含乙酰氯芬酸基质型缓释片的设计、体外评价及释药速度动力学

S. Basak, J. Karthikeyan, B. Bhusan
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引用次数: 9

摘要

以羟丙基甲基纤维素聚合物为缓释片配制肠溶包衣乙酰氯芬酸基质片,并考察其缓释片的缓释行为。采用羟丙基甲基纤维素的不同药物聚合物配比,研制了含200 mg乙酰氯芬酸缓释片。采用湿造粒法制备片剂。以可接受的片剂性能和体外释放度为指标,对处方进行优化。所制片剂硬度最佳,片剂厚度均匀,重量均匀,易碎性低。乙酰氯芬酸片剂释放时间从配制批次的16 h延长至24 h。溶出度研究结果表明,最成功的处方F-V(药物与聚合物的比例为1:0.470)的释药模式与理论释药曲线非常接近。将动力学方程模型应用于F-V批次,结果表明其符合Higuchi模型,线性关系良好,相关系数(R)为0.9911。因此,F-V片以扩散为主释放。加速稳定性研究表明,保质期为40个月(批次F-V),具有良好的药物储存效果。
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Design, In Vitro Evaluation and Release Rate Kinetics of Matrix Type Sustained Release Tablet Containing Aceclofenac
Enteric coated aceclofenac matrix tablets were formulated as sustained release tablets employing hydroxypropyl methylcellulose polymer and the sustained release behavior of the fabricated tablets were investigated. Sustained release matrix tablets containing 200 mg aceclofenac were developed using different drug polymer ratios of hydroxypropyl methylcellulose. Tablets were prepared by wet granulation technique. Formulation was optimized on the basis of acceptable tablet properties and in vitro drug release. The resulting formulations produced monolithic tablets with optimum hardness, uniform thickness, consistent weight uniformity and low friability. Aceclofenac release from tablets was extended from 16 to 24 h from formulated batches. The results of dissolution studies indicated that formulation F-V (drug to polymer 1:0.470), the most successful of the study, exhibited drug release pattern very close to theoretical release profile. Applying kinetic equation models to F-V batch it was found to be followed Higuchi model, as the plots showed high linearity, with correlation coefficient (R) value 0.9911.Therefore, the formulation F-V tablets showed diffusion dominated drug release. The accelerated stability study showed that the shelf life 40 months (batch F-V) and promising drug storage results.
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