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用于提高广藿香油生物利用度的胃漂浮型缓释颗粒的研制与表征

Development and characterization of gastro-floating sustained-release granules for enhanced bioavailability of patchouli oil.

作者信息

Liu Chen, Wu Yanan, Zou Yeli, Wang Jiao, Li Boli, Ma Yanni, Zhang Xia, Wang Wenping

机构信息

General Hospital of Ningxia Medical University, Yinchuan, Ningxia, 750004, China.

College of Pharmacy, Ningxia Medical University, Yinchuan, 750004, China.

出版信息

Heliyon. 2024 Nov 13;10(23):e40374. doi: 10.1016/j.heliyon.2024.e40374. eCollection 2024 Dec 15.

Abstract

UNLABELLED

Patchouli oil (PO), extracted from Benth., a prominent aromatic plant of the Lamiaceae family, has shown considerable protective effects against gastrointestinal infections, particularly those induced by . This study aimed to develop a gastro-floating multi-unit system for PO to enhance its gastric retention and oral bioavailability.

METHODS

The oil-laden granules were prepared using colloidal silicon dioxide (CSD) for oil adsorption and to provide buoyancy, along with ethyl cellulose (EC) and hydroxypropyl methyl cellulose (HPMC) to form a sustained-release matrix. The CSD exhibited favorable characteristics for oil adsorption and floating. Compatibility between PO and CSD was affirmed through DSC thermograms and FTIR spectra. The obtained granules demonstrated a sustained release profile, achieving over 90 % release within 10 h without an initial burst. After oral administration, the granules were observed to remain in the gastric region of rats for over 7 h. The bioavailability of patchouli alcohol from the optimized granules was significantly higher than that from of the PO-loaded powders. The gastro-floating sustained-release granules, based on a CSD/EC/HPMC matrix, offer a simple yet effective strategy to improve the delivery efficacy of PO against infections in the gastric region.

摘要

未标记

广藿香精油(PO)从唇形科一种著名的芳香植物广藿香中提取,已显示出对胃肠道感染有显著的保护作用,特别是由[病原体名称未给出]引起的感染。本研究旨在开发一种用于PO的胃漂浮多单元系统,以提高其胃内滞留时间和口服生物利用度。

方法

使用胶体二氧化硅(CSD)制备载油颗粒,用于吸附油并提供浮力,同时加入乙基纤维素(EC)和羟丙基甲基纤维素(HPMC)形成缓释基质。CSD表现出良好的油吸附和漂浮特性。通过DSC热谱图和FTIR光谱证实了PO与CSD之间的相容性。所得颗粒呈现出缓释特性,在10小时内释放超过90%,且无初始突释。口服给药后,观察到颗粒在大鼠胃区域内停留超过7小时。优化颗粒中广藿香醇的生物利用度显著高于载PO粉末的生物利用度。基于CSD/EC/HPMC基质的胃漂浮缓释颗粒提供了一种简单而有效的策略,可提高PO对胃区域感染的给药效果。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9ec0/11635734/023329fdc4c5/gr1.jpg

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