用 PVP K30 和 β-Cyclodextrin 增强醋氯芬酸的溶解度和溶解性

Manju Singh, Vijay Kumar
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引用次数: 0

摘要

醋氯芬酸(AC)是一种强效非甾体抗炎药(NSAID),以其消炎、镇痛和解热特性而闻名。其疗效与其他非甾体抗炎药不相上下,起效时间也相似。作为生物制药分类系统(BCS)的二级化合物,AC 的口服生物利用度受到其在胃肠道中溶解速度的限制。提高 AC 的溶出率对于改善其生物利用度和疗效至关重要。本研究旨在以β-环糊精和聚乙烯吡咯烷酮 K30(PVP K30)混合辅料体系为载体,制备和表征 AC 的固体分散体,并考察它们对药物溶出率的影响。通过物理混合法和溶剂蒸发法,使用不同比例的 AC 与赋形剂系统制成了固体分散体。对制剂的实际产量、药物含量、体积密度和堆积密度、豪斯纳比率、卡尔指数、静止角和体外药物释放等参数进行了评估。结果表明,与纯药物相比,固体分散体的药物释放量明显增加,溶剂蒸发法比物理混合法更有效。固体分散技术通过改变药物释放特性带来了许多好处,从而加快了药物在体内的释放速度。研究表明,通过固体分散方法,AC 等溶解性差的药物的溶解度可以得到显著改善。PVP K30 和 β-环糊精等水溶性载体的使用有效地改变了药物的释放曲线。采用溶剂蒸发法制备了 PVP K30 与 AC 的固体分散体,药物与载体的比例为 1:1 至 1:5。对配方的产量、质地、颜色、物理特性和适用性进行了筛选。
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Enhancing Aceclofenac Solubility and Dissolution with PVP K30 and β-Cyclodextrin
Aceclofenac (AC) is a potent non-steroidal anti-inflammatory drug (NSAID) known for its anti-inflammatory, analgesic, and antipyretic properties. Its effectiveness is comparable to other NSAIDs, with a similar onset of action. As a Biopharmaceutical Classification System (BCS) Class II compound, the oral bioavailability of AC is limited by its dissolution rate in the gastrointestinal tract. Enhancing the dissolution rate of AC is crucial for improving its bioavailability and therapeutic efficacy. This study aimed to prepare and characterize solid dispersions of AC using a mixed excipient system of β-cyclodextrin and polyvinylpyrrolidone K30 (PVP K30) as carriers, and to examine their effect on the drug's dissolution rate. Solid dispersions were created via physical mixture and solvent evaporation methods using different ratios of AC to the excipient system. The formulations were evaluated for parameters such as practical yield, drug content, bulk and tapped density, Hausner’s ratio, Carr’s index, angle of repose, and in vitro drug release. The results showed a significant increase in drug release for the solid dispersions compared to the pure drug, with the solvent evaporation method proving more effective than the physical mixture method. Solid dispersion techniques offer numerous benefits by altering drug release characteristics, leading to faster drug release within the body. The study demonstrated that the solubility of poorly soluble drugs like AC can be significantly improved through solid dispersion methods. The use of water-soluble carriers such as PVP K30 and β-cyclodextrin effectively modified the drug release profiles. Solid dispersions of AC with PVP K30 were prepared in drug-to-carrier ratios of 1:1 to 1:5 using the solvent evaporation method, while inclusion complexes with β-cyclodextrin were prepared by the kneading method in similar ratios. The formulations were screened for yield, texture, color, physical characteristics, and suitability.
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