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地氯雷他定多组分晶体形成的合成、表征及稳定性研究。

Synthesis, characterization, and stability study of desloratadine multicomponent crystal formation.

作者信息

Ainurofiq Ahmad, Mauludin Rachmat, Mudhakir Diky, Soewandhi Sundani Nurono

机构信息

School of Pharmacy, Bandung Institute of Technology, Ganesha 10, Bandung, 40132, Indonesia.

Department of Pharmacy, Sebelas Maret University, Ir. Sutami 36A, Surakarta, 57126, Indonesia.

出版信息

Res Pharm Sci. 2018 Apr;13(2):93-102. doi: 10.4103/1735-5362.223775.

Abstract

This study describes the formation of multicomponent crystal (MCC) of desloratadine (DES). The objective of this study was to discover the new pharmaceutical MCC of DES using several coformers. The MCC synthesis was performed between DES and 26 coformers using an equimolar ratio with a solvent evaporation technique. The selection of the appropriate solvent was carried out using 12 solvents. The preview of the MCC of DES was performed using polarized light microscopy (PLM). The formation of MCC was confirmed using powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), fourier transform infrared spectroscopy (FTIR), and scanning electron microscopy (SEM). The accelerated stability of MCC at 40 °C and relative humidity of 75% was investigated using PXRD and FTIR. Depending on the prior evaluation, DES and benzoic acid (BA) formed the MCC. PLM and SEM results showed that crystal habit of combination between DES and BA differed from the constituent components. Moreover, the diffractogram pattern of DES-BA was distinct from the constituent components. The DSC thermogram showed a new peak which was distinct from both constituent components. The FTIR study proved a new spectrum. All characterizations indicated that a new solid crystal was formed, ensuring the MCC formation. In addition, DES-BA MCC had both chemical and physical stabilities for a period of 4 months.

摘要

本研究描述了地氯雷他定(DES)多组分晶体(MCC)的形成。本研究的目的是使用几种共形成物发现DES的新型药物MCC。MCC的合成是在DES和26种共形成物之间以等摩尔比采用溶剂蒸发技术进行的。使用12种溶剂进行合适溶剂的选择。DES的MCC的预观察是使用偏光显微镜(PLM)进行的。使用粉末X射线衍射(PXRD)、差示扫描量热法(DSC)、傅里叶变换红外光谱(FTIR)和扫描电子显微镜(SEM)确认MCC的形成。使用PXRD和FTIR研究了MCC在40°C和75%相对湿度下的加速稳定性。根据先前的评估,DES和苯甲酸(BA)形成了MCC。PLM和SEM结果表明,DES和BA组合的晶体习性与组成成分不同。此外,DES-BA的衍射图谱与组成成分不同。DSC热重曲线显示出一个与两种组成成分都不同的新峰。FTIR研究证明了一个新的光谱。所有表征都表明形成了一种新的固体晶体,确保了MCC的形成。此外,DES-BA MCC在4个月内具有化学和物理稳定性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bc9f/5842490/6746a7498099/RPS-13-93-g001.jpg

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