Quercetin has been proposed to exhibit numerous pharmacological benefits yet suffer low bioavailability due to the extremely low solubility. A research to study the impact of cocrystallization of quercetin with succinic acid on the solubility and dissolution profile has been performed. Cocrystallization in molar stoichiometry of 1:1 was carried out via liquid assisted grinding with methanol in ball milling apparatus. Cocrystal formation was identified by hot stage microscopy (HSM) at first, then cocrystal phase was characterized using differential thermal analysis (DTA), powder X-ray diffractometry (PXRD), scanning electron microscopy (SEM), and fourier-transform infrared (FT-IR) spectroscopy. Solubility and dissolution test were conducted as well. DSC thermogram exhibits new endothermic peak at 280.32°C representing the melting point of cocrystal phase alongside with endothermic point of pure compounds. Powder X-ray diffractograms show new diffraction peaks on behalf of cocrystal formation at 2θ=8.92, 9.88, 13.04, 29.78, 35.35°. FT-IR spectroscopy reveals band shifting in –OH group region. On SEM photographs, one can observe crystal habit of succinic acid being covered by crystal with different habit. This indicates that quercetin interacts with succinic acid only on the surfaces and causes imperfect formation of cocrystal phase. Cocrystallization quercetin improves solubility by 1.62 times higher and dissolution rate by 1.25 higher than pure quercetin (one-way ANOVA, p < 0.05).

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The aim of this study was to determine the effect of binder and disintegrant excipients toward tablet properties of levofloxacin as the latter tends to suffer brittle fracture upon compression. The excipients used were povidone K-30 as the binder and sodium starch glycolate (SSG) as the disintegrant which the tablets were formulated according to factorial design 22 with two factors and two levels on each factor. Four formulas were prepared by wet granulation method using 2 and 4% of each povidone K-30 and sodium starch glycolate in various compositions. Tablet properties were evaluated for its hardness, friability, and disintegration time as well as dissolution profile. The data obtained was statistically analyzed using Minitab® 17 software to optimize the formulation and resulted in different impacts caused by each excipient. Povidone K-30 exhibited an increment in hardness, friability, disintegration time but a decrease indissolution profile of levofloxacin tablet. SSG decreased hardnessand disintegration time, but increased friability and dissolution profile of levofloxacin tablet. Overlaid contour plot showed that the optimal formula regarding tablet properties of friability, disintegration time, and dissolution profile is in composition of 2.01% povidone K-30 and 2.01% sodium starch glycolate. Keywords: levofloxacin tablet, povidone K-30, sodium starch glycolate, factorial design.

Loratadine belongs to second generation antihistamine (H1) drug and is known to form cocrystal with succinic acid in stoichiometry of 1:1 using slurry method. This study was conducted to further investigate cocrystal phase behavior upon compression. Sample of cocrystal phase was compressed with various compression forces into tablet form on 10 mm diameter punch. Then, the tablet was characterized for the mechanical properties and physical characterization was conducted using Differential Thermal Analysis (DTA), X-ray Powder Diffraction (XRPD), and Scanning Electron Microscope (SEM). According to tensile strength profile, cocrystal phase showed better mechanical property as it possessed higher tensile strength value compared to loratadine alone. DTA thermograms exhibited succinic acid characteristic peak alongside with endothermic peak of cocrystal phase which were compressed on higher force. It suggests that cocrystal undergoes partial dissociation to the starting components under compression. Powder diffractograms showed reduced intensity of tableted cocrystal compared to powder one for all compression force. SEM photomicrograph observed a loss of particle boundaries of cocrystal upon compression, as sintering phenomena occurred. It is predicted that compression force can influence physical characteristics of cocrystal of loratadine-succinic acid by driving dissociation and sintering phenomena.

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