Tiwari S, Singh S, Rawat M, Tilak R, Mishra B
Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi - 221005, India.
Curr Drug Deliv. 2009 Jul;6(3):305-16. doi: 10.2174/156720109788680921.
The present study was aimed to prepare and evaluate buccoadhesive films of miconazole nitrate (MCZ). The films based on chitosan were prepared by solvent casting method using L(9) orthogonal array design to release the drug above its minimum inhibitory concentration (MIC) for a prolonged period of time so as to reduce its frequency of administration. As per the experimental design, guar gum, HPMC K15M and HEC were added at three different levels to control the drug release. Films showed smooth, uniform and non-sticky surface with good flexibility and folding endurance. Thickness and weight-variation data showed no significant difference among the batches, indicating that the polymeric blend possessed a good film forming ability and its desired properties could easily be achieved by varying the composition of the casting solution. Films composed of chitosan with guar gum appeared to be tougher; comparatively more bioadhesive in vitro, resided to an appropriate time interval and swelled at a more reasonable rate than those containing HPMC and HEC, suggesting the superiority of guar gum over other polymers. In vitro drug release studies conducted on all batches and microbiological studies done on the statistically optimized formulation demonstrated that the films had ability to sustain the drug concentration above its MIC for 6 hrs, despite the incorporation of a smaller dose (2.5 mg/cm(2) of the film). Films, except CF2 and CF3, followed Fickian diffusion of release mechanism. FT-IR spectra revealed no interactions between the drug and polymers.
本研究旨在制备并评价硝酸咪康唑（MCZ）口腔黏附膜。采用溶剂浇铸法，基于壳聚糖并运用L(9)正交试验设计制备薄膜，以使药物在其最低抑菌浓度（MIC）以上持续释放较长时间，从而减少给药频率。根据实验设计，在三个不同水平添加瓜尔胶、羟丙基甲基纤维素K15M和羟乙基纤维素以控制药物释放。薄膜表面光滑、均匀且不粘腻，具有良好的柔韧性和耐折叠性。厚度和重量差异数据显示各批次之间无显著差异，表明该聚合物共混物具有良好的成膜能力，通过改变浇铸溶液的组成可轻松实现其所需性能。由壳聚糖与瓜尔胶组成的薄膜似乎更坚韧；在体外具有相对更强的生物黏附性，在适当的时间间隔内保持，并比含有羟丙基甲基纤维素和羟乙基纤维素的薄膜以更合理的速率溶胀，这表明瓜尔胶优于其他聚合物。对所有批次进行的体外药物释放研究以及对经统计学优化的制剂进行的微生物学研究表明，尽管薄膜中药物剂量较小（2.5 mg/cm²），但这些薄膜仍能够在6小时内将药物浓度维持在其MIC以上。除CF2和CF3外，薄膜遵循菲克扩散释放机制。傅里叶变换红外光谱显示药物与聚合物之间无相互作用。
