Ruppin H, Hagel J, Feuerbach W, Schutt H, Pichl J, Hillebrand I, Bloom S, Domschke W
Department of Medicine, University of Erlangen-Nuremberg, Federal Republic of Germany.
Gastroenterology. 1988 Jul;95(1):93-9. doi: 10.1016/0016-5085(88)90295-8.
The alpha-glucosidase inhibitor acarbose has been successfully used in diabetic patients to decrease the postprandial rise in blood glucose. The aim of the present experiments was to investigate the fate and effects of acarbose along the small intestine using a slow-marker perfusion technique. In 8 healthy volunteers, jejunal and ileal loads of acarbose, glucose, and total carbohydrates were determined following a liquid, 400-kcal formula meal containing either 200 mg of acarbose or placebo. Preprandial and postprandial plasma concentrations of glucose and several polypeptide hormones were determined. Recovery of acarbose during 4 h was 65% +/- 9% (mean +/- SEM) of ingested dose in the ileum but 94% +/- 9% in the jejunum, indicating that the compound was neither degraded nor absorbed by the intestine to a major degree. After acarbose administration, ileal loads of glucose and total carbohydrates were considerably higher, whereas postprandial plasma concentrations of glucose, insulin, and gastric inhibitory polypeptide were lower when compared with placebo. The retardation of carbohydrate digestion to be inferred from these findings is confirmed by significantly elevated plasma concentrations of enteroglucagon after acarbose administration compared with placebo administration.
α-葡萄糖苷酶抑制剂阿卡波糖已成功用于糖尿病患者，以降低餐后血糖升高。本实验的目的是使用慢标记灌注技术研究阿卡波糖在小肠中的转归和作用。在8名健康志愿者中，给予含200mg阿卡波糖或安慰剂的400千卡液体配方餐后，测定空肠和回肠中阿卡波糖、葡萄糖和总碳水化合物的含量。测定餐前和餐后血浆葡萄糖和几种多肽激素的浓度。阿卡波糖在回肠4小时内的回收率为摄入剂量的65%±9%（平均值±标准误），而在空肠中为94%±9%，这表明该化合物在肠道中既未被大量降解也未被大量吸收。与安慰剂相比，给予阿卡波糖后，回肠中的葡萄糖和总碳水化合物含量显著更高，而餐后血浆葡萄糖、胰岛素和胃抑制多肽的浓度更低。与给予安慰剂相比，给予阿卡波糖后血浆肠高血糖素浓度显著升高，证实了从这些发现中推断出的碳水化合物消化延迟。
