Development and Characterization of an Ibuprofen-Salicylic Acid Co-crystal with Improved Solubility

IF 2.7 4区医学 Q2 PHARMACOLOGY & PHARMACY Journal of Pharmaceutical Innovation Pub Date : 2025-04-04 DOI:10.1007/s12247-025-09980-9

Sonal Dubey, Dheerathi T, Dilip R. Reddy, Manisha Rajou

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Abstract

Background

Ibuprofen is a widely used non-steroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic properties. However, its clinical efficacy is limited by poor solubility and bioavailability.

Objectives

This study aimed to: Select an appropriate co-former for ibuprofen using computational tools; synthesize and characterize an ibuprofen-salicylic acid co-crystal and evaluate its solubility and dissolution properties.

Methods

Computational tools, including Avogadro, AutoDock Vina, and MGL Tools, were used for molecular docking, employing the Lamarckian genetic algorithm to determine docking scores to search for the selection of a co-former. Salicylic acid showed the best interaction and was selected. Four different methods were used to make ibuprofen-salicylic acid co-crystals. The co-crystal was analyzed using X-ray diffraction (XRD), thermal analysis, and spectroscopic techniques to confirm its structure. The aqueous solubility and dissolution rate of the co-crystal were evaluated and compared with pure ibuprofen.

Results

The ibuprofen-salicylic acid co-crystals synthesized using solvent-assisted co-crystallization technique exhibited a distinct crystalline structure and thermal behavior compared to their individual components. Aqueous solubility was significantly enhanced in comparison to pure ibuprofen.

Conclusion

The ibuprofen-salicylic acid co-crystal demonstrated improved aqueous solubility and dissolution rate, suggesting its potential for enhancing the oral bioavailability of ibuprofen.

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改善溶解度的布洛芬-水杨酸共晶的研制与表征

背景：布洛芬是一种广泛使用的非甾体抗炎药（NSAID），具有镇痛和解热的特性。但其溶解度和生物利用度较差，限制了其临床疗效。目的：利用计算工具选择合适的布洛芬共成体；合成一种布洛芬-水杨酸共晶，并对其溶解度和溶出性能进行了表征。方法采用Avogadro、AutoDock Vina、MGL tools等计算工具进行分子对接，采用拉马克遗传算法确定对接分值，寻找共成物的选择。水杨酸表现出最佳的相互作用，并被选中。采用四种不同的方法制备布洛芬-水杨酸共晶。利用x射线衍射（XRD）、热分析和光谱技术对共晶进行了分析，以确定其结构。评价了该共晶的水溶性和溶出率，并与纯布洛芬进行了比较。结果采用溶剂辅助共晶技术合成的布洛芬-水杨酸共晶具有不同的晶体结构和热行为。与纯布洛芬相比，水溶性明显增强。结论布洛芬-水杨酸共晶提高了布洛芬的水溶性和溶出度，具有提高布洛芬口服生物利用度的潜力。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Journal of Pharmaceutical Innovation PHARMACOLOGY & PHARMACY-

CiteScore

3.70

自引率

3.80%

发文量

审稿时长

>12 weeks

期刊介绍： The Journal of Pharmaceutical Innovation (JPI), is an international, multidisciplinary peer-reviewed scientific journal dedicated to publishing high quality papers emphasizing innovative research and applied technologies within the pharmaceutical and biotechnology industries. JPI''s goal is to be the premier communication vehicle for the critical body of knowledge that is needed for scientific evolution and technical innovation, from R&D to market. Topics will fall under the following categories: Materials science, Product design, Process design, optimization, automation and control, Facilities; Information management, Regulatory policy and strategy, Supply chain developments , Education and professional development, Journal of Pharmaceutical Innovation publishes four issues a year.