Preparation and Characterization of Fluconazole- Resorcinol Co-crystal

Authors

  • Fikri Alatas Alatas Fakultas Farmasi, Universitas Jenderal Achmad Yani ,
  • Hestiary Ratih Fakultas Farmasi, Universitas Jenderal Achmad Yani ,
  • Titta Hartyana Sutarna Fakultas Farmasi, Universitas Jenderal Achmad Yani ,
  • Yoga Windu Wardhana 2Fakultas Farmasi, Universitas Padjadjaran ,
  • Dini Tereslina Fakultas Farmasi, Universitas Jenderal Achmad Yani ,
  • Sundani Nurono Soewandhi 3Sekolah Farmasi, Institut Teknologi Bandung ,

DOI:

https://doi.org/10.35814/jifi.v18i2.779

Keywords:

fluconazole, resorcinol, solubility, co-crystal, powder X-ray diffraction

Abstract

Fluconazole (FLU), an oral antifungal widely used in the treatment of vaginitis and
candidiasis, is known to have low bioavailability due to its low solubility. The purpose of this study
was to prepare and characterize co-crystal fl uconazole-resoscinol (FLU-RES). The preparation of
co-crystal was performed by grinding together the equimolar mixture of FLU-RES which is dripped
with a few ethanol. Powder X-ray diff raction, diff erential scanning calorimetry (DSC), and polarized
microscopy methods were performed to characterize the formation of FLU-RES co-crystal. Relevant
physicochemical properties include solubility tests in water and dissolution tests in pH 1.2; 4.5 and
6.8 buff er solution. The powder X-ray diff ractogram of FLU-RES milled result showed the presence
of new peaks and loss of the main peaks of FLU and RES. The characterization of grinding result by
DSC and polarized microscopy methods also showed the co-crystal formation between FLU and RES.
The solubility of FLU-RES co-crystal in water is solubility two folds more than pure FLU, while its
dissolution rate is 1.67-1.72 times faster than pure FLU.

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Published

2020-10-28

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Articles