Gault H, Kalra J, Ahmed M, Kepkay D, Barrowman J
Clin Pharmacol Ther. 1980 Jan;27(1):16-21. doi: 10.1038/clpt.1980.3.
3H-digoxin-12 alpha and unlabeled digoxin were administered down a nasogastric tube and digoxin, digoxyigenin and its mono- and bis-digitoxosides, and pH were assayed in gastric fluid of 6 healthy subjects at intervals for 90 min each under 4 conditions: pentagastrin infusion 6 micrograms/kg/hr with the subjects ambulatory and supine, and saline infusion ambulatory and supine. Intragastric hydrolysis occurred at roughly the same rate as reported in vitro. At 90 min, an average of 12.5% of the radioactivity that remained in the gastric fluid was recovered as digoxin for the 2 conditions when pentagastrin was infused, compared with 52.5% for th 2 conditions when saline was infused. The main glycosidic metabolite was digoxigenin and the amount correlated closely with the hydrogen ion activity in gastric fluid at 90 min (r = 0.83, p less than 0.01). Only minor differences were found between the supine and ambulatory conditions. The clinical significance of these results remains to be determined.
将3H-地高辛-12α和未标记的地高辛经鼻胃管给药，在4种条件下，对6名健康受试者的胃液每隔一段时间进行90分钟的检测，测定其中地高辛、洋地黄毒苷及其单洋地黄毒糖苷和双洋地黄毒糖苷以及pH值：静脉输注五肽胃泌素6微克/千克/小时，受试者活动和仰卧状态，以及静脉输注生理盐水，受试者活动和仰卧状态。胃内水解发生的速率与体外报道的大致相同。90分钟时，在输注五肽胃泌素的2种条件下，胃液中残留放射性的平均12.5%以地高辛形式回收，而在输注生理盐水的2种条件下，这一比例为52.5%。主要的糖苷代谢产物是洋地黄毒苷，其含量与90分钟时胃液中的氢离子活性密切相关（r = 0.83，p < 0.01）。仰卧和活动状态之间仅发现微小差异。这些结果的临床意义尚待确定。
