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羟丙甲纤维素对抑制姜黄素无定形固体分散体结晶和提高渗透性的影响。

Impact of HPMC on inhibiting crystallization and improving permeability of curcumin amorphous solid dispersions.

机构信息

Wuya College of Innovation, Shenyang Pharmaceutical University, Shenyang, China.

Wuya College of Innovation, Shenyang Pharmaceutical University, Shenyang, China.

出版信息

Carbohydr Polym. 2018 Feb 1;181:543-550. doi: 10.1016/j.carbpol.2017.12.004. Epub 2017 Dec 6.

Abstract

The purpose of this paper was to elucidate the impacts of hydroxypropylmethyl cellulose E5 as assistant excipient on inhibiting crystallization and improving membrane permeability in curcumin amorphous solid dispersions that formulated by Eudragit E100. Intermolecular interactions formed between curcumin and polymers were probed using in situ Raman imaging and infrared spectroscopy. The abilities of hydroxypropylmethyl cellulose E5 in inhibiting crystallization and improving membrane permeability were confirmed by fluorescence spectroscopy, dynamic light scattering analysis and in vitro permeability experiment. The results demonstrated hydroxypropylmethyl cellulose E5 was significant in maintaining the amorphous drug concentration owing to the hydrogen bond interactions formed with curcumin, rending its ability to inhibit crystallization by reducing drug droplet size. Furthermore, the addition of hydroxypropylmethyl cellulose E5 in curcumin amorphous solid dispersions promoted drug membrane permeability through lowering the order level of phospholipid bilayer layer.

摘要

本文旨在阐明羟丙甲纤维素 E5 作为助剂对抑制姜黄素无定形固体分散体中结晶和提高膜通透性的影响,该固体分散体由 Eudragit E100 制成。通过原位拉曼成像和红外光谱研究了姜黄素和聚合物之间形成的分子间相互作用。荧光光谱、动态光散射分析和体外渗透实验证实了羟丙甲纤维素 E5 抑制结晶和提高膜通透性的能力。结果表明,由于与姜黄素形成氢键相互作用,羟丙甲纤维素 E5 能显著维持无定形药物浓度,从而通过减小药物液滴尺寸来抑制结晶。此外,在姜黄素无定形固体分散体中添加羟丙甲纤维素 E5 通过降低磷脂双层的有序水平来促进药物的膜通透性。

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