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<p>This study developed a novel aprepitant (APT) nanocrystal-containing oral disintegrating tablet (ODT) to enhance the oral bioavailability of APT through “rapid disintegration”. APT nanocrystal suspension (APT-NS) was prepared via miniaturized media milling, with a particle size of 199.25 ± 12.88&#xa0;nm, a polydispersity index (PDI) of 0.148 ± 0.026 and zeta potential of -24.82 ± 1.28&#xa0;mV. The APT-NS was spray-dried into dry powders (APT-NCS) and further processed into ODTs via freeze-drying. Through central composite design-response surface methodology (CCD-RSM) optimization, the final APT-ODT formulation demonstrated rapid disintegration (&lt; 5&#xa0;s) and excellent dissolution (&gt; 95% within 2&#xa0;min). Results of X-ray diffraction (XRD), differential scanning calorimetry (DSC), and Fourier transform infrared spectroscopy (FTIR) confirmed the absence of crystalline transformation or chemical degradation during processing. Pharmacokinetic results demonstrated that both APT-NS and APT-ODTs exhibited approximately twofold higher AUC<sub>0-48&#xa0;h</sub> (28.51 ± 1.62&#xa0;μg·h/mL and 32.61 ± 2.19&#xa0;μg·h/mL, respectively) compared to free APT. In conclusion, the optimized APT-ODT successfully improved the oral bioavailability of APT, representing a promising new strategy for clinical application.</p> Graphical Abstract <p>APT nanocrystalline suspension (APT-NS) was prepared by micro-media milling, with hydroxypropyl cellulose and sodium dodecyl sulfate as the stabilizers. Then the nanosuspension was spray-dried into the dry powder (APT-NCS), based on which the binder pullulan polysaccharide and the backbone agent mannitol were added and then lyophilized to form oral disintegrating tablets (ODTs). In vivo pharmacokinetic data demonstrated that the optimized APT-ODT substantially increased the bioavailability of APT.</p> <p></p>

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A Novel Oral Disintegrating Tablet Containing Aprepitant Nanocrystal Developed by Freeze-Drying Technology: An Effective Strategy to Enhance Aprepitant Bioavailability

  • 期刊论文

  • 发表日期：

    2025年12月10日

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  • Yutong Li,
  • Meihui Yi,
  • Keke Ma,
  • Jingxin Gou,
  • Tian Yin,
  • Yu Zhang,
  • Xing Tang,
  • Haibing He

摘要

This study developed a novel aprepitant (APT) nanocrystal-containing oral disintegrating tablet (ODT) to enhance the oral bioavailability of APT through “rapid disintegration”. APT nanocrystal suspension (APT-NS) was prepared via miniaturized media milling, with a particle size of 199.25 ± 12.88 nm, a polydispersity index (PDI) of 0.148 ± 0.026 and zeta potential of -24.82 ± 1.28 mV. The APT-NS was spray-dried into dry powders (APT-NCS) and further processed into ODTs via freeze-drying. Through central composite design-response surface methodology (CCD-RSM) optimization, the final APT-ODT formulation demonstrated rapid disintegration (< 5 s) and excellent dissolution (> 95% within 2 min). Results of X-ray diffraction (XRD), differential scanning calorimetry (DSC), and Fourier transform infrared spectroscopy (FTIR) confirmed the absence of crystalline transformation or chemical degradation during processing. Pharmacokinetic results demonstrated that both APT-NS and APT-ODTs exhibited approximately twofold higher AUC0-48 h (28.51 ± 1.62 μg·h/mL and 32.61 ± 2.19 μg·h/mL, respectively) compared to free APT. In conclusion, the optimized APT-ODT successfully improved the oral bioavailability of APT, representing a promising new strategy for clinical application.

Graphical Abstract

APT nanocrystalline suspension (APT-NS) was prepared by micro-media milling, with hydroxypropyl cellulose and sodium dodecyl sulfate as the stabilizers. Then the nanosuspension was spray-dried into the dry powder (APT-NCS), based on which the binder pullulan polysaccharide and the backbone agent mannitol were added and then lyophilized to form oral disintegrating tablets (ODTs). In vivo pharmacokinetic data demonstrated that the optimized APT-ODT substantially increased the bioavailability of APT.