Senthil Rajan D, Mandal Uttam Kr, Veeran Gowda K, Bose A, Ganesan M, Pal T K
Department of Pharmaceutical Technology, Jadavpur University, Kolkata, Westbengal, India.
Boll Chim Farm. 2004 Oct;143(8):315-8.
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.
本研究的目的是通过将胰岛素递送至小肠上部,研究一种剂型方法监测胰岛素失活和吸收过程的有效性。该剂型是基于将胰岛素与蛋白酶抑制剂和吸收增强剂掺入聚丙烯酸聚合物Eudragit L-100中。通过溶剂蒸发技术制备胰岛素微球。并且,与皮下注射牛胰岛素溶液后产生的相对低血糖(RH)效应相比,还研究了这些微球对白色糖尿病白化大鼠相对低血糖效应的影响。与单独使用胰岛素以及胰岛素和胆盐的制剂相比,含有抑肽酶和胆盐的制剂口服给药产生了显著的(p<0.01)低血糖。然而,每种制剂的作用持续时间、过程和强度都不同。有趣的是,观察到抑肽酶和胆盐共同给药可使血糖水平长期显著降低。通过与蛋白酶抑制剂和胆盐一起包封,相对于皮下注射可溶性胰岛素溶液,血浆葡萄糖水平可降低4.47-36.81%,相对低血糖约为11.7%。