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尼古丁-硅酸镁铝复合物经共混工艺加工:作为黏膜粘附颊片中药物载体的特性研究。

Nicotine-magnesium aluminum silicate complexes processed by blending: Characterization for usage as drug carriers in mucoadhesive buccal discs.

机构信息

Division of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Khon Kaen University, Khon Kaen 40002, Thailand.

Chulabhorn Royal Pharmaceutical Manufacturing Facility, Chulabhorn Royal Academy, Bangkok 10210, Thailand.

出版信息

Int J Pharm. 2023 Aug 25;643:123243. doi: 10.1016/j.ijpharm.2023.123243. Epub 2023 Jul 16.

DOI:10.1016/j.ijpharm.2023.123243
PMID:37463620
Abstract

Complexation of nicotine (NCT) and magnesium aluminum silicate (MAS) has been formed in the dispersions that required multiple preparation steps. In this study, physical blending was used to produce NCT-MAS complexes. NCT, a free-base liquid state form, was adsorbed onto the MAS granules, where the diffusion and intercalation of NCT molecules into the MAS silicate layers occurred. These processes required a minimum of the 7-d-resting period to reach NCT complete distribution. FTIR, XRD, and Si NMR suggest that NCT could interact with MAS via hydrogen bonding, water bridging, and ionic electrostatic force. The 12 % NCT-MAS complexes enabled a sustained release of NCT, after a 2-min burst, in pH 6 phosphate buffer through a particle diffusion-controlled mechanism. Buccal discs formulated with NCT-MAS complexes and sodium alginate (SA) as drug carriers and matrix former could control NCT released through drug diffusion and swelling-controlled mechanisms. NCT release and membrane permeation increased with increasing NCT-MAS complexes or decreasing SA concentration. All NCT-MAS-containing buccal discs exhibited mucoadhesive properties related to the swelling characteristics of SA and MAS. Conclusively, NCT-MAS complexes can be produced through an uncomplicated single-step blending process, and the complexes obtained presented a potential to serve as drug carriers in buccal matrix formulations.

摘要

已在需要多步制备步骤的分散体中形成尼古丁 (NCT) 和镁铝硅酸盐 (MAS) 的配合物。在这项研究中,使用物理共混法生产 NCT-MAS 配合物。NCT 是一种游离碱的液态形式,被吸附到 MAS 颗粒上,其中 NCT 分子扩散并插入 MAS 硅酸盐层中。这些过程需要至少 7 天的休息时间才能达到 NCT 的完全分布。FTIR、XRD 和 Si NMR 表明,NCT 可以通过氢键、水桥和离子静电力与 MAS 相互作用。12%的 NCT-MAS 配合物通过粒子扩散控制机制,在 pH 6 磷酸盐缓冲液中,在 2 分钟的爆发后,实现了 NCT 的持续释放。将 NCT-MAS 配合物和海藻酸钠 (SA) 作为药物载体和基质形成剂制成的口腔贴片,可以通过药物扩散和溶胀控制机制控制 NCT 的释放。随着 NCT-MAS 配合物或 SA 浓度的增加,NCT 的释放和膜渗透增加。所有含 NCT-MAS 的口腔贴片均表现出与 SA 和 MAS 溶胀特性相关的粘膜粘附特性。总之,NCT-MAS 配合物可以通过简单的单一混合步骤生产,所得到的配合物具有作为口腔基质制剂中药物载体的潜力。

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