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多分散微囊化球形颗粒药物释放的建模

Modelling of drug-release from poly-disperse microencapsulated spherical particles.

作者信息

Sirotti C, Colombo I, Grassi M

机构信息

EURAND International, Via del Follatoio 12, I-34148, Trieste, Italy.

出版信息

J Microencapsul. 2002 Sep-Oct;19(5):603-14. doi: 10.1080/02652040210141075.

Abstract

The topic of this paper is the experimental and theoretical study of drug-release from a system of polydisperse microencapsulated particles that, for the sake of simplicity, are assumed to be spherical. The theoretical analysis performed yields of a mathematical model to describe the physical phenomena involved in drug-release from such a system. In particular, the model is based on the hypothesis of a progressive dissolution of the internal solid drug core (due to solvent penetration through the coating) that gives a liquid solution in the region between the coating and the dissolving solid core. The existence of a concentration gradient between the inner solution and the outer release environment determines drug diffusion through the coating. The coacervation technique was adopted to microencapsulate the solid drug cores (theophylline, a bronchodilator for the treatment of chronic asthma and chronic obstructive lung disease) by an insoluble polymeric layer of ethylcellulose. The amount of drug released from these microencapsulated particles to the external receiver phase is monitored by means of a UV spectrophotometer. As the proposed model fits the experimental results well, it was concluded that it can be a good tool to design and to study this kind of drug-release system.

摘要

本文的主题是对多分散微囊化颗粒系统药物释放进行实验和理论研究,为简便起见,假定这些颗粒为球形。所进行的理论分析得出了一个数学模型,用于描述此类系统药物释放过程中涉及的物理现象。具体而言,该模型基于内部固体药物核心逐渐溶解的假设(由于溶剂透过包衣渗透),这在包衣与正在溶解的固体核心之间的区域形成了一种液体溶液。内部溶液与外部释放环境之间存在的浓度梯度决定了药物透过包衣的扩散。采用凝聚技术,用乙基纤维素不溶性聚合物层对固体药物核心(茶碱,一种用于治疗慢性哮喘和慢性阻塞性肺病的支气管扩张剂)进行微囊化。通过紫外分光光度计监测从这些微囊化颗粒释放到外部接受相的药物量。由于所提出的模型与实验结果拟合良好,得出的结论是,它可以成为设计和研究这类药物释放系统的一个良好工具。

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