Diabetes is characterized by chronic hyperglycemia. Although metformin hydrochloride (MHCl)- and glyburide (GLB)-containing conventional tablets are available in the market and used to treat diabetes, orally disintegrating tablets (ODTs) containing the combination of these drugs are not commercially available. Therefore, the aim of this study was to prepare ODTs containing MHCl and GLB by direct-compression (DC-ODTs) and freeze-drying (FD-ODTs) methods. Physical properties of the powder mixture of DC-ODT formulation were determined (Angle of repose: 37.18 ± 1.27°; compressibility index: 20.31 ± 1.06%; Hausner ratio: 1.25 ± 0.03). Its moisture content was 0.3 ± 0.09%. The hardness values and the disintegration times for DC-ODTs and FD-ODTs were 221.60 ± 40.82 and 66.54 ± 2.68 N, and 80 and 30 s, respectively. Friability values were 0.24% for DC-ODTs and 0.38% for FD-ODTs. In uniformity-of-mass for single-dose-preparations test, the average weight was 684.38 ± 1.97 mg for DC-ODTs and 342.93 ± 2.4 mg for FD-ODTs, with less than 5% deviation for all 20 tablets. Water-absorption ratio for DC-ODTs was 1.30 ± 0.05. More than 90% of MHCl and GLB were dissolved within 5 min in both DC-ODTs and FD-ODTs. Although Caco-2 permeability of MHCl was influenced by the ODTs, GLB permeability was not. These results indicated that MHCl- and GLB-containing ODTs may be used as promising formulations for the treatment of diabetes.

糖尿病的特征在于慢性高血糖症。尽管含二甲双胍盐酸盐（MHCl）和格列本脲（GLB）的常规片剂在市场上可以买到并用于治疗糖尿病，但包含这些药物组合的口腔崩解片（ODT）尚不市售。因此，本研究的目的是通过直接压缩（DC-ODT）和冷冻干燥（FD-ODT）方法制备含有MHCl和GLB的ODT。测定DC-ODT制剂的粉末混合物的物理性质（休止角：37.18±1.27°；可压缩性指数：20.31±1.06％；豪斯纳比：1.25±0.03）。其水分含量为0.3±0.09％。DC-ODT和FD-ODT的硬度值和崩解时间分别为221.60±40.82和66.54±2.68 N，以及80和30 s。脆性值为0。DC-ODT为24％，FD-ODT为0.38％。在单剂量制剂的质量均匀性测试中，DC-ODT的平均重量为684.38±1.97 mg，FD-ODT的平均重量为342.93±2.4 mg，所有20片的偏差均小于5％。DC-ODT的吸水率为1.30±0.05。在5分钟内，超过90％的MHCl和GLB溶解在DC-ODT和FD-ODT中。虽然MHCl的Caco-2渗透性受ODT的影响，但GLB渗透性不受影响。这些结果表明，含有MHCl和GLB的ODT可用作治疗糖尿病的有希望的制剂。在5分钟内，超过90％的MHCl和GLB溶解在DC-ODT和FD-ODT中。虽然MHCl的Caco-2渗透性受ODT的影响，但GLB渗透性不受影响。这些结果表明，含有MHCl和GLB的ODT可用作治疗糖尿病的有希望的制剂。在5分钟内，超过90％的MHCl和GLB溶解在DC-ODT和FD-ODT中。尽管MDT的Caco-2渗透性受ODT的影响，但GLB的渗透性不受影响。这些结果表明，含有MHCl和GLB的ODT可用作治疗糖尿病的有希望的制剂。