화학공학소재연구정보센터
학회 한국고분자학회
학술대회 2005년 가을 (10/13 ~ 10/14, 제주 ICC)
권호 30권 2호
발표분야 의료용 고분자 부문위원회
제목 A new drug carrier, DCK for enhancing insulin absorption in the intestine
초록 The development of orally active insulin formulation will ensure great advantages in the treatment of patients with diabetes mellitus over conventional injectable insulin therapy. Since insulin absorption in the intestine is restricted by the natural physiological characteristics of insulin, a small synthetic compound was newly developed as an insulin carrier in this study to enhance oral delivery. We developed an oral drug carrier called DCK which could physically associate with therapeutic proteins by ion-pair interaction without altering the structure of native proteins1. The efficacy of new oral insulin formulation (insulin/DCK) was evaluated. Streptozotocin (STZ)-induced diabetic rats orally received single doses of insulin (42 U/kg) and insulin/DCK formulation (10, 21, 30 and 42 U/kg) under fasting condition. Blood glucose level and insulin concentration in plasma were measured for 6 h post-administration. An oral glucose tolerance test was also carried out just after the administration of oral insulin/DCK formulation. When 21, 30 and 42 U/kg (based on insulin activity) of insulin/DCK formulation were administered, the glucose level in plasma was reduced as much as 33.0 (median, range 30.6-70.2)%, 78.5 (39.4-86.8)% and 75.2 (67.0-87.4)%, respectively, compared to basal glycaemia. In particular, the insulin concentration in plasma was rapidly increased. In the oral glucose tolerance test, the insulin/DCK formulation reduced AUC0-240 of glucose for 4 h by 30.8 (22.3-54.9)%, p<0.01, and stabilized glycaemia up to 4 h. This study finds that the insulin/DCK formulation can be absorbed in the intestine and also shows the systemic biological efficacy of insulin. Therefore, we suggest that this oral formulation could be used as an alternative method to the injectable insulin with enhanced clinical effects.

1. S. Lee, J. Lee, D. Y. Lee, S. K. Kim, Y. Lee, and Y. Byun, Diabetologia, 48, 405 (2005)
저자 이슬기, 변영로
소속 서울대
키워드 Bile acid derivative; enhancer; insulin; oral delivery
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