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提高基于静电纺丝纳米纤维的对乙酰氨基酚固体分散体的溶出度。

Dissolution improvement of electrospun nanofiber-based solid dispersions for acetaminophen.

机构信息

College of Chemistry, Chemical Engineering and Biotechnology, Donghua University, 2999 North Renmin Road, Songjiang District, Shanghai, 201620, China.

出版信息

AAPS PharmSciTech. 2010 Jun;11(2):809-17. doi: 10.1208/s12249-010-9438-4. Epub 2010 May 6.

Abstract

The objective of the present investigation was to prepare novel solid dispersions (SDs) of poorly water-soluble drugs with special microstructural characteristics using electrospinning process. With the hydrophilic polymer polyvinylpyrrolidone as the filament-forming polymer and acetaminophen (APAP) as the poorly water-soluble drug model, SDs having a continuous web structure, and in the form of non-woven nanofiber membranes, were successfully prepared. The electrospun nanofiber-based SDs were compared with those prepared from three traditional SD processes such as freeze-drying, vacuum drying, and heating drying. The surface morphologies, the drug physical status, and the drug-polymer interactions were investigated by scanning electron microscopy, differential scanning calorimetry, X-ray diffraction, and attenuated total reflectance Fourier transform infrared. In vitro dissolution tests demonstrated that the electrospun nanofibers released 93.8% of the APAP content in the first 2 minutes and that the dissolution rates of APAP from the different SDs had the following order: electrospun membrane > vacuum-dried membrane approximately freeze-dried membrane > heat-dried membrane. Electrospun nanofiber-based SDs showed markedly better dissolution-improving effects than the other SDs, mainly due to their huge surface area, high porosity resulting from web structure, and the more homogeneous distribution of APAP in the nanofiber matrix.

摘要

本研究的目的是使用静电纺丝工艺制备具有特殊微观结构特征的新型难溶性药物固体分散体(SD)。以亲水性聚合物聚乙烯吡咯烷酮(PVP)为纤维形成聚合物,以对乙酰氨基酚(APAP)为难溶性药物模型,成功制备了具有连续网状结构和无纺纳米纤维膜形式的 SD。将静电纺纳米纤维基 SD 与三种传统 SD 工艺(冷冻干燥、真空干燥和加热干燥)制备的 SD 进行了比较。通过扫描电子显微镜、差示扫描量热法、X 射线衍射和衰减全反射傅里叶变换红外光谱研究了表面形态、药物物理状态和药物-聚合物相互作用。体外溶出度试验表明,静电纺纳米纤维在最初的 2 分钟内释放了 93.8%的 APAP 含量,不同 SD 中 APAP 的溶出速率顺序为:静电纺丝膜>真空干燥膜≈冷冻干燥膜>加热干燥膜。静电纺纳米纤维基 SD 显示出明显更好的改善溶解效果,主要归因于其巨大的表面积、网状结构导致的高孔隙率以及 APAP 在纳米纤维基质中更均匀的分布。

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