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美洛昔康与匹配的亲水性聚合物和环糊精组成的三元体系,用于提高液体制剂的稳定性。

A ternary system of meloxicam with matching hydrophilic polymer and cyclodextrin for improved stability in liquid preprations.

作者信息

Li Si, Kou Longfa, Qin Yimeng, Wang Yimeng, Sun Yinghua, He Zhonggui, Liu Xiaohong

机构信息

School of Pharmacy, Shenyang Pharmaceutical University 103 Wenhua Road Shenyang 110016 China.

Department of Pharmacy, The Second Affiliated Hospital and Yuying Children's Hospital of Wenzhou Medical University Wenzhou 325035 China.

出版信息

RSC Adv. 2024 Jul 5;14(30):21260-21268. doi: 10.1039/d4ra02811b.

Abstract

The purpose of the study is to investigate the effect of ternary systems consisting of meloxicam with cyclodextrins (HP-β-CD or SBE-β-CD) and different polymers (HA, HPMC and PVP) on the stability of meloxicam. The values of meloxicam were determined within all the aforementioned systems and the influence of various polymers on the alteration in meloxicam's stability was evaluated. All three polymers altered the stability of meloxicam to varying degrees, with the extent of the effect being related to hydrophilicity, concentration of components, and the interaction of the newly formed ternary system. Among them, meloxicam demonstrated its highest degree of stabilization within the ternary system formed by SBE-β-CD&HPMC and HP-β-CD&HA. We characterized the ternary system of meloxicam using differential scanning calorimetry (DSC), X-ray diffraction, and scanning electron microscopy analysis, which determined the presence of ternary system inclusions. In addition, we investigated the optimized prescription of eye drops of meloxicam using the ternary system and further determined that the ternary system improved the stability of the drug in liquid formulations.

摘要

本研究的目的是调查由美洛昔康与环糊精(羟丙基-β-环糊精或磺丁基醚-β-环糊精)以及不同聚合物(透明质酸、羟丙基甲基纤维素和聚乙烯吡咯烷酮)组成的三元体系对美洛昔康稳定性的影响。在所有上述体系中测定了美洛昔康的 值,并评估了各种聚合物对美洛昔康稳定性变化的影响。所有三种聚合物均不同程度地改变了美洛昔康的稳定性,其影响程度与亲水性、组分浓度以及新形成的三元体系的相互作用有关。其中,美洛昔康在由磺丁基醚-β-环糊精&羟丙基甲基纤维素和羟丙基-β-环糊精&透明质酸形成的三元体系中表现出最高程度的稳定化。我们使用差示扫描量热法(DSC)、X射线衍射和扫描电子显微镜分析对美洛昔康的三元体系进行了表征,确定了三元体系包合物的存在。此外,我们使用该三元体系研究了美洛昔康滴眼液的优化处方,并进一步确定该三元体系提高了药物在液体制剂中的稳定性。

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