PREPARATION OF ACYCLOVIR-NICOTINAMIDE COCRYSTAL BY SOLVENT EVAPORATION TECHNIQUE WITH VARIATION OF SOLVENT

Roisah Nawatila; Agnes Nuniek W; Siswandono Siswodihardjo; Dwi Setyawan

doi:10.22159/ajpcr.2017.v10i3.16149

Authors

Roisah Nawatila Airlangga University
Agnes Nuniek W
Siswandono Siswodihardjo
Dwi Setyawan

DOI:

https://doi.org/10.22159/ajpcr.2017.v10i3.16149

Abstract

ABSTRACT
Objective: This research aims to prepare cocrystal of acyclovir (ACV)-nicotinamide (NCT) by solvent evaporation with a variation of solvent (ethanol,
glacial acetic acid, and HCl 0.1 N) to improve the bioavailability of ACV as an antiviral drug.
Methods: Cocrystal were developed by solvent evaporation with 1:1 molar fraction, using variation of solvent such as ethanol, glacial acetic acid, and
HCl 0.1 N. Further, the prepared ACV-NCT cocrystal were characterized for differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD),
Fourier transform infrared spectroscopy (FT-IR), scanning electron microscope (SEM), and in vitro dissolution.
Results: DSC thermogram showed that ACV-NCT cocrystal in ethanol and glacial acetic acid exhibited new endothermic peak at 221.16Â°C and
216.40Â°C, whereas no peaks were found for HCl 0.1 N. PXRD diffractogram showed that ACV-NCT cocrystal in ethanol exhibited new diffraction peaks
at 2Î¸ 5.9Â°; 9.2Â°; dan 13.3Â°, whereas no peaks were found for glacial acetic acid and HCl 0.1 N. FT-IR characterization of ACV-NCT cocrystal in ethanol
showed disappearance of transmission peaks at 3373/cm indicating the loss of NH bands of NCT. Furthermore, C=O of ACV and NCT were observed at
1693/cm, and 1666/cm indicated a formation of hydrogen bonding between ACV and NCT. SEM micrographs showed that cocrystals have a different
shape compared to ACV and NCT. DE15 showed that there was a significant increase of ACV-NCT cocrystal dissolution rate in ethanol compared to the
physical mixture and ACV.
Conclusion: The study concludes that ACV-NCT cocrystal in ethanol were successfully formed and the dissolution rate of ACV can increase significantly
(Î±=0.05).
Keywords: Cocrystallization, Solvent, Acyclovir, Nicotinamide, Solvent evaporation.

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References

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