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Formulation Study and Evaluation of Matrix and Three-layer Tablet Sustained Drug Delivery Systems Based on Carbopols with Isosorbite Mononitrate

机译:卡波姆与单硝酸异山梨酯的基质和三层片剂持续药物递送系统的配方研究与评价

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摘要

The purpose of this research was to develop and evaluate different preparations of sustained delivery systems, using Carbopols as carriers, in the form of matrices and three-layer tablets with isosorbite mononitrate. Matrix tablets were prepared by direct compression whereas three-layer tablets were prepared by compressing polymer barrier layers on both sides of the core containing the drug. The findings of the study indicated that all systems demonstrated sustained release. The properties of the polymer used and the structure of each formulation appear to considerably affect drug release and its release rate. The three-layer formulations exhibit lower drug release compared to the matrices. This was due to the fact that the barrier-layers hindered the penetration of liquid into the core and modified drug dissolution and release. The geometrical characteristics/structure of the tablets as well as the weight/thickness of the barriers-layers considerably influence the rate of drug release and the release mechanisms. Kinetic analysis of the data indicated that drug release from matrices was mainly attributed to Fickian diffusion while three-layer tablets exhibited either anomalous diffusion or erosion/relaxation mechanisms. The advantage of Carbopol formulations is that a range of release profiles can easily be obtained through variations in tablet structure and thus Carbopols are appropriate carriers of oral sustained drug delivery systems for soluble drugs such as the isosorbite mononitrate.
机译:这项研究的目的是开发和评估以Carbopols为载体,以基质和单硝酸异山梨酯的三层片剂形式的持续递送系统的不同制剂。通过直接压制制备基质片剂,而通过压制包含药物的药芯两侧的聚合物阻隔层制备三层片剂。研究结果表明,所有系统均显示出持续释放。所用聚合物的性质和每种制剂的结构似乎大大影响了药物的释放及其释放速率。与基质相比,三层制剂显示出较低的药物释放。这是由于以下事实:阻隔层阻碍了液体渗透到核心中,并阻碍了药物的溶解和释放。片剂的几何特征/结构以及屏障层的重量/厚度极大地影响药物释放速率和释放机理。数据的动力学分析表明,从基质释放的药物主要归因于菲克扩散,而三层片剂则表现出反常扩散或侵蚀/松弛机制。 Carbopol制剂的优点是可以通过改变片剂结构轻松获得一定范围的释放曲线,因此Carbopols是口服持续药物递送系统的载体,适用于可溶性药物(如一硝酸异山梨酯)。

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