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用于糖尿病治疗的控释胃肠道传递的胰岛素的扩散系数受基质组成、球体大小和激素浓度的影响。

Effect of matrix composition, sphere size and hormone concentration on diffusion coefficient of insulin for controlled gastrointestinal delivery for diabetes treatment.

机构信息

a Chemical Engineering Department , Federal University of Paraná , Curitiba , Brazil.

出版信息

J Microencapsul. 2018 Jan;35(1):13-25. doi: 10.1080/02652048.2017.1409820. Epub 2017 Dec 12.

Abstract

Oral insulin administration is limited due to its degradation by proteases. The hormone was encapsulated in spheres made of either pure calcium alginate (ALG) or its association with whey protein isolate (WPI-ALG) in order to minimise loss in the stomach region while allowing liberation in the maximum absorption area, located in the intestine. Diffusion coefficients for both matrix compositions were determined in vitro for gastric pH (5.88 and 10.26 × 10 m s) and intestinal pH (21.11 and 79.29 × 10 m s). Higher initial insulin concentrations and lower diameters accelerated its release, confirming Fickian behaviour. The analytic model exhibited a good fit in most cases. Computer simulations revealed that ALG spheres are more convenient for oral administration because they release more insulin in the intestine than the WPI-ALG ones, thus supporting its therapeutic viability for the purpose of reducing stress in those who depend on insulin.

摘要

口服胰岛素由于被蛋白酶降解而受到限制。该激素被包裹在由纯海藻酸钠(ALG)或其与乳清蛋白分离物(WPI-ALG)组成的球体中,以最大限度地减少在胃区域的损失,同时允许在最大吸收区域(位于肠道)中释放。在体外测定了两种基质成分在胃 pH 值(5.88 和 10.26×10 m s)和肠 pH 值(21.11 和 79.29×10 m s)下的扩散系数。较高的初始胰岛素浓度和较低的粒径加速了其释放,证实了菲克行为。分析模型在大多数情况下都具有良好的拟合度。计算机模拟表明,ALG 球体更适合口服给药,因为它们在肠道中释放的胰岛素比 WPI-ALG 球体更多,因此支持其用于减少依赖胰岛素的人的应激的治疗可行性。

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