首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex.
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Synthesis, characterization and in vitro release studies of a new acetazolamide-HP-beta-CD-TEA inclusion complex.

机译:新型乙酰唑胺-HP-β-CD-TEA包合物的合成,表征和体外释放研究。

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The aim of our work was to develop a multicomponent inclusion complex of acetazolamide (ACZ) in order to investigate the combined effect of hydroxypropyl-beta-cyclodextrin (HP-beta-CD) and triethanolamine (TEA) on the solubility of ACZ and its possibility of ophthalmic delivery. Phase solubility study was used to evaluate the complexation in solution at 25 degrees C. Complex formation was also evaluated by comparing the infrared (FT-IR) spectra of the solid complexes with a simple physical mixture containing the same amount of ACZ. FT-IR experiments provided data indicating that the carbonamido group of ACZ is involved in the inclusion process. In vitro release data showed that both formulations, containing the freeze-dried ternary complex and the corresponding simple physical mixture of ACZ with HP-beta-CD and TEA presented the fastest release rate of ACZ. These results suggest that the ACZ-HP-beta-CD-TEA complex represents an effective novel formulation to enhance ACZ solubility in water, turning it promising for ophthalmic administration.
机译:我们的工作目的是开发乙酰唑胺(ACZ)的多组分包合物,以研究羟丙基-β-环糊精(HP-β-CD)和三乙醇胺(TEA)对ACZ溶解度的联合作用及其可能性眼药水。相溶解度研究用于评估25℃下溶液中的络合作用。还通过将固体络合物的红外光谱(FT-IR)与包含相同量ACZ的简单物理混合物进行比较来评估络合物的形成。 FT-IR实验提供的数据表明,ACZ的碳酰胺基团参与了包含过程。体外释放数据表明,包含冷冻干燥的三元复合物和相应的ACZ与HP-β-CD和TEA的简单物理混合物的两种制剂均表现出ACZ的最快释放速率。这些结果表明,ACZ-HP-β-CD-TEA复合物代表了一种有效的新型制剂,可增强ACZ在水中的溶解度,使其有望用于眼科给药。

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