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采用核磁共振晶体学方法对槲皮素膳食补充剂整片制剂中活性成分的高灵敏度固体形态鉴别。

Highly sensitive solid forms discrimination on the whole tablet of the active ingredients in quercetin dietary supplements by NMR crystallography approaches.

作者信息

Miclaus Maria O, Filip Xenia, Filip Claudiu, Martin Flavia A, Grosu Ioana G

机构信息

National Institute for Research and Development of Isotopic and Molecular Technologies, 400293 Cluj-Napoca, Romania; Babeş-Bolyai University, Faculty of Physics, Mihail Kogalniceanu, no. 1, RO-400084 Cluj-Napoca, Romania.

National Institute for Research and Development of Isotopic and Molecular Technologies, 400293 Cluj-Napoca, Romania.

出版信息

J Pharm Biomed Anal. 2016 May 30;124:274-280. doi: 10.1016/j.jpba.2016.03.006. Epub 2016 Mar 4.

Abstract

Similarly to synthetic drugs, the exact crystalline form of active ingredients in solid formulations of dietary supplements may directly influence the dissolution rate, bioavailability, and stability of the final product, but this information is usually not provided by manufacturers. Working on the examples of two commercial quercetin dietary supplements a quick, reliable, and sensitive method is introduced for quercetin solid forms discrimination directly on the marketed products, without the need for prior sample preparation. It exploits the complementarity between solid-state Nuclear Magnetic Resonance (ss-NMR) and Powder X-Ray Diffraction (PXRD), which proved essential for performing a complete and accurate solid-state characterization of the two commercial products, and for obtaining new insights into the complex quercetin solid-forms landscape. The method can be readily generalized also to other dietary supplements based on bio-flavonoids/polyphenols.

摘要

与合成药物类似,膳食补充剂固体剂型中活性成分的确切晶体形式可能直接影响最终产品的溶解速率、生物利用度和稳定性,但制造商通常不会提供此类信息。以两种市售槲皮素膳食补充剂为例,介绍了一种快速、可靠且灵敏的方法,可直接在市售产品上鉴别槲皮素的固体形式,无需事先进行样品制备。该方法利用了固态核磁共振(ss-NMR)和粉末X射线衍射(PXRD)之间的互补性,事实证明,这对于对两种市售产品进行完整而准确的固态表征以及深入了解复杂的槲皮素固体形式情况至关重要。该方法也可以很容易地推广到其他基于生物类黄酮/多酚的膳食补充剂。

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