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首页> 美国卫生研究院文献>AAPS PharmSciTech >Study of isopropyl myristate microemulsion systems containing cyclodextrins to improve the solubility of 2 model hydrophobic drugs
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Study of isopropyl myristate microemulsion systems containing cyclodextrins to improve the solubility of 2 model hydrophobic drugs

机译：含环糊精的肉豆蔻酸异丙酯微乳液体系研究以提高2种模型疏水性药物的溶解度

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摘要

The objectives of this project were to evaluate the effect of alkanols and cyclodextrins on the phase behavior of an isopropyl myristate microemulsion system and to examine the solubility of model drugs. Triangular phase diagrams were developed for the microemulsion systems using the water titration method, and the solubility values of progesterone and indomethacin were determined using a conventional shake-flask method. The water assimilation capacities were determined to evaluate the effective microemulsion formation in different systems. The alkanols showed higher microemulsion formation rates at higher concentrations. A correlation between the carbon numbers of the alkanol and water assimilation capacity in the microemulsions studied was observed; isobutanol and isopentanol produced the best results. The addition of cyclodextrins showed no effect or had a negative effect on the microemulsion formation based on the type of cyclodextrin used. Isopropyl myristate-based microemulsion systems alone could increase the solubility values of progesterone and indomethacin up to 3300-fold and 500-fold, respectively, compared to those in water. However, the addition of cyclodextrins to the microemulsion systems did not show a synergistic effect in increasing the solubility values of the model drugs. In conclusion, microemulsion systems improve the solubility of progesterone and indomethacin. But the two types of cyclodextrins studied affected isopropyl myristatebased microemulsion systems negatively and did not improve the solubilization of 2 model drugs.
机译：该项目的目的是评估链烷醇和环糊精对肉豆蔻酸异丙酯微乳液体系相行为的影响，并检验模型药物的溶解度。使用水滴定法建立了微乳液系统的三角相图，并使用常规摇瓶法测定了孕酮和消炎痛的溶解度值。测定水的同化能力以评估不同系统中有效的微乳液形成。链烷醇在较高浓度下显示出较高的微乳液形成速率。观察到的微乳液中链烷醇的碳原子数与水同化能力之间存在相关性；异丁醇和异戊醇的效果最佳。基于所使用的环糊精的类型，环糊精的添加对微乳液形成没有影响或具有负面影响。与在水中的那些相比，仅基于肉豆蔻酸异丙酯的微乳液系统可以将黄体酮和消炎痛的溶解度值分别提高至3300倍和500倍。但是，将环糊精添加到微乳液体系中并没有显示出增加模型药物溶解度值的协同作用。总之，微乳体系可改善孕酮和消炎痛的溶解度。但是，研究的两种类型的环糊精对肉豆蔻酸异丙酯基微乳剂体系产生了负面影响，并没有改善两种模型药物的增溶作用。

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