Department of Pharmaceutical Sciences, Federal University of Santa Catarina, Quality Control Laboratory, J/K 207, 88040-900 Florianópolis-SC, Brazil.
Int J Pharm. 2011 Feb 28;405(1-2):90-6. doi: 10.1016/j.ijpharm.2010.11.050. Epub 2010 Dec 4.
The aim of this research was to design and study norfloxacin (NFX) release in floating conditions from compressed hydrophilic matrices of hydroxypropylmethylcellulose (HPMC) or poly(ethylene oxide) (PEO). Module assembling technology for drug delivery system manufacturing was used. Two differently cylindrical base curved matrix/modules, identified as female and male, were assembled in void configuration by friction interlocking their concave bases obtaining a floating release system. Drug release and floatation behavior of this assembly was investigated. Due to the higher surface area exposed to the release medium, faster release was observed for individual modules compared to their assembled configuration, independently on the polymer used and concentration. The release curves analyzed using the Korsmeyer exponential equation and Peppas & Sahlin binomial equation showed that the drug release was controlled both by drug diffusion and polymer relaxation or erosion mechanisms. However, convective transport was predominant with PEO and at low content of polymers. NFX release from PEO polymeric matrix was more erosion dependent than HPMC. The assembled systems were able to float in vitro for up to 240min, indicating that this drug delivery system of norfloxacin could provide gastro-retentive site-specific release for increasing norfloxacin bioavailability.
本研究旨在设计并研究从压缩亲水性羟丙甲纤维素（HPMC）或聚环氧乙烷（PEO）的漂浮条件下的诺氟沙星（NFX）释放。用于药物传递系统制造的模块组装技术被用于研究。两个不同的圆柱形基底部弯曲基质/模块，分别标记为雌性和雄性，通过摩擦将它们的凹基部分别装配在空隙中，形成一个漂浮释放系统。对该组件的药物释放和漂浮行为进行了研究。由于暴露于释放介质的表面积更高，与组装构型相比，单个模块的释放速度更快，而与使用的聚合物和浓度无关。使用 Korsmeyer 指数方程和 Peppas & Sahlin 二项式方程分析的释放曲线表明，药物释放由药物扩散和聚合物松弛或侵蚀机制共同控制。然而，对于 PEO 而言，对流传输是主要的，并且在聚合物的低浓度下也是如此。与 HPMC 相比，PEO 聚合物基质中 NFX 的释放更依赖于侵蚀。组装系统能够在体外漂浮长达 240 分钟，这表明诺氟沙星的这种药物传递系统可以提供胃滞留的特定部位释放，从而提高诺氟沙星的生物利用度。
