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Celecoxib Crystallized from Hydrophilic Polymeric Solutions Showed Modified Crystalline Behavior with an Improved Dissolution Profile
ASSAY and Drug Development Technologies ( IF 1.8 ) Pub Date : 2021-06-02 , DOI: 10.1089/adt.2020.1058
Rudra Narayan Sahoo 1, 2 , Bhabani Sankar Satapathy 1 , Jayashree Ray 1 , Rasmita Dash 1 , Subrata Mallick 1
Affiliation  

The crystallization technique has been established as a cost-effective and simple approach to improve the dissolution rate and oral bioavailability of poorly soluble drugs. This study was carried out to study the effect of some selected hydrophilic polymers such as methyl cellulose, hydroxypropyl methylcellulose (HPMC), polyvinyl alcohol, and carboxymethyl cellulose on the crystal behavior and dissolution properties of celecoxib (CLX), a common nonsteroidal anti-inflammatory drug. Structural and spectral characteristics of crystallized CLX have been studied by Fourier transform infrared (FTIR) spectroscopy, diffraction scanning calorimetry (DSC), and X-ray diffraction (XRD) analysis. From FTIR and DSC analysis, no significant shifting of peaks or appearance of any new peaks (for polymers) were observed, which indicated the absence of any major interaction between drug and polymers as well as the absence of polymers in the final crystallized product of CLX. The XRD analysis showed a change in crystalline morphology to some extent. The dissolution rate of crystallized CLX in the presence of polymers (particularly with HPMC) was significantly improved compared with plain CLX. The improved dissolution profile of the experimental CLX crystal products could be an indication of improved bioavailability of CLX for better clinical outcome.

中文翻译:

从亲水性聚合物溶液中结晶的塞来昔布表现出改进的结晶行为和改进的溶出度曲线

结晶技术已被确立为一种具有成本效益且简单的方法,可提高难溶性药物的溶出度和口服生物利用度。本研究旨在研究某些选定的亲水性聚合物,如甲基纤维素、羟丙基甲基纤维素 (HPMC)、聚乙烯醇和羧甲基纤维素对塞来昔布 (CLX)(一种常见的非甾体抗炎药)晶体行为和溶出特性的影响。药品。已通过傅里叶变换红外 (FTIR) 光谱、衍射扫描量热法 (DSC) 和 X 射线衍射 (XRD) 分析研究了结晶 CLX 的结构和光谱特性。从 FTIR 和 DSC 分析中,没有观察到明显的峰移动或任何新峰的出现(对于聚合物),这表明药物和聚合物之间不存在任何主要的相互作用,并且在 CLX 的最终结晶产物中不存在聚合物。XRD分析显示结晶形态有一定程度的变化。与普通 CLX 相比,在聚合物(尤其是 HPMC)存在下结晶 CLX 的溶解速率显着提高。实验性 CLX 晶体产品改善的溶出曲线可能表明 CLX 的生物利用度得到改善,从而获得更好的临床结果。与普通 CLX 相比,在聚合物(尤其是 HPMC)存在下结晶 CLX 的溶解速率显着提高。实验性 CLX 晶体产品改善的溶出曲线可能表明 CLX 的生物利用度得到改善,从而获得更好的临床结果。与普通 CLX 相比,在聚合物(尤其是 HPMC)存在下结晶 CLX 的溶解速率显着提高。实验性 CLX 晶体产品改善的溶出曲线可能表明 CLX 的生物利用度得到改善,从而获得更好的临床结果。
更新日期:2021-06-04
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