Yamasaki Y, Shichiri M, Kawamori R, Kikuchi M, Yagi T, Arai S, Tohdo R, Hakui N, Oji N, Abe H
Diabetes Care. 1981 Jul-Aug;4(4):454-8. doi: 10.2337/diacare.4.4.454.
The effectiveness of insulin administration by rectal suppository was examined in normal and non-insulin-dependent nonobese diabetic subjects. A 100-U insulin suppository (mean 1.8 U/kg) given to the diabetic subjects caused four times as great a fall in plasma glucose compared with the normal subjects given the same dose (mean 1.6 U/kg). The insulin response after suppository administration demonstrated a significantly positive correlation (r = 0.83, P less than 0.01) with the plasma glucose level before administration. Diabetic subjects given a 100-U insulin suppository (mean 1.7 U/kg) 15 min after meals three times daily showed a significant (P less than 0.05) improvement in postprandial hyperglycemia accompanied by a restoration of the normal circadian profile of plasma IRI and a reduction of urinary glucose from 26 +/- 5.9 to 2.0 +/- 1.0 g/day. No untoward reactions were observed. These data strongly imply a unique characteristic of the insulin suppository in spite of low bioavailability.
在正常和非胰岛素依赖型非肥胖糖尿病受试者中检测了直肠栓剂给药胰岛素的有效性。给予糖尿病受试者100单位胰岛素栓剂(平均1.8单位/千克)导致血浆葡萄糖下降幅度是给予相同剂量(平均1.6单位/千克)正常受试者的四倍。栓剂给药后的胰岛素反应与给药前的血浆葡萄糖水平呈显著正相关(r = 0.83,P<0.01)。糖尿病受试者每日三餐后15分钟给予100单位胰岛素栓剂(平均1.7单位/千克),餐后高血糖有显著改善(P<0.05),同时血浆IRI的正常昼夜节律得以恢复,尿糖从26±5.9克/天降至2.0±1.0克/天。未观察到不良反应。尽管生物利用度较低,但这些数据强烈暗示了胰岛素栓剂的独特特性。