Improvement in vitro Dissolution Rate of Quercetin Using Cocrystallization of Quercetin-Malonic Acid

https://doi.org/10.22146/ijc.28511

Dwi Setyawan(1*), Sukma Adhi Permata(2), Ahmad Zainul(3), Maria Lucia Ardhani Dwi Lestari(4)

(1) Department of Pharmaceutics, Faculty of Pharmacy, Universitas Airlangga, Jl. Dharmawangsa Dalam, Surabaya 60286, Indonesia
(2) Department of Pharmaceutics, Faculty of Pharmacy, Universitas Airlangga, Jl. Dharmawangsa Dalam, Surabaya 60286, Indonesia
(3) Department of Pharmaceutics, Faculty of Pharmacy, Universitas Airlangga, Jl. Dharmawangsa Dalam, Surabaya 60286, Indonesia
(4) Department of Pharmaceutics, Faculty of Pharmacy, Universitas Airlangga, Jl. Dharmawangsa Dalam, Surabaya 60286, Indonesia
(*) Corresponding Author

Abstract


The aim of the study was to improve the in-vitro dissolution rate of quercetin (Qu) using cocrystallization of quercetin. Cocrystals of quercetin (Co Qu) were produced with malonic acid (Ma) as coformer at ratio 1:2 using solvent evaporation method. Cocrystals quercetin-malonic acid (Co Qu-Ma) was characterized using Differential Thermal Analysis (DTA), Powder X-Ray Diffraction (PXRD), Scanning Electron Microscope (SEM), and Fourier Transforms Infrared Spectrophotometer (FTIR) and in-vitro dissolution study. A new endothermic peak at 277.9 °C was shown from the thermogram. Diffractogram of Co Qu-Ma showed a new diffraction peak at 2θ 9.81, 12.99, and 19.80°. Microphotograph showed that Qu and Ma exhibited a columnar-shaped and a pebble-shaped crystal, respectively, and FTIR wavenumber of O-H functional group of quercetin was shifted from its original position at 3411 to 3428 cm-1 in the physical mixture (pm) of Qu-Ma and 3418 cm-1 in Co Qu-Ma, respectively. The physicochemical characterizations using DTA, PXRD, SEM and FTIR indicated that Co Qu-Ma were successfully obtained through solvent evaporation method. The in-vitro dissolution rate of Co Qu-Ma was 95.30% at 60 min. Cocrystals effectively increased dissolution rate and dissolution efficiency in comparison to the pure quercetin and physical mixture of quercetin-malonic acid.

Keywords


quercetin; malonic acid; cocrystal; in vitro dissolution

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DOI: https://doi.org/10.22146/ijc.28511

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