胰岛素直肠给药剂型研究 Ⅲ.用放射免疫分析法测定胰岛素栓家兔的生物利用度

Biopharmaceutical studies on insulin rectal dosage form . Ⅲ.Bioavailability of insulin suppositories in rabbits by radioimmunoassay.

摘要: 本文报导了用可可豆油做基质含有1%表面活性剂(NO-10)的胰岛素栓(剂量按家兔体重3IU/kg 计)家兔直肠吸收的研究,并用胰岛素灌肠剂作对照。用放射免疫法测定各间隔时间的胰岛素血浓度并和用 Folin Malmoros 法测得的血糖浓度进行对比。从得到的 lg C-t 图中看出,胰岛素在体内的转运过程为单隔室模型,达峰时((?)max)为0.5hr,峰值为547 IU/kg,消除半衰期(t~1/2)为0.27hr,测得胰岛素栓的相对生物利用度为83%。实验结果看出,3 IU/kg 剂量的胰岛素栓直肠给药后,家免血糖在1.5小时时降至最低,胰岛素血浓度在0.5小时时出现峰值。

Abstract: Insulin suppositories prepared with cocoa butter and 1 % surfactant NO-10 werestudied in rabbits at the dose of 3 IU/kg,and insulin enema was used as a control.The insulin level in blood at given intervals determined by radioimmunoassay was compared with the blood sugar level assayed by Folin-Malmoros method.In the lgG-t figure it is showm that the fatality of the drug in vivo was conformed with the single compartment model in which the peak time (tmax) was 0.5hr, the peak value (Cmax) was 547 IU/ml and the eliminating half-life(t 1/2) was 0.27 hr. The relative bioavailability of insulin suppository was 83%. The time for decreasing the blood sugar level to the minimum was 1.5 hr, while the time for blood insulin concentration peak was 0.5 hr.