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采用共晶方法作为一种有前景的药物递送系统，使用咪唑共形成剂提高芒柄花素的溶出度和生物利用度。

Using the Cocrystal Approach as a Promising Drug Delivery System to Enhance the Dissolution and Bioavailability of Formononetin Using an Imidazole Coformer.

作者信息

Kim Jongyeob, Lim Sohyeon, Kim Minseon, Ban Eunmi, Kim Yongae, Kim Aeri

机构信息

College of Pharmacy, CHA University, Seongnam 13844, Republic of Korea.

Department of Chemistry, Hankuk University of Foreign Studies, Yongin 17035, Republic of Korea.

出版信息

Pharmaceuticals (Basel). 2024 Oct 28;17(11):1444. doi: 10.3390/ph17111444.

DOI:10.3390/ph17111444
PMID:39598356
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11597446/
Abstract

Natural isoflavones are recognized for their diverse pharmacological activities; however, their low aqueous solubility presents a significant challenge for further development. Here, we aimed to develop a cocrystal of formononetin (FMN) to improve its solubility. The formononetin-imidazole (FMN-IMD) cocrystal was prepared using liquid-assisted grinding method. The prepared cocrystal was identified through a thermal analysis of physical mixtures with various coformers. FTIR and solid-state NMR confirmed the presence of hydrogen bonds and π-π interactions in the FMN-IMD cocrystal. The solubility of FMN-IMD was two to three times higher than that of crystalline FMN. The FMN-IMD cocrystal showed a 4.93-fold increase in the Cmax value and a 3.58-fold increase in the AUC compared to FMN after oral administration in rats. There were no changes in the PXRD of the FMN-IMD cocrystal after six months of storage at 40 °C. Thus, the FMN-IMD cocrystal is proposed as an effective solid form for oral delivery, offering enhanced solubility and physical stability.

摘要

天然异黄酮因其多样的药理活性而受到认可；然而，它们在水中的低溶解度对其进一步开发构成了重大挑战。在此，我们旨在开发一种芒柄花素（FMN）共晶以提高其溶解度。采用液体辅助研磨法制备了芒柄花素 - 咪唑（FMN - IMD）共晶。通过对与各种共形成物的物理混合物进行热分析来鉴定所制备的共晶。傅里叶变换红外光谱（FTIR）和固态核磁共振（NMR）证实了FMN - IMD共晶中存在氢键和π - π相互作用。FMN - IMD的溶解度比结晶FMN高两到三倍。在大鼠口服给药后，与FMN相比，FMN - IMD共晶的Cmax值增加了4.93倍，AUC增加了3.58倍。在40°C下储存六个月后，FMN - IMD共晶的粉末X射线衍射（PXRD）没有变化。因此，FMN - IMD共晶被认为是一种有效的口服给药固体形式，具有增强的溶解度和物理稳定性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a09/11597446/c883558a6117/pharmaceuticals-17-01444-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a09/11597446/77954102f6aa/pharmaceuticals-17-01444-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a09/11597446/9ef93bf58352/pharmaceuticals-17-01444-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a09/11597446/b1e0acd30fbd/pharmaceuticals-17-01444-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a09/11597446/d709c917c26e/pharmaceuticals-17-01444-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a09/11597446/44ac8dfa5116/pharmaceuticals-17-01444-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a09/11597446/7fbc6a5216ee/pharmaceuticals-17-01444-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a09/11597446/95749a4b5394/pharmaceuticals-17-01444-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a09/11597446/5a4e275a4b5b/pharmaceuticals-17-01444-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a09/11597446/4476fedcc901/pharmaceuticals-17-01444-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a09/11597446/6014ef15c5bd/pharmaceuticals-17-01444-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a09/11597446/c883558a6117/pharmaceuticals-17-01444-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a09/11597446/77954102f6aa/pharmaceuticals-17-01444-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a09/11597446/9ef93bf58352/pharmaceuticals-17-01444-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a09/11597446/b1e0acd30fbd/pharmaceuticals-17-01444-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a09/11597446/d709c917c26e/pharmaceuticals-17-01444-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a09/11597446/44ac8dfa5116/pharmaceuticals-17-01444-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a09/11597446/7fbc6a5216ee/pharmaceuticals-17-01444-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a09/11597446/95749a4b5394/pharmaceuticals-17-01444-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a09/11597446/5a4e275a4b5b/pharmaceuticals-17-01444-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a09/11597446/4476fedcc901/pharmaceuticals-17-01444-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a09/11597446/6014ef15c5bd/pharmaceuticals-17-01444-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1a09/11597446/c883558a6117/pharmaceuticals-17-01444-g010.jpg

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