In vitro characteristics of an insulin suppository developed using palm oil base (HAMIN®) and its hypoglycaemic effect on rabbits

Q1 Biochemistry, Genetics and Molecular Biology Frontiers in Life Science Pub Date : 2015-07-03 DOI:10.1080/21553769.2015.1063549
Sritharan Nair, Z. Chik, M. I. Noordin
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引用次数: 1

Abstract

The long-term administration of insulin requires the development of new delivery routes. Using a base developed in-house, called HAMIN®, an insulin suppository containing 100 units (U) of insulin was formulated. The suppository was subjected to stability testing at various temperatures and the assay value was monitored. Other physical factors such as hardness, disintegration time, thermal analysis and dissolution were also tested. The suppository released more than 80% of its drug content in 30 min, and was stable for up to 11 months at −20°C. The suppository effect was studied on 11 New Zealand white rabbits, with body weight ranging from 1.6 to 2.1 kg. The results show that there was a marked reduction in glucose content when the suppository was inserted. The average drop in glucose content was 2.7 mmol/L in 15 min from the time of insertion. The maximum drop in glucose content reached 3.9 mmol/L in 2 h. Plasma insulin level, quantified using an enzyme-linked immunosorbent assay, showed a value of more than 100 µIU insulin/ml blood after 30 min. Although the insulin bioavailability was expectedly low, the rate at which the hypoglycaemic effect took place and the percentage of glucose reduction were comparable to results after subcutaneous injection.
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棕榈油基胰岛素栓剂(HAMIN®)的体外特性及其对家兔的降糖作用
胰岛素的长期给药需要开发新的给药途径。使用内部开发的基础,称为HAMIN®,胰岛素栓剂含有100单位(U)的胰岛素配制。在不同温度下对栓剂进行稳定性试验,并监测其测定值。其他物理因素如硬度、崩解时间、热分析和溶解也进行了测试。该栓剂在30分钟内释放80%以上的药物含量,并在- 20°C下稳定长达11个月。以11只体重1.6 ~ 2.1 kg的新西兰大白兔为实验对象,研究了栓剂的作用。结果表明,当栓剂插入时,葡萄糖含量显着降低。葡萄糖含量在15 min内平均下降2.7 mmol/L。葡萄糖含量在2 h内最大下降3.9 mmol/L。血浆胰岛素水平,用酶联免疫吸附法定量,显示30分钟后超过100 μ IU胰岛素/ml血。虽然胰岛素的生物利用度预期较低,但降糖效果发生的速度和葡萄糖减少的百分比与皮下注射后的结果相当。
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来源期刊
Frontiers in Life Science
Frontiers in Life Science MULTIDISCIPLINARY SCIENCES-
CiteScore
5.50
自引率
0.00%
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0
期刊介绍: Frontiers in Life Science publishes high quality and innovative research at the frontier of biology with an emphasis on interdisciplinary research. We particularly encourage manuscripts that lie at the interface of the life sciences and either the more quantitative sciences (including chemistry, physics, mathematics, and informatics) or the social sciences (philosophy, anthropology, sociology and epistemology). We believe that these various disciplines can all contribute to biological research and provide original insights to the most recurrent questions.
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