Abstract

The aim of this work is to investigate the solubility enhancement of ibuprofen by formation of stable amorphous ternary system (ibuprofen, polyvinylpyrrolidon, β-cyclodextrin) compared to the binary system (ibuprofen, β-cyclodextrin). Ibuprofen was co-milled at ambient temperature in presence of PVP K30 and β‑cyclodextrin. The characterization of obtained mixtures was carried out using X-ray diffraction, infrared spectroscopy, scanning electronic microscope, differential scanning calorimetry and spectroscopy (¹H/¹³C). The dissolution test was carried out in order to evaluate the release rate profiles of ibuprofen in the prepared mixtures. A thermodynamically stable and water-soluble ternary system was obtained, the released amount of ibuprofen in the ternary system increased considerably in comparison to the pure drug. These results highlighted the effect of PVP which enhanced the aqueous solubility of the binary system ibuprofen/β-cyclodextrin in solid state by reinforcing intermolecular interactions and improving complexing abilities of β‑cyclodextrin.

中文翻译：

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水溶性稳定的三元体系的形成：布洛芬/β-环糊精/ PVP

摘要

这项工作的目的是研究与二元体系（布洛芬，β-环糊精）相比，通过形成稳定的无定形三元体系（布洛芬，聚乙烯吡咯烷酮，β-环糊精）来提高布洛芬的溶解度。布洛芬在存在PVP K30和β-环糊精的环境温度下共同研磨。使用X射线衍射，红外光谱，扫描电子显微镜，差示扫描量热法和光谱法（¹ H / ¹³C）。进行溶出试验以评估布洛芬在制备的混合物中的释放速率分布。获得了热力学稳定且水溶性的三元体系，与纯药物相比，布洛芬在三元体系中的释放量大大增加。这些结果突出了PVP的作用，该作用通过增强分子间的相互作用并改善β-环糊精的络合能力，从而提高了二元系统布洛芬/β-环糊精在固态下的水溶性。