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Objective <p> This study aimed to investigate the pH-dependent dissolution of the weakly basic drug carvedilol (BCS Class II) and systematically examine the influence of citric acid concentration and particle size on its release.</p> Methods <p> A series of dissolution studies was conducted in media simulating the gastrointestinal pH range (1.2-7.8), specifically evaluating the effects of citric acid concentration (3% and 9%) and particle size (fine<b> D</b><b>v</b><b>50</b> 44 μm vs. coarse <b>D</b><b>v</b><b>50</b> 608 μm).</p> Results <p> Under acidic conditions (pH 1.2-1.6), carvedilol solubility was high and the effect of citric acid particle size was negligible (&lt;1.3% difference). In the mid-pH range (3.8-6.5), fine citric acid particles rapidly created an acidic microenvironment (pH 3.5±0.2), enhancing carvedilol solubility 2.1-2.8-fold and improving dissolution by 3.1-15.7% compared to coarse particles; increasing the citric acid concentration from 3% to 9% reduced this particle size-dependent variability. At high pH (6.8-7.8), the effect of citric acid weakened, though coarse particles still prolonged acid release.</p> Conclusion <p> While citric acid concentration universally enhanced carvedilol dissolution, the effect of its particle size was pH-dependent, being negligible at low pH but pronounced at higher pH, where larger particles sustained drug release more effectively.</p>

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Optimizing Particle Size of pH Modifiers Enhances Dissolution of Weakly Basic Drugs

  • 期刊论文

  • 发表日期：

    2026年4月18日

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  • Kejia Wu,
  • Yupeng Feng,
  • Zherui Zhang,
  • Junyao Jiao,
  • Weiwei Zhang,
  • Dandan Wei,
  • Haibing He,
  • Yu Zhang,
  • Tian Yin,
  • Zhihong Bao,
  • Yanjiao Wang,
  • Xing Tang

摘要

Objective

This study aimed to investigate the pH-dependent dissolution of the weakly basic drug carvedilol (BCS Class II) and systematically examine the influence of citric acid concentration and particle size on its release.

Methods

A series of dissolution studies was conducted in media simulating the gastrointestinal pH range (1.2-7.8), specifically evaluating the effects of citric acid concentration (3% and 9%) and particle size (fine Dv50 44 μm vs. coarse Dv50 608 μm).

Results

Under acidic conditions (pH 1.2-1.6), carvedilol solubility was high and the effect of citric acid particle size was negligible (<1.3% difference). In the mid-pH range (3.8-6.5), fine citric acid particles rapidly created an acidic microenvironment (pH 3.5±0.2), enhancing carvedilol solubility 2.1-2.8-fold and improving dissolution by 3.1-15.7% compared to coarse particles; increasing the citric acid concentration from 3% to 9% reduced this particle size-dependent variability. At high pH (6.8-7.8), the effect of citric acid weakened, though coarse particles still prolonged acid release.

Conclusion

While citric acid concentration universally enhanced carvedilol dissolution, the effect of its particle size was pH-dependent, being negligible at low pH but pronounced at higher pH, where larger particles sustained drug release more effectively.