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利帕林 I 的固态形式特征。

Solid-State Form Characterization of Riparin I.

机构信息

Pharmaceutical Sciences Departament, Federal University of Paraíba, University City, João Pessoa PB 58059-970, Brazil.

Biotechnology Departament, Federal University of Paraíba, University City, João Pessoa PB 58059-970, Brazil.

出版信息

Molecules. 2017 Oct 9;22(10):1615. doi: 10.3390/molecules22101615.

DOI:10.3390/molecules22101615
PMID:28991202
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6151621/
Abstract

Riparin I is an alkamide with potential anxiolytic activity in preclinical studies. The characterization and understanding of solid-state properties play an importance role in drug development. For this work, the solid state of five riparin I batches (RIP-1, RIP-2, RIP-3, RIP-4, and RIP-5), obtained by the same synthesis process, were characterized by Scanning Electron Microscopy (SEM), Differential Scanning Calorimetry (DSC), DSC-photovisual, Thermogravimetry (TG), Fourier Transform Infrared (FTIR), Pyrolysis (Pyr-GC/MS), X-ray Powder Diffraction (PXRD), and Solid-State Nuclear Magnetic Resonance (ssNMR) techniques. Batches of riparin I with different crystal habits resulting in crystallization impurities were observed, which can be attributed to the presence of triethylamine. The main differences were observed by DSC, PXRD, and ssNMR analysis. DSC curves of RIP-2 and RIP-3 presented endothermic peaks at different temperatures of fusion, which can be attributed to the mixture of different crystalline forms. PXRD and ssNMR results confirmed crystallinity differences. The results offer evidence of the importance of controlling the reproducibility of the synthesis in order to obtain the adequate morphology for therapeutic efficacy and avoiding future problems in quality control of riparin I products.

摘要

利帕林 I 是一种具有潜在抗焦虑活性的醇酰胺，在临床前研究中。对固体状态特性的表征和理解在药物开发中起着重要作用。在这项工作中，通过相同的合成工艺获得的五个利帕林 I 批次（RIP-1、RIP-2、RIP-3、RIP-4 和 RIP-5）的固体状态通过扫描电子显微镜（SEM）、差示扫描量热法（DSC）、DSC-光电、热重分析（TG）、傅立叶变换红外光谱（FTIR）、热解（Pyr-GC/MS）、X 射线粉末衍射（PXRD）和固态核磁共振（ssNMR）技术进行了表征。观察到具有不同晶体习性的利帕林 I 批次产生结晶杂质，这可归因于三乙胺的存在。DSC、PXRD 和 ssNMR 分析观察到主要差异。RIP-2 和 RIP-3 的 DSC 曲线在不同的熔融温度呈现吸热峰，这可归因于不同晶型的混合物。PXRD 和 ssNMR 结果证实了结晶度的差异。结果表明，为了获得治疗效果所需的合适形态并避免利帕林 I 产品质量控制方面的未来问题，控制合成的重现性非常重要。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d51b/6151621/b05357287607/molecules-22-01615-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d51b/6151621/126f957e1edc/molecules-22-01615-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d51b/6151621/9ced62376f53/molecules-22-01615-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d51b/6151621/6d35bd45df2d/molecules-22-01615-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d51b/6151621/32aec1738559/molecules-22-01615-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d51b/6151621/2fdb1a66e73d/molecules-22-01615-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d51b/6151621/39df63af7a16/molecules-22-01615-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d51b/6151621/8f1e9161befa/molecules-22-01615-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d51b/6151621/b05357287607/molecules-22-01615-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d51b/6151621/126f957e1edc/molecules-22-01615-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d51b/6151621/9ced62376f53/molecules-22-01615-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d51b/6151621/6d35bd45df2d/molecules-22-01615-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d51b/6151621/32aec1738559/molecules-22-01615-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d51b/6151621/2fdb1a66e73d/molecules-22-01615-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d51b/6151621/39df63af7a16/molecules-22-01615-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d51b/6151621/8f1e9161befa/molecules-22-01615-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d51b/6151621/b05357287607/molecules-22-01615-g008.jpg

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Molecular perspectives on solid-state phase transformation and chemical reactivity of drugs: metoclopramide as an example.药物固态相变和化学反应性的分子视角：以甲氧氯普胺为例。
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Talanta. 2011 Oct 30;86:233-40. doi: 10.1016/j.talanta.2011.09.008. Epub 2011 Sep 10.
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