Dpto. Farmacia y Tecnología Farmacéutica, Universidad de Sevilla, Sevilla, Spain.
Eur J Pharm Biopharm. 2010 May;75(1):42-7. doi: 10.1016/j.ejpb.2010.01.004. Epub 2010 Jan 18.
This paper studies the Riboflavin release from compressed disc modules of Dome Matrix(R) technology using tapioca starch-ethylmethacrylate (TSEMA) and tapioca hydroxypropylstarch-ethylmethacrylate (THSEMA), graft copolymers produced by two different drying methods. The comparison with the release behaviour of similar HPMC modules was performed. Two different shape modules have been made, identified as female and male modules, in order to obtain their assemblage by interlocking the disc bases. HPMC matrices showed quasi-linear Riboflavin release in case of both female and male modules, with faster drug release than TSEMA modules. In the case of THSEMA modules, a faster release was observed compared to HPMC modules. Furthermore, matrices obtained with TSEMA copolymers remained nearly intact after dissolution process, while matrices containing HPMC experimented a complete dissolution of the modules. Combining these results with the release curve analysis using the Korsmeyer and Peppas exponential equation, HPMC modules controlled the drug release by polymer relaxation or erosion. For TSEMA and THSEMA, the drug release mechanism was controlled mainly by drug diffusion. The pronounced faster releases for the matrices containing THSEMA copolymers compared with the ones with TSEMA were due to a more important erosive support; however, the main structure of the matrix remains coherent. Porosity and tortuosity values and the shape of the modules explained the drug release observed.
本文研究了使用两种不同干燥方法制备的淀粉接枝共聚物——木薯淀粉-甲基丙烯酸乙酯(TSEMA)和木薯羟丙基淀粉-甲基丙烯酸乙酯(THSEMA)压缩盘模块中的核黄素释放情况。并与类似 HPMC 模块的释放行为进行了比较。为了通过互锁盘基获得它们的组合,制作了两种不同形状的模块,分别标识为母模块和公模块。HPMC 基质在母模块和公模块中均表现出准线性核黄素释放,药物释放速度快于 TSEMA 模块。在 THSEMA 模块的情况下,与 HPMC 模块相比,观察到更快的释放。此外,与含有 HPMC 的基质相比,含有 TSEMA 共聚物的基质在溶解过程后几乎保持完整,而含有 HPMC 的基质则经历了模块的完全溶解。将这些结果与使用 Korsmeyer 和 Peppas 指数方程的释放曲线分析结合起来,可以发现 HPMC 基质通过聚合物松弛或侵蚀来控制药物释放。对于 TSEMA 和 THSEMA,药物释放机制主要受药物扩散控制。与含有 TSEMA 的基质相比,含有 THSEMA 共聚物的基质释放速度更快,这是由于侵蚀性支撑更为重要;然而,基质的主要结构仍然保持连贯。孔隙率和曲折度值以及模块的形状解释了观察到的药物释放。