Open AccessPreparation and characterization of solid dispersion freeze-dried efavirenz – polyvinylpyrrolidone K-30
Author(s) -
Lili Fitriani,
Alianshar Haqi,
Erizal Zaini
Publication year - 2016
Publication title -
journal of advanced pharmaceutical technology and research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.325
H-Index - 33
eISSN - 2231-4040
pISSN - 0976-2094
DOI - 10.4103/2231-4040.184592
Subject(s) - polyvinylpyrrolidone , solubility , efavirenz , analytical chemistry (journal) , amorphous solid , chemistry , nuclear chemistry , dispersion (optics) , thermal analysis , fourier transform infrared spectroscopy , scanning electron microscope , materials science , chromatography , crystallography , chemical engineering , organic chemistry , thermal , medicine , physics , family medicine , human immunodeficiency virus (hiv) , meteorology , antiretroviral therapy , engineering , viral load , optics , composite material
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).