Purpose

The prevalence of rheumatic disease patients was estimated at 25% of the population. Rheumatic diseases are the leading cause of disability. The main objective of the study was to investigate the kinetic drug release characteristics of aceclofenac sustained-release (SR) matrix tablets for the management of rheumatic diseases.

Methods

The novel formulation of aceclofenac was prepared by using hydrophilic polymers such as HPMC K4M with a fixed concentration along with the varying concentration of Carbopol 946 and cationic guar gum in the formulation FA1–FA3 and FB1–FB3 respectively. The powder mixture was compressed by the direct compression method into tablets using a rotary tablet compression machine. Prepared SR matrix tablets were evaluated for uniformity of content, hardness, thickness, weight variation, friability, and in vitro dissolution studies.

Results

The drug content, hardness, thickness, weight variation, and friability of prepared tablets were found to be within the acceptable range. The optimized formulation was subjected to various kinetic release studies such as first-order model, zero-order model, Higuchi model, and Korsmeyer-Peppas model. When the data were plotted according to the Higuchi model, the formulations showed the best linearity, with regression values 0.9248 and diffusion mechanism of the formulation FB1 follows super case II transport mechanism.

Conclusion

The optimized formulation FB1 with the super case II transport mechanism prolonged the drug release, due to the polyionic interaction between the polymers. It could be an ideal formulation for the management of rheumatic diseases.

中文翻译：

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风湿性疾病选择性COX-2抑制剂的动力学药物释放特性研究和缓释基质片剂的体外评价

目的

风湿病患者的患病率估计为人口的25％。风湿性疾病是致残的主要原因。该研究的主要目的是研究风湿性疾病的醋氯芬酸缓释（SR）基质片剂的动态药物释放特性。

方法

通过使用固定浓度的亲水性聚合物（例如HPMC K4M）以及配方FA1-FA3和FB1-FB3中不同浓度的Carbopol 946和阳离子瓜尔胶来制备醋氯芬酸的新配方。使用旋转压片机通过直接压片法将粉末混合物压制成片剂。评价了制备的SR基质片剂的含量，硬度，厚度，重量变化，易碎性和体外溶出度研究的均匀性。

结果

发现制备的片剂的药物含量，硬度，厚度，重量变化和脆性在可接受的范围内。对优化的制剂进行了各种动力学释放研究，例如一阶模型，零阶模型，Higuchi模型和Korsmeyer-Peppas模型。根据Higuchi模型绘制数据时，配方显示出最佳线性，回归值为0.9248，配方FB1的扩散机理遵循超级案例II转运机理。

结论

由于聚合物之间的聚离子相互作用，具有超级案例II转运机制的优化配方FB1延长了药物释放。它可能是治疗风湿性疾病的理想配方。