Preparation and characterization of solid dispersion freeze-dried efavirenz - polyvinylpyrrolidone K-30

The aim of this research is to prepare and characterize solid dispersion of efavirenz - polyvinylpyrrolidone (PVP) K-30 by freeze drying to increase its solubility. Solid dispersion of efavirenz - PVP K-30 was prepared by solvent evaporation method with ratio 2:1, 1:1, and 1:2 and dried using a free...

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Bibliographic Details
Published in:Journal of advanced pharmaceutical technology and research 2016-07, Vol.7 (3), p.105-109
Main Authors: Fitriani, Lili, Haqi, Alianshar, Zaini, Erizal
Format: Article
Language:English
Subjects:
Acetic acid
Acetonitrile
Aluminum
Analysis
Antiretroviral agents
Carbon dioxide
Chemical properties
Drying
Efavirenz
Evaporation
Fourier transforms
freeze dried
High-performance liquid chromatography
Hydrogen
Infrared spectroscopy
Liquid chromatography
Morphology
Nitriles
Original
Polyethylene glycol
Polyvinylpyrrolidone
polyvinylpyrrolidone K-30
Powder
Ratios
Scanning electron microscopy
solid dispersion
Solubility
Solvents
Spectrum analysis
X-ray diffraction
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Summary:The aim of this research is to prepare and characterize solid dispersion of efavirenz - polyvinylpyrrolidone (PVP) K-30 by freeze drying to increase its solubility. Solid dispersion of efavirenz - PVP K-30 was prepared by solvent evaporation method with ratio 2:1, 1:1, and 1:2 and dried using a freeze dryer. Characterizations were done by scanning electron microscopy (SEM), powder X-ray diffraction analysis, differential thermal analysis (DTA), and Fourier transform infrared (FT-IR) spectroscopy. Solubility test was carried out in CO2-free distilled water, and efavirenz assay was conducted using high-performance liquid chromatography with acetonitrile:acetic acid (80:20) as the mobile phases. Powder X-ray diffractogram showed a decrease in the peak intensity, which indicated the crystalline altered to amorphous phase. DTA thermal analysis showed a decrease in the melting point of the solid dispersion compared to intact efavirenz. SEM results indicated the changes in the morphology of the crystal into an amorphous form compared to pure components. FT-IR spectroscopy analysis showed a shift wavenumber of the spectrum efavirenz and PVP K-30. The solubility of solid dispersion at ratio 2:1, 1:1, and 1:2 was 6.777 μg/mL, 6.936 μg/mL, and 14,672 μg/mL, respectively, whereas the solubility of intact efavirenz was 0.250 μg/mL. In conclusion, the solubility of solid dispersion increased significantly (P < 0.05).
ISSN:2231-4040
0976-2094
DOI:10.4103/2231-4040.184592