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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.wascompared with the blood sugar level assayed by Folin-Malmoros method.In the lgC-t figure it is shown that the fatality of the drug in vivo was conform-ed with the single compartment model in which the peak time(tmax)was 0.5 hr,the peak value(Cmax)was 547 IU/ml and the eliminating half-life(t(1/2))was 0.27hr.The relative bioavailability of insulin suppository was 83%.The time for decreasing the blood sugar level to the minimum was 1.5 hr,whilethe time for blood insulin concentration peak was 0.5 hr.
【Key words】 Bioavailability; Insulin suppository; Surfactant NO-10; Radioimmunoassay;
- 【文献出处】 南京药学院学报 , 编辑部邮箱 ,1982年03期
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