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用于难溶性模型药物呋塞米持续释放的漂浮固体纤维素纳米纤维纳米泡沫。

Floating solid cellulose nanofibre nanofoams for sustained release of the poorly soluble model drug furosemide.

机构信息

Royal Insitute of Technology, Wallenberg Wood Science Center, Stockholm, Sweden.

Department of Pharmacy, University of Copenhagen, Copenhagen, Denmark.

出版信息

J Pharm Pharmacol. 2017 Nov;69(11):1477-1484. doi: 10.1111/jphp.12793. Epub 2017 Aug 15.

DOI:10.1111/jphp.12793
PMID:28809440
Abstract

OBJECTIVES

This study aimed to prepare a furosemide-loaded sustained release cellulose nanofibre (CNF)-based nanofoams with buoyancy.

METHODS

Dry foams consisting of CNF and the model drug furosemide at concentrations of 21% and 50% (w/w) have been prepared by simply foaming a CNF-drug suspension followed by drying. The resulting foams were characterized towards their morphology, solid state properties and dissolution kinetics.

KEY FINDINGS

Solid state analysis of the resulting drug-loaded foams revealed that the drug was present as an amorphous sodium furosemide salt and in form of furosemide form I crystals embedded in the CNF foam cell walls. The foams could easily be shaped and were flexible, and during the drug release study, the foam pieces remained intact and were floating on the surface due to their positive buoyancy. Both foams showed a sustained furosemide release compared to a marketed tablet. It was found that the extent of sustained release from both foams was dependent on the drug loading, the dimension of the foam piece, as well as the solid state of the drug.

CONCLUSIONS

Furosemide-loaded CNF-based foams with sustained release and buoyancy have been successfully prepared in a simple casting and drying procedure.

摘要

目的

本研究旨在制备一种具有浮力的呋塞米负载型纤维素纳米纤维(CNF)基缓释纳米泡沫。

方法

通过简单地将 CNF-药物悬浮液起泡并干燥,制备了浓度分别为 21%和 50%(w/w)的 CNF 和模型药物呋塞米的干泡沫。对所得泡沫的形态、固体状态特性和溶解动力学进行了表征。

主要发现

对所得载药泡沫的固态分析表明,药物以无定形呋塞米钠盐和嵌入 CNF 泡沫细胞壁的呋塞米 I 型晶体的形式存在。这些泡沫可以很容易地成型和具有柔韧性,并且在药物释放研究中,由于其正浮力,泡沫块保持完整并漂浮在表面上。与市售片剂相比,两种泡沫均表现出持续的呋塞米释放。结果发现,两种泡沫的缓释程度均取决于药物载药量、泡沫块的尺寸以及药物的固体状态。

结论

通过简单的浇铸和干燥工艺,成功制备了具有持续释放和浮力的呋塞米负载型 CNF 基泡沫。

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