ENHANCEMENT OF SOLUBILITY AND DISSOLUTION RATE OF ACETYLSALICYLIC ACID VIA CO-CRYSTALLIZATION TECHNIQUE: A NOVEL ASA-VALINE COCRYSTAL

  • SHANTHALA H. K. Department of Chemistry, Sri Siddhartha Academy of Higher Education, Tumkur, India 572107
  • JAYAPRAKASH H. V. Department of Chemistry, Sri Siddhartha Institute of Technology, Tumkur, India 572105
  • MUNIGANTI RADHAKRISHNA Department of Chemistry, Sri Siddhartha Academy of Higher Education, Tumkur, India 572107
  • JASWANTH GOWDA B. H. Department of Pharmaceutics, Yenepoya Pharmacy College and Research Centre, Yenepoya (Deemed to be University), Mangaluru, India 575018
  • KARTHIKA PAUL Department of Pharmaceutical Sciences, Vivekananda College of Pharmacy, Dr. Rajkumar Road, Rajajinagar 2nd Stage, Bengaluru, India 560055
  • S. J. SHANKAR Department of Pharmaceutical Sciences, Vivekananda College of Pharmacy, Dr. Rajkumar Road, Rajajinagar 2nd Stage, Bengaluru, India 560055
  • MOHAMMED GULZAR AHMED Department of Pharmaceutics, Yenepoya Pharmacy College and Research Centre, Yenepoya (Deemed to be University), Mangaluru, India 575018
  • SANJANA A. Department of Pharmaceutics, Yenepoya Pharmacy College and Research Centre, Yenepoya (Deemed to be University), Mangaluru, India 575018,

Abstract

Objective: This study aims to synthesize acetylsalicylic acid (ASA) cocrystals using valine as a coformer via a co-crystallization technique to increase the solubility and dissolution rate of ASA.


Methods: The ASA-valine cocrystal (1:1 molar ratio) was prepared using the solvent evaporation technique with ethanol: water (50:50). The cocrystal was characterized using Fourier transform infrared spectroscopy (FT-IR), Differential scanning calorimetry (DSC), Powder X-ray diffraction (PXRD), Scanning electron microscopy (SEM), melting point to confirm the formation of cocrystal. The evaluation of cocrystal was done by drug content determination, solubility and dissolution studies.


Results: The prepared cocrystal was successfully confirmed for the formation of a hydrogen bond. The melting point of prepared cocrystal was decreased compared to pure ASA and valine, which indicated the formation of a new crystalline form. The FT-IR studies showed the formation of a new hydrogen bond by shifting the-O-H,-C=O and-N-H functional groups. SEM studies ensured that the prepared cocrystals were in needle-like appearance. Finally, DSC and PXRD studies were also indicated the successful formation of ASA-valine cocrystal. The drug release of cocrystal was found to be 100% at 60th min. Where in the case of pure ASA and marketed product of ASA exhibited the dissolution rate of 59% and 69% at 60th min respectively.


Conclusion: The co-crystallization technique can be adopted as the best strategy to increase the solubility and dissolution rate of BCS class 2 drugs. Therefore the prepared ASA-valine cocrystal can be a greater alternative to increase the solubility and dissolution rate compared with pure and marketed ASA.

Keywords: Acetylsalicylic acid, Valine, Co-crystallization, Solvent evaporation technique, Solubility enhancement, Dissolution rate, Cocrystals, Powder x-ray diffraction, Differential scanning calorimetry

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H. K., S., H. V., J., RADHAKRISHNA, M., B. H., J. G., PAUL, K., SHANKAR, S. J., AHMED, M. G., & A., S. (2021). ENHANCEMENT OF SOLUBILITY AND DISSOLUTION RATE OF ACETYLSALICYLIC ACID VIA CO-CRYSTALLIZATION TECHNIQUE: A NOVEL ASA-VALINE COCRYSTAL. International Journal of Applied Pharmaceutics, 13(1), 199-205. https://doi.org/10.22159/ijap.2021v13i1.40054
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