇负载的Eudragit E / HCl固体分散体为开发高质量的保健品，营养品和药物产品提供了具有高口服生物利用度的有前途的配制策略。