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两种新型α-葡萄糖苷酶抑制剂对正常志愿者混合餐代谢反应的影响。

The effect of two new alpha-glucosidase inhibitors on metabolic responses to a mixed meal in normal volunteers.

作者信息

Kennedy F P, Miles J M, Heiling V, Gerich J E

机构信息

Department of Medicine, Mayo Medical School, Rochester, Minnesota.

出版信息

Clin Exp Pharmacol Physiol. 1987 Aug;14(8):633-40. doi: 10.1111/j.1440-1681.1987.tb01884.x.

Abstract
  1. alpha-Glucosidase inhibitors delay carbohydrate absorption and have been proposed as adjunctive therapy for diabetes mellitus. 2. To determine the effects of two new alpha-glucosidase inhibitors, Bay-m-1099 and Bay-o-1248, on meal carbohydrate and lipid tolerance, plasma glucose, insulin and triglyceride levels were measured at 15-60 min intervals over 12 h after ingestion of a standard breakfast, lunch and dinner of identical composition in 31 normal volunteers. 3. The volunteers were randomized to receive either Bay-m-1099 (50 or 25 mg) or placebo prior to each meal, or the single administration of Bay-o-1248 (20 or 10 mg) or placebo prior to breakfast. 4. Only Bay-m-1099 at the 50 mg dose reduced significantly the postprandial increase in plasma insulin levels after each meal when compared with placebo (25, 36, 54% at breakfast, lunch, and dinner, respectively; P less than 0.05). Both drugs were well tolerated, with side effects limited to complaints of flatulence. 5. Thus, with the dosage schedule employed, Bay-m-1099, but not Bay-o-1248, significantly reduced postprandial increments in plasma insulin.
摘要
  1. α-葡萄糖苷酶抑制剂可延缓碳水化合物吸收,已被提议作为糖尿病的辅助治疗药物。2. 为了确定两种新型α-葡萄糖苷酶抑制剂Bay-m-1099和Bay-o-1248对餐时碳水化合物和脂质耐受性的影响,在31名正常志愿者摄入成分相同的标准早餐、午餐和晚餐后12小时内,每隔15 - 60分钟测量一次血浆葡萄糖、胰岛素和甘油三酯水平。3. 志愿者被随机分组,在每餐之前接受Bay-m-1099(50毫克或25毫克)或安慰剂,或者在早餐前单次服用Bay-o-1248(20毫克或10毫克)或安慰剂。4. 与安慰剂相比,仅50毫克剂量的Bay-m-1099显著降低了每餐餐后血浆胰岛素水平的升高(早餐、午餐和晚餐时分别降低25%、36%和54%;P < 0.05)。两种药物耐受性良好,副作用仅限于肠胃胀气的主诉。5. 因此,在所采用的给药方案下,Bay-m-1099而非Bay-o-1248显著降低了餐后血浆胰岛素的增量。

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