Meyer B H, Müller F O, Clur B K, Grigoleit H G
Br J Clin Pharmacol. 1983 Aug;16(2):145-8. doi: 10.1111/j.1365-2125.1983.tb04978.x.
Tendamistate (Hoe 467) reduces gastrointestinal absorption of starch by inactivating α-amylase. Two trials were performed to investigate the influence of timing and mode of administration of tendamistate, relative to starch intake, on the pharmacodynamics of the drug. (i) In the first trial 400 mg enteric coated capsules, 400 mg non-enteric coated capsules and placebo were compared in 12 volunteers. Medication (400 mg tendamistate capsules or placebo) was administered after 10 h fasting, 15 min before a starch meal. Post-prandial plasma glucose concentration-time curves were plotted. No significant differences could be shown between tendamistate capsules and placebo in respect of areas under the curve (AUC), maximal concentration () and time to maximal concentration (). No side effects were reported. (ii) In a second trial tendamistate powder, mixed with a starch meal, was compared with placebo in eight volunteers. Blood specimens for measurement of glucose, insulin and C-peptide were taken up to 8 h after this starch meal. AUC as well as in respect of glucose values were significantly lower after Hoe 467 plus starch than after placebo plus starch. Insulin and C-peptide values were closely correlated with glucose. Flatulence and diarrhoea were reported by two subjects. It is concluded that the administration of tendamistate with, but not prior to, starch ingestion is effective in reducing post-prandial glucose levels.
坦地铵（Hoe 467）通过使α-淀粉酶失活来减少淀粉的胃肠道吸收。进行了两项试验，以研究坦地铵相对于淀粉摄入的给药时间和给药方式对该药物药效学的影响。（i）在第一项试验中，对12名志愿者比较了400毫克肠溶胶囊、400毫克非肠溶胶囊和安慰剂。禁食10小时后，在淀粉餐前进食15分钟时服用药物（400毫克坦地铵胶囊或安慰剂）。绘制餐后血浆葡萄糖浓度-时间曲线。坦地铵胶囊和安慰剂在曲线下面积（AUC）、最大浓度（）和达到最大浓度的时间（）方面无显著差异。未报告有副作用。（ii）在第二项试验中，将与淀粉餐混合的坦地铵粉末与八名志愿者的安慰剂进行比较。在该淀粉餐后长达8小时采集用于测量葡萄糖、胰岛素和C肽的血样。与安慰剂加淀粉相比，Hoe 467加淀粉后葡萄糖值的AUC以及均显著降低。胰岛素和C肽值与葡萄糖密切相关。两名受试者报告有肠胃胀气和腹泻。得出的结论是，在摄入淀粉时而非之前服用坦地铵可有效降低餐后血糖水平。
