Abstract

Miglitol (MT) is an α-glucosidase inhibitor with a postmeal blood glucose level lowering effect that is used to treat type 2 diabetes. In addition, α-cyclodextrin (αCD) 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 αCD or γCD (molar ratio of MT/αCD = 1/1, MT/γCD = 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, αCD, and γCD 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 αCD or γCD in the FD. 1H-1H NOESY NMR spectroscopy (D2O) revealed an intermolecular interaction in the FD. The results of the α-glucosidase activity inhibition test and the α-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.

Highlights

  • The incidence of diabetes has increased in developed countries

  • Thereafter, the prefrozen product was freeze-dried in a vacuum freeze-dryer (FZ-6 model manufactured by ALS Co., Ltd.) for 24 h to produce the freeze-dried product (FD)

  • Powder X-Ray Diffraction (PXRD) was performed to examine the crystalline state of MT and CDs in the FD (MT/αCD) and FD (MT/γCD) preparations (Figure 2)

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Summary

Introduction

The incidence of diabetes has increased in developed countries. This has been attributed to smoking, an inadequate diet, and lack of exercise, and diabetes has become a major cause of the increasing death rate [1]. According to the International Diabetes Federation report, the world diabetes population continues to increase and in 2015, 415 million people were suffering from diabetes For this reason, the treatment of prediabetes by controlling blood glucose at levels lower than that required for a diabetes diagnosis to prevent the development of full blown diabetes has been gaining attention. MT is different from the other two drugs and is quickly absorbed in the upper part of the small intestine This characteristic suppresses the rise in blood glucose level starting 30 min after a meal and continuing until 2 h after a meal. This study focused on MT and aimed to develop a formulation that would provide an additive synergistic suppressive effect on blood glucose elevation by forming a complex with αCD.

Materials and Methods
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