Oral delivery system of insulin microspheres: effect on relative hypoglycemia of diabetic albino rats.

Bollettino chimico farmaceutico Pub Date : 2004-10-01
D Senthil Rajan, Uttam Kr Mandal, K Veeran Gowda, A Bose, M Ganesan, T K Pal
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Abstract

The aim of the present work was to investigate the effectiveness of a dosage form approach for monitoring both the inactivation and the absorption process by targeting insulin delivery to the upper region of small intestine. The dosage form is based on the incorporation of insulin with protease inhibitor and absorption enhancer into polyacrylic polymer Eudragit L-100. Insulin microspheres were prepared by solvent evaporation technique. And also study the effect of these microspheres upon the relative hypoglycemia (RH) effect in white diabetic albino rats has been studied in comparison to that produced after subcutaneous injection of bovine insulin solution. The oral administration of formulation with aprotinin and bile salts gave significant (p< 0.01) hypoglycemia when compared with formulation with insulin alone and with insulin and bile salts. However, the duration, course and the intensity of effect were different for each formulation. It was interesting to observe that the co-administration of aprotinin and bile salts produce prolonged and significant reduction of blood glucose level. A reduction of 4.47-36.81% in plasma glucose levels and RH of about 11.7% relative to subcutaneous injection of soluble insulin solution can be achieved by encapsulation along with protease inhibitor and bile salts.

胰岛素微球口服给药系统对糖尿病白化大鼠相对低血糖的影响。
本研究的目的是研究一种剂型方法的有效性,通过靶向胰岛素递送到小肠上部区域来监测失活和吸收过程。该剂型是基于将胰岛素与蛋白酶抑制剂和吸收促进剂掺入聚丙烯酸聚合物Eudragit L-100中。采用溶剂蒸发法制备胰岛素微球。并研究了这些微球对白化糖尿病大鼠的相对低血糖(RH)效果的影响,并与皮下注射牛胰岛素溶液产生的效果进行了比较。口服抑酶蛋白和胆汁盐制剂与单独使用胰岛素和胰岛素加胆汁盐制剂相比,降糖效果显著(p< 0.01)。然而,每种制剂的持续时间、疗程和作用强度不同。有趣的是,抑酶蛋白和胆汁盐的联合用药可使血糖水平持续显著降低。与皮下注射可溶性胰岛素溶液相比,通过与蛋白酶抑制剂和胆汁盐一起包封可使血浆葡萄糖水平降低4.47-36.81%,RH降低约11.7%。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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