Dipartimento di Scienze Farmaceutiche e Biomediche, Università degli Studi di Salerno, Fisciano, Italy.
Pharm Dev Technol. 2013 Nov-Dec;18(6):1399-406. doi: 10.3109/10837450.2012.727005. Epub 2012 Oct 15.
The objective of this work is to prepare oral dosage systems based on enteric materials in order to verify their possible use as Colon-Specific Drug Delivery Systems (CSDDSs).
In particular, three different copolymers of methyl-methacrylate (MMA) - acrylic acid (AA) are synthesized with increasing percentage of MMA (from 70% to 73%) and they are used to produce microparticles by the double-emulsion solvent evaporation method. The microparticles, loaded using theophylline as model drug, are then tested for drug release under varying pH to reproduce what happens in the human GI tract.
All the investigated systems have shown an effective pH sensitiveness: they show a good gastro-resistance, releasing the model drug only at higher pH, small intestine or colon, depending on the kind of used copolymer.
The results confirm the usefulness of both the materials and the methods proposed in this study for colon-specific delivery applications.
本工作旨在制备基于肠溶材料的口服剂型系统，以验证其作为结肠定位给药系统（CSDDS）的可能性。
特别地，用甲基丙烯酸甲酯（MMA）-丙烯酸（AA）合成了三种不同比例的共聚物（从 70%增加到 73%），并采用双乳液溶剂蒸发法制备微球。然后，使用茶碱作为模型药物对微球进行载药，并在不同 pH 下进行药物释放测试，以模拟人体胃肠道中的情况。
所有研究的系统都表现出有效的 pH 敏感性：它们具有良好的胃耐受性，仅在较高 pH 值（小肠或结肠）下释放模型药物，具体取决于所用共聚物的类型。
研究结果证实了本研究中提出的材料和方法在结肠定位给药应用中的有效性。
