TY - JOUR
T1 - Co-crystalization of quercetin and malonic acid using solvent-drop grinding method
AU - Setyawan, Dwi
AU - Jovita, Rachel Olivia
AU - Iqbal, Muhammad
AU - Paramanandana, Abhimata
AU - Yusuf, Helmy
AU - Lestari, Maria L.A.D.
N1 - Publisher Copyright:
© Pharmacotherapy Group, Faculty of Pharmacy, University of Benin, Benin City, 300001 Nigeria and 2018 The authors.
PY - 2018/6
Y1 - 2018/6
N2 - Purpose: To determine the physicochemical properties and in vitro dissolution profile of quercetin-malonic acid co-crystals prepared using solvent-drop grinding method. Methods: Co-crystallization of quercetin (Q) and malonic acid (MA) in molar ratios of 1:1 (CC1) and 1:2 (CC2) was performed by solvent-drop grinding method with addition of 20 % (w/v) ethanol in a shaker mill run for 30 min. The co-crystal phase was characterized by differential scanning calorimetry (DSC), powder x-ray diffractometry (PXRD), scanning electron microscopy (SEM), and fourier transform infrared (FT-IR) spectroscopy. In vitro dissolution was performed using the paddle method at 100 rpm in the medium of citrate buffer (pH 5.0 ± 0.05) containing 2.0 % (w/v) sodium lauryl sulfate at 37 ± 0.5 °C. Results: Thermograms from DSC showed that CC1 and CC2 co-crystals had endothermic peaks at 283.02 and 266.61 °C, respectively. These peaks were in-between the melting points of Ma and Q. The powder diffractogram of CC1 showed new diffraction peaks at 16.21, 19.87, and 28.88 °, while CC2 showed new ones at 16.18, 19.86, and 28.83 °. There were OH-band shifts in IR spectra from 3411 to 3427 cm-1 for CC1, and from 3411 to 3466 cm-1 for CC2. Images from SEM indicate that the crystal habits and morphologies of the co-crystals differed from those of the original components. The dissolution efficiency of CC2 increased 1.056 times relative to pure Q. Conclusion: Co-crystal phase of Q and MA prepared using solvent-drop grinding (CC1 and CC2) displays physicochemical characteristics different from those of the physical mixtures and their pure components. There is an increase in vitro dissolution as a result of co-crystal formation.
AB - Purpose: To determine the physicochemical properties and in vitro dissolution profile of quercetin-malonic acid co-crystals prepared using solvent-drop grinding method. Methods: Co-crystallization of quercetin (Q) and malonic acid (MA) in molar ratios of 1:1 (CC1) and 1:2 (CC2) was performed by solvent-drop grinding method with addition of 20 % (w/v) ethanol in a shaker mill run for 30 min. The co-crystal phase was characterized by differential scanning calorimetry (DSC), powder x-ray diffractometry (PXRD), scanning electron microscopy (SEM), and fourier transform infrared (FT-IR) spectroscopy. In vitro dissolution was performed using the paddle method at 100 rpm in the medium of citrate buffer (pH 5.0 ± 0.05) containing 2.0 % (w/v) sodium lauryl sulfate at 37 ± 0.5 °C. Results: Thermograms from DSC showed that CC1 and CC2 co-crystals had endothermic peaks at 283.02 and 266.61 °C, respectively. These peaks were in-between the melting points of Ma and Q. The powder diffractogram of CC1 showed new diffraction peaks at 16.21, 19.87, and 28.88 °, while CC2 showed new ones at 16.18, 19.86, and 28.83 °. There were OH-band shifts in IR spectra from 3411 to 3427 cm-1 for CC1, and from 3411 to 3466 cm-1 for CC2. Images from SEM indicate that the crystal habits and morphologies of the co-crystals differed from those of the original components. The dissolution efficiency of CC2 increased 1.056 times relative to pure Q. Conclusion: Co-crystal phase of Q and MA prepared using solvent-drop grinding (CC1 and CC2) displays physicochemical characteristics different from those of the physical mixtures and their pure components. There is an increase in vitro dissolution as a result of co-crystal formation.
KW - Dissolution
KW - Malonic acid
KW - Quercetin
KW - SCo-crystal
KW - Solvent-drop grinding
UR - http://www.scopus.com/inward/record.url?scp=85049458251&partnerID=8YFLogxK
U2 - 10.4314/tjpr.v17i6.3
DO - 10.4314/tjpr.v17i6.3
M3 - Article
AN - SCOPUS:85049458251
SN - 1596-5996
VL - 17
SP - 997
EP - 1002
JO - Tropical Journal of Pharmaceutical Research
JF - Tropical Journal of Pharmaceutical Research
IS - 6
ER -