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Spherical Agglomeration of Platy Crystals: Curious Case of Etodolac

机译:板状晶体的球形团聚:Etodolac的奇怪案例

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The present study reports an intriguing case study of agglomeration of platy crystals into spheroids. Etodolac a nonsteroidal anti-inflammatory drug is mainly used for rheumatoid arthritis, with emerging applications in management of prostate cancer and Alzheimer's disease. It is a BCS class II drug with poor flow and compressibility issues. Recrystallization using various solvents resulted in platy crystals. Different polymers like hydroxypropyl cellulose (HPC), hydroxypropyl methyl cellulose (HPMC), and polyvinylpyrrolidone (PVP), and copolymers poly(ethylene glycol) (PEG 400), poly(vinyl alcohol) (PVA), and Poloxamer were explored at various concentrations and in different combinations to provide systematic inputs for the development of spherical agglomerates with optimal sphericity, dissolution, yield, and mechanical properties suitable for direct compression. Effects of different process parameters on agglomeration were studied. Agglomerates obtained were characterized using SEM, DSC, and P-XRD and were evaluated for enhancements in flow, compressibility, and dissolution. All the agglomerates have shown improved flow properties and compressibility. Unlike plain drug, all spherical agglomerates have shown acceptable plastic behavior during compression studies resulting in tablets at low pressures. Agglomerates developed using a unique combination of HPMC, HPC, and PEG has shown 94% drug release in 15 min. The recrystallized spherical agglomerates can be used as readily compressible material for continuous manufacturing.
机译:本研究报告了一个有趣的案例,即板状晶体聚集成球体。 Etodolac是一种非甾体类抗炎药,主要用于类风湿关节炎,在治疗前列腺癌和阿尔茨海默氏病方面正在出现新的应用。它是BCS II类药物,具有不良的流动性和可压缩性问题。使用各种溶剂进行重结晶,得到片状晶体。探索了不同浓度的不同聚合物,例如羟丙基纤维素(HPC),羟丙基甲基纤维素(HPMC)和聚乙烯吡咯烷酮(PVP),以及共聚物聚乙二醇(PEG 400),聚乙烯醇(PVA)和泊洛沙姆并以不同的组合形式提供系统的投入,以开发具有最佳球形度,溶解度,屈服力和适用于直接压缩的机械性能的球形附聚物。研究了不同工艺参数对团聚的影响。使用SEM,DSC和P-XRD对获得的附聚物进行表征,并评估其流动性,可压缩性和溶解性的增强。所有附聚物均显示出改善的流动性和可压缩性。与普通药物不同,在压制研究期间,所有球形附聚物均显示出可接受的塑性行为,从而使片剂处于低压状态。使用HPMC,HPC和PEG的独特组合开发的附聚物在15分钟内显示94%的药物释放。重结晶的球形附聚物可用作连续生产的易压缩材料。

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