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槲皮素在纤维素衍生物基质中的固体分散体影响其溶解度和稳定性。

Solid dispersion of quercetin in cellulose derivative matrices influences both solubility and stability.

机构信息

Department of Sustainable Biomaterials, Macromolecules and Interfaces Institute, and Institute for Critical Technology and Applied Sciences, Virginia Tech, Blacksburg, VA 24061, USA.

出版信息

Carbohydr Polym. 2013 Feb 15;92(2):2033-40. doi: 10.1016/j.carbpol.2012.11.073. Epub 2012 Dec 3.

Abstract

Amorphous solid dispersions (ASD) of quercetin (Que) in cellulose derivative matrices, carboxymethylcellulose acetate butyrate (CMCAB), hydroxypropylmethylcellulose acetate succinate (HPMCAS), and cellulose acetate adipate propionate (CAAdP) were prepared with the goal of identifying an ASD that effectively increased Que aqueous solution concentration. Crystalline quercetin and Que/poly(vinylpyrrolidinone) (PVP) ASD were evaluated for comparison. Powder X-ray diffraction (XRPD) and differential scanning calorimetry (DSC) were used to examine the crystallinity of ASDs, physical mixtures (PM) and quercetin. ASDs were amorphous up to 50 wt% Que. Que stability against crystallization and solution concentrations from these ASDs were significantly higher than those observed for physical mixtures and crystalline Que. PVP stabilizes against both Que degradation and recrystallization; in contrast, these carboxylated cellulose derivatives inhibit recrystallization but release Que slowly. PVP ASDs afforded fast and complete drug release, while ASDs using these three cellulose derivatives provide slow, incomplete, pH-triggered drug release.

摘要

无定形固体分散体(ASD)的槲皮素(Que)在纤维素衍生物基质中,醋酸丁酸纤维素(CMCAB),羟丙甲基纤维素醋酸琥珀酸酯(HPMCAS)和醋酸丁酸纤维素己二酸丙酯(CAAdP),目的是确定一种能有效提高Que 水溶液浓度的 ASD。比较了结晶槲皮素和 Que/聚乙烯吡咯烷酮(PVP)ASD。粉末 X 射线衍射(XRPD)和差示扫描量热法(DSC)用于研究 ASD、物理混合物(PM)和槲皮素的结晶度。ASD 在 50wt%Que 以下为无定形。Que 的稳定性和这些 ASD 的溶液浓度明显高于物理混合物和结晶 Que。PVP 可稳定 Que 防止降解和重结晶;相比之下,这些羧基化纤维素衍生物抑制重结晶但缓慢释放 Que。PVP ASD 可快速完全释放药物,而使用这三种纤维素衍生物的 ASD 可提供缓慢、不完全、pH 触发的药物释放。

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