Open AccessENHANCEMENT OF SOLUBILITY AND DISSOLUTION RATE OF ACETYLSALICYLIC ACID VIA CO-CRYSTALLIZATION TECHNIQUE: A NOVEL ASA-VALINE COCRYSTAL
Author(s) -
H K Shanthala,
H. V. Jayaprakash,
Muniganti Radhakrishna,
B.H. Jaswanth Gowda,
Karthika Paul,
S. J. Shankar,
Mohammed Gulzar Ahmed,
A Sanjana
Publication year - 2021
Publication title -
international journal of applied pharmaceutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.238
H-Index - 15
ISSN - 0975-7058
DOI - 10.22159/ijap.2021v13i1.40054
Subject(s) - cocrystal , crystallization , solubility , dissolution , differential scanning calorimetry , melting point , fourier transform infrared spectroscopy , chemistry , nuclear chemistry , hydrogen bond , organic chemistry , chemical engineering , molecule , physics , engineering , thermodynamics
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.