ABSTRACT

The objective of this study was to formulate hydrophilic matrices for a controlled delivery of Piroxicam using carboxymethyl xanthan gum derivatives (CMX). CMXs with various degrees of substitution (DS = 0.22, 1.70 and 2.85) were synthesized by an etherification reaction, and their characterization was realized by FT-IR spectroscopy, X-ray diffraction, and scanning electron microscopy. Different tablets were prepared using the direct compression method. The powder mixtures were characterized by the determination of their angle of repose, compressibility index and Hausner ratio, whereas weight uniformity, hardness, friability, drug content, and in-vitro drug dissolution were employed to test the tablets under simulated gastric and intestinal conditions. The obtained results indicated that the drug release rate increases with the CMX ratio. The matrices based on CMX2 (DS = 1.7) were found to be the best candidates in controlling the release profile, where the optimal formulation contains 40% of CMX2 (F9). The dissolution data showed that all matrices fit well with Korsmeyer–Peppas model, whereas the release kinetics of F9 followed non-Fickian type release. The highest mean dissolution time value was obtained for F9. Finally, these results revealed that CMXs are suitable excipients for the sustained release dosage forms for as long as 20 h.

摘要

这项研究的目的是使用羧甲基黄原胶衍生物（CMX）配制用于控制吡罗昔康递送的亲水性基质。通过醚化反应合成了各种取代度（DS = 0.22、1.70和2.85）的CMX，并通过FT-IR光谱，X射线衍射和扫描电子显微镜对它们进行了表征。使用直接压片法制备不同的片剂。通过确定其休止角，可压缩指数和豪斯纳比来表征粉末混合物，而在模拟的胃和肠条件下，采用重量均匀性，硬度，脆性，药物含量和体外药物溶出度对片剂进行测试。所得结果表明，药物释放速率随CMX比的增加而增加。发现基于CMX2的基质（DS = 1.7）是控制释放曲线的最佳候选者，其中最佳配方包含40％的CMX2（F9）。溶出度数据表明，所有基质都与Korsmeyer-Peppas模型非常吻合，而F9的释放动力学遵循非Fickian型释放。获得了F9的最高平均溶解时间值。最后，这些结果表明，CMX是适合于长达20小时的缓释剂型的赋形剂。获得了F9的最高平均溶解时间值。最后，这些结果表明，CMX是适合于长达20小时的缓释剂型的赋形剂。获得了F9的最高平均溶解时间值。最后，这些结果表明，CMX是适合于长达20小时的缓释剂型的赋形剂。