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首页> 外文期刊>Current Science: A Fortnightly Journal of Research >Solubility enhancement of hydrophobic drugs using synergistically interacting cyclodextrins and cosolvent
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Solubility enhancement of hydrophobic drugs using synergistically interacting cyclodextrins and cosolvent

机译：使用环糊精和助溶剂协同相互作用提高疏水性药物的溶解度

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摘要

The purpose of the present study was to examine the cosolvency and cyclodextrins (CD) addition as a combined approach on the solubility of the hydrophobic drug, valdecoxib, since solubilization of nonpolar drugs constitutes one of the most important tasks in liquid orals and parenteral formulation design. An attempt has been made to improve the solubility of valdecoxib in water, using PEG-400, poloxamer-188 and 2 CDs (beta-CD and Hp-beta-CD). The aqueous solubility of valdecoxib was 0.01 mg/ml, which was significantly improved by addition of PEG-400, CDs and poloxamer-188. In systems containing varying amounts of PEG-400 and 1, 2, 3 and 6% of beta-CD or Hp-beta-CD in water, theoretical solubility was calculated by adding the solubilities in the individual system. The theoretical solubility values were less compared to the observed solubility values. Hp-beta-CD showed better solubility than beta-CD. Addition of poloxamer-188 to the PEG-400/water systems containing CDs showed significant increase in the solubility of valdecoxib; hence synergism was observed. Solubility enhancement is due to affinity between the drug and interior of the CD host molecules, while the small non-polar hydrocarbon region in the cosolvent can reduce the ability of the aqueous system to squeeze out non-polar solutes. The results show that both cosolvency and CD addition are promising approaches for enhancing the solubility of valdecoxib.
机译：本研究的目的是研究添加疏水性和环糊精（CD）作为疏水性药物valdecoxib溶解度的组合方法，因为非极性药物的增溶构成液体口服和肠胃外制剂设计中最重要的任务之一。已尝试使用PEG-400，泊洛沙姆188和2张CD（β-CD和Hp-β-CD）来提高伐地昔布在水中的溶解度。伐地考昔的水溶解度为0.01 mg / ml，通过添加PEG-400，CD和泊洛沙姆188可以显着提高。在含有变化量的PEG-400和1、2、3和6％的β-CD或Hp-β-CD的系统中，通过添加各个系统的溶解度来计算理论溶解度。与观察到的溶解度值相比，理论溶解度值较小。 Hp-β-CD显示出比β-CD更好的溶解度。向含有CD的PEG-400 /水系统中添加poloxamer-188会显示valdecoxib的溶解度有显着增加。因此观察到协同作用。溶解度的提高归因于药物与CD宿主分子内部之间的亲和力，而助溶剂中小的非极性碳氢化合物区域可能会降低水性体系挤出非极性溶质的能力。结果表明，共溶和CD添加都是提高valdecoxib溶解度的有前途的方法。

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