溶剂蒸发与热熔挤出技术制备布洛芬共晶的对比评价,Journal of Drug Delivery Science and Technology

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溶剂蒸发与热熔挤出技术制备布洛芬共晶的对比评价
Journal of Drug Delivery Science and Technology ( IF 4.5 ) Pub Date : 2021-12-12 , DOI: 10.1016/j.jddst.2021.103003
Sharvari M. Kshirsagar ₁ , Bandoo C. Chatale ₁ , Purnima D. Amin ₁

Affiliation

布洛芬（IBP）是BCS II类药物，属于非甾体抗炎药（NSAID）类别，溶解度非常差。在本研究中，我们探索了共结晶作为增强 IBP 溶解度的方法。基于其与 IBP 的 pKa 差异、汉森溶解度参数 (HSP) 和计算研究，选择 -脯氨酸作为共形成剂。最初的试验采用溶剂蒸发法，后来通过热熔挤出技术进行研究以比较结果。通过视觉形态、扫描电子显微镜 (SEM)、差示扫描量热法 (DSC)、傅里叶变换红外光谱 (FT-IR) 和粉末 X 射线衍射 (PXRD) 研究对共晶进行表征。进一步评估共晶的接触角研究、溶解度研究、溶解研究、流动特性和压缩性研究。与普通 IBP 相比，共晶在 SEM 研究中显示出不同的形态。DSC 热分析图揭示了共晶的新熔化吸热线。在 FT-IR 研究中还观察到峰移和谱带展宽，表明形成了共晶。使用 PXRD 研究证实了晶格的变化。体外溶出研究表明，与物理混合物相比，共晶的药物释放量更高，但不同介质中的释放情况不同。在压缩性研究期间没有观察到共晶结晶度的变化。因此，成功地探索了以β-脯氨酸作为共形成剂的IBP共晶的熔融挤出技术。

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Comparative evaluation of ibuprofen co-crystals prepared by solvent evaporation and hot melt extrusion technology

Ibuprofen (IBP) is a BCS Class – II drug that belongs to Non-Steroidal Anti-Inflammatory Drug (NSAID) category, having very poor solubility. In the present study, we have explored co-crystallization as a method of solubility enhancement of IBP. -proline was selected as co-former based on its pKa difference with IBP, Hansen Solubility Parameter (HSP), and computational studies. The initial trials were taken using solvent evaporation method and later studied by hot melt extrusion technique to compare the results. The co-crystals were characterized by visual morphology, Scanning Electron Microscopy (SEM), Differential Scanning Calorimetry (DSC), Fourier Transform-Infrared Spectroscopy (FT-IR), and Powder X-Ray Diffraction (PXRD) studies. The co-crystals were further evaluated for contact angle studies, solubility studies, dissolution studies, flow properties, and compressibility studies. Co-crystals showed distinct morphology in the SEM study compared to plain IBP. The DSC thermogram revealed a new melting endotherm of the co-crystals. Peak shifts and band broadening were also observed in FT-IR study indication formation co-crystals. The change in crystal lattice was confirmed using PXRD studies. In-vitro dissolution studies have shown higher drug release of co-crystals compared to physical mixture however the release differed in different media. No change in crystallinity of co-crystals was observed during compressibility studies. Thus, melt extrusion technique was successfully explored for IBP co-crystals using -proline as the co-former.

更新日期：2021-12-12

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