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Granulation Methods and the Mechanisms for Improving Hardness of Loxoprofen Sodium Hydrate-Containing Tablets

  • 0Research & Development Headquarters Self-Medication, Taisho Pharmaceutical Co., Ltd., 1-403 Yoshino-Cho, Kita-ku, Saitama 331-9530, Japan.
Pharmaceutics +

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April 26, 2025

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April 26, 2025

View abstract on PubMed

Summary

This summary is machine-generated.

Tablet hardness of loxoprofen sodium (LXP) tablets is influenced by granulation solvent and drying temperature. Ethanol and lower drying temperatures improved tablet hardness by affecting surface free energy and particle cohesion.

Area Of Science

  • Pharmaceutical Sciences
  • Materials Science

Background

  • Loxoprofen sodium (LXP) commonly exists as a dihydrate.
  • Tablet hardness is a critical quality attribute for pharmaceutical formulations.
  • Wet granulation is a common method for preparing tablets.

Purpose Of The Study

  • To investigate the compression mechanisms of loxoprofen sodium (LXP).
  • To identify parameters influencing LXP tablet hardness during wet granulation.
  • To understand the role of solvent and drying conditions on LXP tablet properties.

Main Methods

  • LXP granules were prepared using water or ethanol as solvents.
  • Granules were dried under varied conditions and sieved for particle size.
  • Tablets were compressed after adding 1% magnesium stearate (Mg-st).
  • Principal Component Analysis (PCA) and crystal structure analysis were employed.

Main Results

  • Granulation solvent and drying temperature significantly impacted tablet hardness.
  • Ethanol as a solvent resulted in higher tablet hardness compared to water.
  • Tablet hardness correlated positively with surface free energy (SFE) and polar component (γ(p)), and negatively with the dispersive component (γ(d)).
  • Anhydrous LXP forms, favored by specific drying temperatures, exhibited higher hardness due to increased γ(p).

Conclusions

  • Optimizing solvent selection and drying temperature is crucial for enhancing LXP tablet hardness.
  • Surface free energy assessment aids in selecting appropriate excipients for improved tablet properties.
  • Understanding LXP hydration states and their impact on physical properties is key for formulation development.

Keywords:

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