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基于羟丙基-β-环糊精/美洛昔康包合物构建热敏凝胶以提高美洛昔康溶解度并延长药物在角膜中的滞留时间。

Construction of a thermosensitive gel based on hydroxypropyl-β-cyclodextrin/meloxicam inclusion complexes for improving meloxicam solubility and prolonging drug retention time in the cornea.

作者信息

Yang Lvyao, Li Xiu'e, Zhang Yuanke, Tian Jingjing, Ling Guixia, Zhang Peng

机构信息

Wuya College of Innovation, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang, 110016, China.

CSPC Pharmaceutical Group Zhongqi Pharmacy (Shijiazhuang) Co., Ltd., Shiiazhuang, China.

出版信息

Drug Deliv Transl Res. 2025 Jan 23. doi: 10.1007/s13346-025-01797-w.

DOI:10.1007/s13346-025-01797-w
PMID:39849286
Abstract

The eyes are easily stimulated by external factors, which can cause inflammation. Anti-inflammatory drugs are usually used to inhibit the production of inflammatory factors. Many nonsteroidal anti-inflammatory drugs have been used for the eye, but due to the poor solubility of meloxicam, there are currently no marketed meloxicam preparations for the treatment of eye diseases. This article uses hydroxypropyl-β-CD (HP-β-CD) to encapsulate meloxicam and combined with thermosensitive gel to prepare an HP-β-CD/meloxicam inclusion complex eye thermosensitive gel, which can improved the water solubility of meloxicam and extend the retention time of the drug in the cornea, and achieve the goal of slow release through continuous dissolution. It not only has the advantages of convenient administration and accurate dosage of eye drops, but also overcomes the disadvantage of easy loss of eye drops, showing the advantages of long retention time and fewer administration times, and provides a basis for the development of other dosage forms of meloxicam.

摘要

眼睛容易受到外部因素刺激,进而引发炎症。通常使用抗炎药物来抑制炎症因子的产生。许多非甾体抗炎药物已用于眼部,但由于美洛昔康溶解度较差,目前尚无用于治疗眼部疾病的美洛昔康上市制剂。本文采用羟丙基-β-环糊精(HP-β-CD)包封美洛昔康,并与热敏凝胶相结合制备HP-β-CD/美洛昔康包合物眼用热敏凝胶,可提高美洛昔康的水溶性,延长药物在角膜中的滞留时间,并通过持续溶解实现缓释目的。它不仅具有滴眼液给药方便、剂量准确的优点,还克服了滴眼液易流失的缺点,展现出滞留时间长、给药次数少的优势,为美洛昔康其他剂型的开发提供了依据。

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Studying the Complex Formation of Sulfonatocalix[4]naphthalene and Meloxicam towards Enhancing Its Solubility and Dissolution Performance.
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