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采用珠磨法制备并表征塞来昔布纳米混悬剂。

Preparation and Characterization of Celecoxib Nanosuspension Using Bead Milling.

机构信息

Department of Pharmaceutical Engineering, Inje University, Gimhae 50834, Republic of Korea.

Department of Pharmacy, College of Pharmacy, Chosun University, Gwangju 61452, Republic of Korea.

出版信息

J Nanosci Nanotechnol. 2019 Feb 1;19(2):1184-1187. doi: 10.1166/jnn.2019.15917.

Abstract

The aim of this study is to develop nanosuspension for improved dissolution of poorly water-soluble celecoxib. We first prepared coarse suspension of celecoxib with Tween 80 and hydroxypropyl methylcellulose as stabilizers, and then fabricated nanosuspension using the bead milling technique. Depending on milling time, the physical properties of nanosuspension were evaluated by photon correlation spectroscopy (e.g., particle size and distribution) and scanning electron microscopy (SEM) (e.g., morphology). As results, the mean size of crystalline celecoxib particles was highly reduced (368.1±14.5 nm) as milling process proceeded comparing to celecoxib powder (6.5±1.0 m). Morphology of milled celecoxib particles has changed considerably from bar-shape or plate-shape to needle-shape due to a high energy caused by milling. In the dissolution test, the celecoxib nanosuspension showed an improved dissolution profile at pH 1.2 compared to celecoxib powder (less than 1%). In contrast, 53.4% of celecoxib in nanosuspension was dissolved up to 30 minutes, demonstrating improved dissolution of celecoxib. Taken together, bead-milled nanosuspension could be an effective strategy that can improve the dissolution and bioavailability.

摘要

本研究旨在制备纳米混悬剂以提高难溶性塞来昔布的溶解性能。我们首先使用吐温 80 和羟丙基甲基纤维素作为稳定剂制备塞来昔布粗混悬剂,然后采用珠磨技术制备纳米混悬剂。根据研磨时间,通过光子相关光谱法(例如,粒径和分布)和扫描电子显微镜(SEM)(例如,形态)评估纳米混悬剂的物理性质。结果表明,与塞来昔布粉末(6.5±1.0μm)相比,研磨过程中结晶塞来昔布颗粒的平均粒径显著减小(368.1±14.5nm)。由于研磨产生的高能量,研磨后的塞来昔布颗粒的形态从棒状或板状发生了很大变化,变成了针状。在溶解试验中,与塞来昔布粉末(不到 1%)相比,塞来昔布纳米混悬剂在 pH 1.2 时显示出改善的溶解曲线。相比之下,纳米混悬剂中 53.4%的塞来昔布在 30 分钟内溶解,表明塞来昔布的溶解得到了改善。综上所述,珠磨纳米混悬剂可能是一种有效的策略,可以提高塞来昔布的溶解度和生物利用度。

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