Tregopil胰岛素与2型糖尿病患者餐前给药时间，进餐间隔和进餐成分之间的药代动力学和药效动力学。,Clinical Pharmacology in Drug Development

当前位置： X-MOL 学术 › Clin. Pharmacol. Drug Dev. › 论文详情

Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)

Tregopil胰岛素与2型糖尿病患者餐前给药时间，进餐间隔和进餐成分之间的药代动力学和药效动力学。
Clinical Pharmacology in Drug Development ( IF 1.5 ) Pub Date : 2019-08-07 , DOI: 10.1002/cpdd.730
Anand Khedkar ₁ , Harold Lebovitz ₂ , Alexander Fleming ₃ , Alan Cherrington ₄ , Vinu Jose ₁ , Sandeep N Athalye ₅ , Ashwini Vishweswaramurthy ₅

Affiliation

在由3个连续队列组成的随机，安慰剂对照，交叉研究中，我们评估了2型糖尿病患者口服tregopil胰岛素与餐前给药时间，餐间隔和进餐成分类型相关的药代动力学和药效学。在第1组中，与30分钟组相比，在饭前10至20分钟服用tregopil胰岛素可获得最佳的餐后暴露，并显示出更好的餐后降糖效果（浓度-时间曲线[AUC]下的葡萄糖面积）。在队列2中，胰岛素tregopil的药代动力学暴露（血浆AUC）在进餐间隔的4、5和6小时内逐渐增加。与4小时和5小时的间隔相比，6小时的进餐间隔可以更好地吸收tregopil。然而，_0-180分钟在tregopil胰岛素治疗的4小时组中，下午进餐与早上进餐相比。在第3组中，高纤维餐对tregopil胰岛素的吸收影响最小，导致下午血浆葡萄糖水平降低最多。高脂饮食可减少下午服用tregopil的胰岛素。然而，药效学反应并未显着降低。tregopil胰岛素具有大约10分钟的快速起效作用，并且在饭前10至20分钟给药时，与基线相比，血糖水平降低了13％至18％。每次5小时的进餐间隔可最大程度地减少餐食对随后（下午）的tregopil胰岛素吸收的影响，并且餐食的成分不会改变tregopil的药效学反应。

"点击查看英文标题和摘要"

Pharmacokinetics and Pharmacodynamics of Insulin Tregopil in Relation to Premeal Dosing Time, Between Meal Interval, and Meal Composition in Patients With Type 2 Diabetes Mellitus.

We evaluated the pharmacokinetics and pharmacodynamics of oral insulin tregopil in relation to premeal dosing time, between‐meal interval, and meal composition type in type 2 diabetes mellitus patients in a randomized, placebo‐controlled, crossover study consisting of 3 sequential cohorts. In Cohort 1, insulin tregopil administered 10 to 20 minutes before a meal resulted in optimal postmeal exposure and demonstrated better postprandial glucose‐lowering effect (glucose area under concentration‐time curve [AUC]) compared to the 30‐minute group. In Cohort 2, insulin tregopil pharmacokinetic exposure (plasma AUC) showed a progressive increase through 4, 5, and 6 hours of between‐meal interval. The 6‐hour between‐meal interval resulted in better absorption of insulin tregopil in comparison to 4‐ and 5‐hour intervals. However, no significant differences were observed in pharmacodynamic parameters except for higher glucose AUC_0‐180min in the insulin tregopil 4‐hour group during the afternoon meal as compared to the morning meal. In Cohort 3, a high‐fiber meal had the least impact on insulin tregopil absorption and resulted in the highest reduction in plasma glucose levels in the afternoon. A high‐fat meal reduced insulin tregopil absorption in the afternoon meal; however, pharmacodynamic response was not diminished significantly. Insulin tregopil has a rapid onset of action of approximately 10 minutes and, when administered 10 to 20 minutes before a meal, demonstrated up to 13% to 18% reduction in blood glucose levels compared to baseline. A 5‐hour between‐meal interval minimizes the impact of a meal on absorption of subsequent (afternoon) insulin tregopil dose, and the pharmacodynamic response of insulin tregopil is not altered by meal composition. Insulin tregopil was well tolerated in patients with type 2 diabetes mellitus.

更新日期：2019-08-07

点击分享查看原文

点击收藏

公开下载

阅读更多本刊新发论文本刊介绍/投稿指南