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胰岛素直肠给药剂型研究——Ι表面活性剂对胰岛素栓在家兔直肠吸收的影响

Biopharmaceutical Study of Insulin Rectal Dosage Form Ι:Effect of Surfactants on Rectal Absorption of Insulin Suppositories in Rabbits

  • 摘要: 在研制胰岛素新剂型的工作中,作者利用栓剂直肠给药的特点用家兔对胰岛素栓直肠给药剂量(以降低血糖值为指标)进行了研究,结果初步表明胰岛素能从直肠吸收,但有效剂量较大(50 IU/kg-75 IU/kg)表面活性剂有显著促进作用,使剂量减小能获得适宜的治疗剂量。作者研究了 Tween-80等九种表面活性剂,观察了它们的降糖效果。其顺序为:NO-10>十二烷基硫酸钠>聚氧乙烯月桂醚(Brij 35)>聚氧乙烯蓖麻油>Cremophor EL>去氧胆酸>Cremophor RH40>卵磷脂>Tween-80

     

    Abstract: The suitability of insulin administration in suppcsitory by using different surfactants was studied. The effect of surfactants on rectal absorption of insulin from rabbit rectum was examined by measuring the blood sugar level after each administration of various doses. Nine selected surfactants and their order of enhancing the rectal absorption of insulin were observed: NO - 10, Sodium Lauryl sulphate, Polyoxylene lauryl ether, Polyoxyethylene Castor Oil, Cremopher KL, Deoxychlolic acid, Cremophor RH4O, Lecithin, Tween - 80. The optimal effect (lowering blocd sugar level) was reached with 1% of NO - 10. Insulin Suppository containing selected surfactant enhances its rectal absorption which was comparable with the absorption of intramuscular injection.

     

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