Federlin K F, Mehlburger L, Hillebrand I, Laube H
III. Medizinische Klinik und Poliklinik, Universität Giessen, FRG.
Acta Diabetol Lat. 1987 Jul-Sep;24(3):213-21. doi: 10.1007/BF02732040.
Two new glucosidase inhibitors (BAY m 1099 and BAY o 1248) were studied in volunteers and type II diabetics under various conditions. In 6 non-diabetic controls BAY m 1099 when given 3 X 50 mg/day caused a marked depression of the post-meal glucose rise. The effect was found to be more marked after breakfast than after lunch or after dinner. In type II diabetics BAY m 1099, when given in a dose of 2 X 25 mg/day over one week, had no significant effect on post-meal glucose or serum insulin levels. BAY o 1248, when given as a single dose of 15 mg in the morning to type II diabetics, induced a significant decrease of post-meal glucose rise (35 mg/dl after breakfast, 25 mg/dl after lunch) when compared to placebo. Although in parallel serum insulin levels were slightly lower, this change was statistically not significant. The drug reduced glycosuria by 50%. Both compounds induced side effects, such as flatulence or diarrhea when given in therapeutically effective amounts, but were tolerable in most cases. On a weight basis BAY o 1248 was found to have greater therapeutic effects than BAY m 1099. Both drugs can be recommended for use in unsatisfactorily controlled type II diabetics. Further studies should concentrate on the critical dosage which may strike a satisfactory balance between effects and side effects.
在不同条件下,对志愿者和II型糖尿病患者研究了两种新型葡糖苷酶抑制剂(BAY m 1099和BAY o 1248)。在6名非糖尿病对照者中,BAY m 1099按每日3次、每次50 mg给药时,可显著抑制餐后血糖升高。发现早餐后这种作用比午餐或晚餐后更明显。在II型糖尿病患者中,BAY m 1099以每日2次、每次25 mg的剂量给药一周,对餐后血糖或血清胰岛素水平无显著影响。BAY o 1248在早晨给II型糖尿病患者单次口服15 mg时,与安慰剂相比,可显著降低餐后血糖升高幅度(早餐后降低35 mg/dl,午餐后降低25 mg/dl)。尽管同时血清胰岛素水平略有降低,但这种变化在统计学上不显著。该药物可使糖尿减少50%。两种化合物在给予治疗有效量时均会引起副作用,如肠胃胀气或腹泻,但在大多数情况下可以耐受。按重量计算,发现BAY o 1248比BAY m 1099具有更大的治疗效果。两种药物均可推荐用于控制不佳的II型糖尿病患者。进一步的研究应集中在可能在疗效和副作用之间取得满意平衡的关键剂量上。