Effect of Hydrophilic Polymers on Solubility Properties of Ketoprofen - 2,5-Dihydroxybenzoic Acid Multicomponent Solids

Q3 Chemistry Molekul Pub Date : 2023-11-20 DOI:10.20884/1.jm.2023.18.3.7292

Yudi Wicaksono, Budipratiwi Wisudyaningsih, Karina Priyadi Devi Wahyu Priyadi, Aisyah Prida Laily, Salsabila Bara Putri

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Abstract

Ketoprofen is a medicinal compound derivative of phenyl alkanoic acid that works as an anti-inflammatory, antipyretic, and analgesic. In the Biopharmaceutical Classification Systems, ketoprofen is a class II drug with high permeability but low solubility. Due to its low solubility, the absorption and bioavailability of ketoprofen are very limited, which can affect its therapeutic effectiveness. This study aimed to increase ketoprofen's solubility by forming multicomponent solids using 2,5-dihydroxybenzoic acid coformer with adding hydrophilic polymers ((hydroxypropyl)methylcellulose, polyvinylpyrrolidone K90, and polyethylene glycol 4000). The results showed that ketoprofen with 2,5-dihydroxybenzoic acid coformer prepared using the solvent evaporation method formed a eutectic mixture. Adding hydrophilic polymers to the ketoprofen - 2,5-dihydroxybenzoic acid multicomponent solid increased the crystallinity and decreased the melting point of the multicomponent solids. The multicomponent solids of ketoprofen - 2,5-dihydroxybenzoic acid with the addition of hydrophilic polymers had solubility and dissolution efficiency significantly higher (p<0.05) than the ketoprofen - 2,5-dihydroxybenzoic acid multicomponent solids without hydrophilic polymers.

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亲水性聚合物对酮洛芬-2,5-二羟基苯甲酸多组分固体溶解特性的影响

酮洛芬是一种苯烷酸衍生物，具有消炎、解热和镇痛作用。在生物制药分类系统中，酮洛芬属于第二类药物，具有高渗透性和低溶解性。由于溶解度低，酮洛芬的吸收和生物利用度非常有限，从而会影响其治疗效果。本研究旨在利用 2,5-二羟基苯甲酸共聚物与亲水性聚合物（（羟丙基）甲基纤维素、聚乙烯吡咯烷酮 K90 和聚乙二醇 4000）形成多组分固体，从而提高酮洛芬的溶解度。结果表明，用溶剂蒸发法制备的酮洛芬与 2,5-二羟基苯甲酸共聚物形成共晶混合物。在酮洛芬-2,5-二羟基苯甲酸多组分固体中加入亲水性聚合物，可提高多组分固体的结晶度，降低熔点。添加了亲水聚合物的酮洛芬-2,5-二羟基苯甲酸多组分固体的溶解度和溶解效率明显高于未添加亲水聚合物的酮洛芬-2,5-二羟基苯甲酸多组分固体（p<0.05）。

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