Post Graduation Program in Pharmaceutical Sciences, Universidade Estadual do Centro Oeste (UNICENTRO), 85040-080 Guarapuava, PR, Brazil.
Biomed Res Int. 2013;2013:716736. doi: 10.1155/2013/716736. Epub 2013 Sep 8.
The aim of this research was to develop a new hydrophilic matrix system containing norfloxacin (NFX). Extended-release tablets are usually intended for once-a-day administration with benefits to the patient and lower discontinuation of the therapy. Formulations were developed with hydroxypropylmethylcellulose or poly(ethylene oxide) as hydrophilic polymers, with different molecular weights (MWs) and concentrations (20 and 30%). The tablets were found to be stable (6 months at 40 ± 2°C and 75 ± 5% relative humidity), and the film-coating process is recommended to avoid NFX photodegradation. The dissolution profiles demonstrated an extended-release of NFX for all developed formulations. Dissolution curves analyzed using the Korsmeyer exponential equation showed that drug release was controlled by both drug diffusion and polymer relaxation or erosion mechanisms. A more erosion controlled system was obtained for the formulations containing lower MW and amount of polymer. With the increase in both MW and amount of polymer in the formulation, the gel layer became stronger, and the dissolution was more drug-diffusion dependent. Formulations containing intermediate MW polymers or high concentration (30%) of low MW polymers demonstrated a combination of extended and complete in vitro drug release. This way, these formulations could provide an increased bioavailability in vivo.
本研究旨在开发一种含有诺氟沙星(NFX)的新型亲水性基质系统。缓控释片剂通常旨在每天给药一次,对患者有好处,并且降低治疗中断的可能性。采用羟丙基甲基纤维素或聚环氧乙烷(PEO)作为亲水聚合物,具有不同的分子量(MW)和浓度(20%和 30%)来开发制剂。结果表明,片剂在 40°C±2°C 和 75%±5%相对湿度下稳定(6 个月),建议采用薄膜包衣工艺以避免 NFX 光降解。溶出曲线分析表明,所有开发的制剂均表现出 NFX 的缓释效果。用 Korsmeyer 指数方程分析的溶出曲线表明,药物释放由药物扩散和聚合物溶蚀或松弛机制共同控制。对于含有低 MW 和低聚合物用量的制剂,得到了更受溶蚀控制的体系。随着制剂中 MW 和聚合物用量的增加,凝胶层变得更强,溶出更依赖于药物扩散。含有中等 MW 聚合物或高浓度(30%)低 MW 聚合物的制剂表现出延长和完全的体外药物释放相结合。通过这种方式,这些制剂可以在体内提供更高的生物利用度。