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首页> 外文期刊>Pharmaceutical development and technology >Effects of lipid formulations on clove extract spray dried powders: comparison of physicochemical properties, storage stability and in vitro intestinal permeation
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Effects of lipid formulations on clove extract spray dried powders: comparison of physicochemical properties, storage stability and in vitro intestinal permeation

机译:脂质制剂对丁香提取物喷雾干燥粉末的影响:物理化学性质,储存稳定性和体外肠渗透的比较

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摘要

Clove is an aromatic plant spice with potent antioxidant and anti-inflammatory activity. Eugenol is the main compound which contributes to such medicinal and nutritional benefits. To date, the formulation of unstable, volatile and poorly water-soluble compounds remains a challenging task. Lipid formulations can be used to improve physicochemical and biopharmaceutical properties of poorly soluble compounds. The aim of this study is to investigate the effects of lipids, such as Gelucire and Compritol on physicochemical properties; stability and in vitro intestinal permeation of spray dried powdered formulations loaded with clove's bioactive compounds. Results showed that eugenol retention in spray-dried powders could be correlated with antioxidant activity and with mass recovery after spray drying. Adding Gelucire but not Compritol to clove extract formulations, improved solubility of spray dried powders. Stability test in high humidity environment (63.5% RH) suggested that formulations including both Gelucire and Compritol were significantly more stable compared to the formulation without any lipid at the two tested temperatures (25 degrees C and 40 degrees C). This suggests that lipid additions to clove (Syzygium aromaticum) extract formulations provide protective effects for the spray dried powders in high-humidity environments. In addition, results from in vitro intestinal permeation studies suggested that eugenol uptake, was not being hindered by transporters nor was the absorption being affected by lipid formulations.
机译:丁香是一种具有有效的抗氧化剂和抗炎活性的芳香植物香料。丁二酚是有助于这种药用和营养益处的主要化合物。迄今为止,不稳定,挥发性和水溶性差的化合物的配方仍然是一个具有挑战性的任务。脂质制剂可用于改善可溶性化合物的物理化学和生物制药特性。本研究的目的是探讨脂质的影响,例如Gelucire和包含在物理化学性质上的影响;喷雾干燥粉末配方的稳定性和体外肠道渗透,载有丁香的生物活性化合物。结果表明,喷雾干燥粉末中的丁醇保持与抗氧化活性和喷雾干燥后的质量恢复相关。添加gelucire但不包含丁香提取物配方,改善喷雾干燥粉末的溶解度。高湿度环境中的稳定性试验(63.5%RH)表明,与在两个测试温度(25℃和40℃)上没有任何脂质的制剂相比,包括Gelucire和杂种醇的配方明显更稳定。这表明对丁香(Syzygium aromaticum)提取制剂的脂质添加提供了高湿度环境中的喷雾干燥粉末的保护作用。此外,体外肠道渗透研究的结果表明,丁烯醇摄取不会受到转运蛋白的阻碍,也不是受脂质制剂的影响。

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