Nelson-Piercy C, Hammond P J, Gwilliam M E, Khandan-Nia N, Myers M J, Ghatei M A, Bloom S R
Department of Diagnostic Physics, Royal Postgraduate Medical School, Hammersmith Hospital, London, United Kingdom.
J Clin Endocrinol Metab. 1994 Feb;78(2):329-36. doi: 10.1210/jcem.78.2.7906279.
Sixteen healthy male volunteers participated in a randomized, double blind, parallel groups study. Subjects received either 1 or 5 mg SDZ CO 611 (a new, orally active somatostatin analog) twice daily over a 14-day period and acted as their own controls. Gastric emptying of 99mTc and mouth to cecum transit time, as measured by the breath hydrogen technique, after a mixed meal containing lactulose and 99mTc-diethylenetriaminepentaacetate, were assessed once before, twice during, and once after the period of study medication. Gastric emptying of 99mTc was significantly accelerated by the higher dose of SDZ CO 611, whereas mouth to cecum transit time was prolonged by the drug in a dose-dependent manner. Both doses of SDZ CO 611 led to suppression of the fasting level and postprandial release of several gastrointestinal and pancreatic hormones. This effect was more marked in those subjects taking 10 mg/day of the study medication. Motilin and pancreatic polypeptide were the most sensitive to the inhibitory actions of the analog. Glucose tolerance was significantly impaired by the 10-mg dose of the drug. We conclude that this new, orally active derivative of somatostatin is as effective on the gastrointestinal tract as the sc somatostatin analog octreotide. It would, therefore, be a useful advance in the treatment of gastroenteropancreatic tumors.
16名健康男性志愿者参与了一项随机、双盲、平行组研究。受试者在14天内每日两次接受1毫克或5毫克的SDZ CO 611(一种新型口服活性生长抑素类似物),并作为自身对照。在含有乳果糖和99mTc-二乙烯三胺五乙酸的混合餐后,通过呼气氢技术测量99mTc的胃排空和口至盲肠转运时间,在研究用药期之前、期间两次以及之后各评估一次。较高剂量的SDZ CO 611显著加速了99mTc的胃排空,而口至盲肠转运时间则以剂量依赖方式被该药物延长。两种剂量的SDZ CO 611均导致几种胃肠和胰腺激素的空腹水平及餐后释放受到抑制。这种作用在服用10毫克/天研究药物的受试者中更为明显。胃动素和胰多肽对该类似物的抑制作用最为敏感。10毫克剂量的药物显著损害了葡萄糖耐量。我们得出结论,这种新型口服活性生长抑素衍生物在胃肠道上与皮下注射生长抑素类似物奥曲肽一样有效。因此,它将是胃肠胰腺肿瘤治疗方面的一项有益进展。