Solubility Enhancement

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Solubility results vary from batch-to-batch? Or you’ve obtained out-of-specification dissolution test results?

Possible checklist: 

  • Polymorphism of your drug substance
  • Variation in particle size distribution from batch-to-batch
  • Quality problem due to particle segregation in manufacturing
  • Water-induced phase transformation in the solubility buffer
  • The crystallisation of the amorphous material
  • Precipitation due to salt disproportionation or co-crystal dissociation
  • Instability of suspension formulation due to particle size growth during storage
  • Formation of rubbery state for amorphous drug/excipient or gelatine capsule
  • The thickness of the coating for control release (CR) or modified release (MR) product 

Consult our Experts

Dr. Wenbo Wang
QC Chemist

Dr. Anna Shevchenko
Principal Scientist

Literature

Chauhan H, Kuldipkumar A, Barder T, Medek A, Gu C H, Atef E (2014) Correlation of Inhibitory Effects of Polymers on Indomethacin Precipitation in Solution and Amorphous Solid Crystallization Based on Molecular Interaction, Pharm Res 31(2): 500-515.

Jensen LG, Skautrup FB, Müllertz A, Abrahamsson B, Rades T, Priemel PA (2017) Amorphous is not always better—A dissolution study on solid state forms of carbamazepine. Int J Pharm 522(1-2):74-9.

Konno H, Taylor L S (2006) Influence of Different Polymers on the Crystallisation Tendency of Molecularly Dispersed Amorphous Felodipine. J Pharm Sci 95(12): 2692-2705.

Lehto P, Aaltonen J, Tenho M, Rantanen J, Hirvonen J, Tanninen VP, Peltonen L. (2009) Solvent-Mediated Solid Phase Transformations of cArbamazepine: Effects of Simulated Intestinal Fluid and Fasted State Simulated Intestinal Fluid, J Pharm Sci, 98(3): 985-996..

Shevchenko A, Bimbo LM, Miroshnyk I, Haarala J, Jelínková K, Syrjänen K, van Veen B, Kiesvaara J, Santos HA, Yliruusi J. (2012 ) A new co-crystal and salts of itraconazole: comparison of solid-state properties, stability and dissolution behaviour. Int J Pharm 436(1-2):403-409.

Sovago I, Wang W,  Qiu D, Raijada D, Rantanen J, Grohganz H, Rades T, Bond A D, Löbmann K (2016) Properties of the Sodium Naproxen-Lactose-Tetrahydrate Co-Crystal upon Processing and Storage. Molecules 21(4), 509.

Xia D, Wu J X, Cui F, Qu H, Rades T, Rantanen J, Yang M (2012) Solvent-mediated amorphous-to-crystalline transformation of nitrendipine in amorphous particle suspensions containing polymers. Eur J Pharm Sci 46(5): 446-454  

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