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Cocrystal formation between didanosine and two aromatic acids

Alatas F.a,b, Soewandhi S.N.a, Sasongko L.a, Ismunandara, Uekusa H.c

a School of Pharmacy, Bandung Institute of Technology, Indonesia
b Department of Pharmacy, University of Jenderal Achmad Yani, Indonesia
c Department Chemistry and Material Science, Tokyo Institute of Technology, Japan

[vc_row][vc_column][vc_row_inner][vc_column_inner][vc_separator css=”.vc_custom_1624529070653{padding-top: 30px !important;padding-bottom: 30px !important;}”][/vc_column_inner][/vc_row_inner][vc_row_inner layout=”boxed”][vc_column_inner width=”3/4″ css=”.vc_custom_1624695412187{border-right-width: 1px !important;border-right-color: #dddddd !important;border-right-style: solid !important;border-radius: 1px !important;}”][vc_empty_space][megatron_heading title=”Abstract” size=”size-sm” text_align=”text-left”][vc_column_text]Objective: Cocrystal is becoming attractive as solid form to be developed in the pharmaceutical industry. The formation of intermolecular bonds between active pharmaceutical ingredient (API) and coformer can change the physicochemical properties of an API without altering its pharmacological activity. Methods: In this research, cocrystals formation between an anti-HIV drug didanosine (DDI) and two aromatic acids (benzoic acid and salicylic acid) coformer in equimolar ratio have been prepared by solvent-drop grinding with methanol and acetonitrile as solvents. Cocrystal formation of didanosine-benzoic acid (DDI-BA) and didanosine-salicylic acid (DDI-SAA) was characterized by powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), fourier transform infrared (FTIR) spectroscopy, and polarized microscopy methods. Results: The PXRD patterns of DDI-BA and DDI-SAA after solvent-drop grinding are different from pure components. As the solvent drop grinding proceed, the characteristic peaks of DDI in 6.1° and 10.7° 2θ disappeared, while new peaks appear at 5.0° and 10.1° 2θ in DDI-BA cocrystal and 4.7° and 10.0° 2θ in DDI-SAA cocrystal. In addition, physical characterization showed that DDI-BA and DDI-SAA cocrystals after solvent-drop grinding have unique thermal, spectroscopic, and microscopic. Conclusion: The characterization results indicate that didanosine form cocrystals with benzoic acid and salicylic acid by solvent-drop grinding method with methanol and acetonitrile as solvents.[/vc_column_text][vc_empty_space][vc_separator css=”.vc_custom_1624528584150{padding-top: 25px !important;padding-bottom: 25px !important;}”][vc_empty_space][megatron_heading title=”Author keywords” size=”size-sm” text_align=”text-left”][vc_column_text][/vc_column_text][vc_empty_space][vc_separator css=”.vc_custom_1624528584150{padding-top: 25px !important;padding-bottom: 25px !important;}”][vc_empty_space][megatron_heading title=”Indexed keywords” size=”size-sm” text_align=”text-left”][vc_column_text]Benzoic acid,Cocrystal,Didanosine,Salicylic acid,Solvent-drop grinding[/vc_column_text][vc_empty_space][vc_separator css=”.vc_custom_1624528584150{padding-top: 25px !important;padding-bottom: 25px !important;}”][vc_empty_space][megatron_heading title=”Funding details” size=”size-sm” text_align=”text-left”][vc_column_text][/vc_column_text][vc_empty_space][vc_separator css=”.vc_custom_1624528584150{padding-top: 25px !important;padding-bottom: 25px !important;}”][vc_empty_space][megatron_heading title=”DOI” size=”size-sm” text_align=”text-left”][vc_column_text][/vc_column_text][/vc_column_inner][vc_column_inner width=”1/4″][vc_column_text]Widget Plumx[/vc_column_text][/vc_column_inner][/vc_row_inner][/vc_column][/vc_row][vc_row][vc_column][vc_separator css=”.vc_custom_1624528584150{padding-top: 25px !important;padding-bottom: 25px !important;}”][/vc_column][/vc_row]