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<p>The dissolution behaviour of sub-micronized nanocrystals, especially for poorly soluble drugs, is quite unpredictable. Mesalamine (MES) is a high-dose, poorly soluble drug with two pKa and four ionic forms. The fabrication of sub-micronized nanocrystals reduces the dose, pill burden, and improves the therapeutic adherence. The present study investigates the dissolution behaviour of sub-micronized mesalamine (SMES), also known as nanocrystals, micronized crystals, suspension, and tablets, using different dissolution methods and the USP dissolution apparatus. The method parameters, including the choice of apparatus, hydrodynamics, buffer capacity, pH, and volume of the media, were optimized to achieve the optimal dissolution method for discriminating particle sizes. The particle size discriminatory powder dissolution method (method 5) was developed using the 1&#xa0;mm beads in the USP Type I apparatus. The dissolution efficacy of MES and SMES was found to be 31.2% and 88.2%, respectively, at 60&#xa0;min. The suspension dissolution studies for both MES and SMES were performed using the USP Type II apparatus. The dissolution efficacy at 30&#xa0;min was found to be 74% and 93% for MES and SMES. The sonication of the suspension provides better discrimination due to the de-aggregation of particles. The dissolution profiles of tablets with MES and SMES were compared, using hydrodynamics as the key variable, and a six-fold reduction in the extent of the dissolution was observed with SMES. This finding suggests the need for formulation and process optimization for improving the dissolution and bioavailability of MES using sub-micronized particles.</p>

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Dissolution behaviour of mesalamine nanocrystals, micronised crystals, suspensions, and tablets: a method development perspective

  • 期刊论文

  • 发表日期：

    2026年4月17日

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  • Sonam Sharma,
  • Sakshi Anil Kunjir,
  • Prajakta Raosaheb Pathare,
  • Sadhana Dhayagala,
  • Prakash Kumar Sirvi,
  • Rajkumar Malayandi

摘要

The dissolution behaviour of sub-micronized nanocrystals, especially for poorly soluble drugs, is quite unpredictable. Mesalamine (MES) is a high-dose, poorly soluble drug with two pKa and four ionic forms. The fabrication of sub-micronized nanocrystals reduces the dose, pill burden, and improves the therapeutic adherence. The present study investigates the dissolution behaviour of sub-micronized mesalamine (SMES), also known as nanocrystals, micronized crystals, suspension, and tablets, using different dissolution methods and the USP dissolution apparatus. The method parameters, including the choice of apparatus, hydrodynamics, buffer capacity, pH, and volume of the media, were optimized to achieve the optimal dissolution method for discriminating particle sizes. The particle size discriminatory powder dissolution method (method 5) was developed using the 1 mm beads in the USP Type I apparatus. The dissolution efficacy of MES and SMES was found to be 31.2% and 88.2%, respectively, at 60 min. The suspension dissolution studies for both MES and SMES were performed using the USP Type II apparatus. The dissolution efficacy at 30 min was found to be 74% and 93% for MES and SMES. The sonication of the suspension provides better discrimination due to the de-aggregation of particles. The dissolution profiles of tablets with MES and SMES were compared, using hydrodynamics as the key variable, and a six-fold reduction in the extent of the dissolution was observed with SMES. This finding suggests the need for formulation and process optimization for improving the dissolution and bioavailability of MES using sub-micronized particles.