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冷冻干燥法制备的β-葡萄糖苷酶抑制剂/环糊精复合物的表征

Characterization of -Glucosidase Inhibitor/Cyclodextrin Complex Prepared by Freeze-Drying.

作者信息

Inoue Yutaka, Narumi Sachie, Mitsumori Akiho, Murata Isamu, Kanamoto Ikuo

机构信息

Laboratory of Drug Safety Management, Faculty of Pharmacy and Pharmaceutical Sciences, Josai University, 1-1 Keyakidai, Sakado-shi, Saitama 3500295, Japan.

出版信息

J Pharm (Cairo). 2018 May 7;2018:3202719. doi: 10.1155/2018/3202719. eCollection 2018.

Abstract

Miglitol (MT) is an -glucosidase inhibitor with a postmeal blood glucose level lowering effect that is used to treat type 2 diabetes. In addition, -cyclodextrin (CD) has been reported to inhibit increases in postmeal blood glucose. The aim of this study was to prepare a freeze-dried product (FD) composed of MT and CD or CD (molar ratio of MT/CD = 1/1, MT/CD = 1/1) and to evaluate the physicochemical properties and biological activity of the FD. The PXRD profile of FD exhibited a halo pattern, and characteristic peaks derived from MT, CD, and CD were not observed. The TG-DTA results for FD indicated an increased weight loss temperature and the absence of an endothermic peak for MT. The NIR absorption spectrum measurement suggested an intermolecular interaction between MT and CD or CD in the FD. H-H NOESY NMR spectroscopy (DO) revealed an intermolecular interaction in the FD. The results of the -glucosidase activity inhibition test and the -amylase activity inhibition test indicated that the FD exhibited the same inhibition rate as MT alone and the effects of MT were not altered by the freeze-drying method.

摘要

米格列醇(MT)是一种具有降低餐后血糖水平作用的α-葡萄糖苷酶抑制剂,用于治疗2型糖尿病。此外,据报道,β-环糊精(CD)可抑制餐后血糖升高。本研究的目的是制备由MT和CD或γ-环糊精(MT/CD = 1/1,MT/γ-CD = 1/1摩尔比)组成的冻干产品(FD),并评估该FD的物理化学性质和生物活性。FD的粉末X射线衍射(PXRD)图谱呈现出晕圈模式,未观察到源自MT、CD和γ-CD的特征峰。FD的热重-差示热分析(TG-DTA)结果表明失重温度升高,且未出现MT的吸热峰。近红外(NIR)吸收光谱测量表明FD中MT与CD或γ-CD之间存在分子间相互作用。异核单量子相干核磁共振(H-H NOESY NMR)光谱(D2O)揭示了FD中的分子间相互作用。α-葡萄糖苷酶活性抑制试验和α-淀粉酶活性抑制试验的结果表明,FD表现出与单独MT相同的抑制率,且冻干方法未改变MT的作用效果。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d32f/5964620/3eba66d02799/JPHAR2018-3202719.001.jpg

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