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新型水杨苷 - 环糊精复合物的制备与表征

Preparation and Characterization of a Novel Salicin-Cyclodextrin Complex.

作者信息

Căta Adina, Ienaşcu Ioana Maria Carmen, Frum Adina, Ursu Daniel, Svera Paula, Orha Corina, Rusu Gerlinde, Chiș Adriana Aurelia, Dobrea Carmen Maximiliana, Morgovan Claudiu, Pop Oana-Raluca

机构信息

National Institute of Research and Development for Electrochemistry and Condensed Matter, 144 Dr. A. P. Podeanu, 300569 Timişoara, Romania.

Department of Pharmaceutical Sciences, Faculty of Pharmacy, "Vasile Goldiș" Western University of Arad, 86 Liviu Rebreanu, 310045 Arad, Romania.

出版信息

Pharmaceutics. 2024 Mar 6;16(3):369. doi: 10.3390/pharmaceutics16030369.

Abstract

Bioactive compounds extracted from plants can provide wide health benefits. However, some molecules have limited applications as pharmaceuticals due to their limited solubility, poor bioavailability, and low stability when exposed to environmental factors. Their integration in formulations that can deliver them to physiological targets while preserving their biological activity can enhance their usage in improving human health. This research provides a delivery system design to enhance the solubility, stability and to mask the bitter taste of salicin. Thus, a novel salicin-β-cyclodextrin complex was prepared and analyzed by X-ray diffraction, scanning electron microscopy, thermogravimetric analysis, FTIR, Raman and UV-Vis spectroscopy. The analytical and computational methods provided clear and distinct evidence for inclusion of salicin within the β-cyclodextrin cavity and brought important findings for the characterization of the inclusion complex. The present study showed that salicin and β-cyclodextrin can form inclusion complexes, both in solution and in solid state, and that the inclusion of salicin in the cavity of β-cyclodextrin leads to the improvement of its solubility and stability. Thus, the study communicates both qualitative and quantitative knowledge about the preparation of a new salicin-β-cyclodextrin inclusion complex suggesting its potential applications in pharmaceutical industry and medical sciences, as formulations with better compliance for the patient, with increased bioavailability, and easier control of dosage.

摘要

从植物中提取的生物活性化合物具有广泛的健康益处。然而,一些分子由于其溶解度有限、生物利用度差以及在暴露于环境因素时稳定性低,作为药物的应用受到限制。将它们整合到能够将其递送至生理靶点同时保留其生物活性的制剂中,可以提高它们在改善人类健康方面的用途。本研究提供了一种递送系统设计,以提高水杨苷的溶解度、稳定性并掩盖其苦味。因此,制备了一种新型的水杨苷-β-环糊精复合物,并通过X射线衍射、扫描电子显微镜、热重分析、傅里叶变换红外光谱、拉曼光谱和紫外可见光谱进行了分析。分析和计算方法为水杨苷包合在β-环糊精腔内提供了清晰明确的证据,并为包合物的表征带来了重要发现。本研究表明,水杨苷和β-环糊精在溶液和固态中均可形成包合物,并且水杨苷包合在β-环糊精腔内可提高其溶解度和稳定性。因此,该研究传达了关于新型水杨苷-β-环糊精包合物制备的定性和定量知识,表明其在制药工业和医学科学中的潜在应用,作为对患者依从性更好、生物利用度更高且剂量控制更容易的制剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6a1b/10976097/816b36966253/pharmaceutics-16-00369-g001.jpg

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