Studies on Improving Solubility in Different Media for Said Formulations with Topical Application

Emin Cadâr, A. Ionescu, R. Sîrbu
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Abstract

The studied compounds are gels with meloxicam, piroxicam and tenoxicam in different solvents. The problem of solubilization of these compounds is generated by their poor solubility in hydrophilic media. Also, when applying local non-steroidal anti-inflammatory drugs (NSAIDs) in the form of ointments, the local concentration of the active substance is much higher than in the untreated tissue. The amount of NSAIDs required to produce a therapeutic effect by topical administration is much lower than in oral administration. Side effects may, however, occur as a local irritation from the time a topical formulation is applied. This paper presents the solubilization tests performed for pharmaceutical compounds of the NSAID class in different hydrophilic media. The test conclusions are useful because their solubility can be increased by using solvents (polar or non-polar) and surfactants. The conclusions of the solubility tests help in choosing solvents in the formulation and technologicalization of semi-solid preparations with topical application.
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局部应用提高该制剂在不同介质中的溶解度的研究
所研究的化合物是在不同溶剂中与美洛昔康、吡罗西康和替诺昔康的凝胶。这些化合物的增溶问题是由于它们在亲水性介质中的溶解度差而产生的。此外,当以软膏的形式局部应用非甾体抗炎药(NSAIDs)时,活性物质的局部浓度远高于未经治疗的组织。局部给药产生治疗效果所需的非甾体抗炎药的剂量远低于口服给药。然而,副作用可能会在局部配方应用后出现局部刺激。本文介绍了非甾体抗炎药类药物化合物在不同亲水性介质中的增溶试验。测试结论是有用的,因为它们的溶解度可以通过使用溶剂(极性或非极性)和表面活性剂来提高。溶解度试验的结论有助于外用半固体制剂的配方和工艺的选择。
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