Crystal Engineering of Quercetin by Liquid Assisted Grinding Method

Athiyah, Umi; Kusuma, Putu Andika; Tutik, Tutik; Lestari, Maria Lucia Ardhani Dwi; Isadiartuti, Dewi; Paramita, Diajeng Putri; Setyawan, Dwi

doi:10.11113/jt.v81.12639

Cited by 10 publications

(11 citation statements)

References 22 publications

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“…This is because drugs need to dissolve in the gastrointestinal tract's biological fluids in order to be absorbed and provide their pharmacological effects [1]. Therefore, drugs with low solubility and dissolution rates usually experience oral bioavailability problems which pose challenges to pharmaceutical development [2,3].…”

Section: Introductionmentioning

confidence: 99%

Preparation of Spray Dried Coamorphous Solids to Improve the Solubility and Dissolution Rate of Atorvastatin Calcium

et al. 2021

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Atorvastatin calcium (AC) is a statin drug used to lower cholesterol. Its crystalline form is usually found in the market with low solubility properties. The amorphization of crystalline AC is a technique used to increase its solubility however; the amorphous form has less thermodynamic stability. Therefore, to increase the solubility properties of its crystalline form, an AC coamorphous solid was prepared. This coamorphous solid was prepared using spray drying techniques, and coformers such as isonicotinamide (INA) and maleic acid (MA). Furthermore, characterization was carried out using powder X-ray diffraction, differential scanning calorimetry, fourier transform infrared spectroscopy, and scanning electron microscopy, while the solubility properties test was conducted using the shake-flask and paddle method. The results showed that the spray-dried solids were coamorphous with single-phase homogeneous systems. Furthermore, the coamorphous solids, AC-INA and AC-MA were found to have a higher Tg than the melting points of other components, and formed intermolecular interactions between them. The higher Tg and presence of intermolecular interactions indicate that coamorphous solids are more stable than the amorphous form. Therefore, the results of the solubility and dissolution test showed that the coamorphous solid of AC-INA and AC-MA have better solubility properties compared to the AC crystalline form.

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Section: Introductionmentioning

confidence: 99%

Preparation of Spray Dried Coamorphous Solids to Improve the Solubility and Dissolution Rate of Atorvastatin Calcium

et al. 2021

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“…Wet grinding (also known as liquid-assisted grinding) is a similar technique, but it requires an addition of small quantities of solvent that act as a catalyst in the formation of MCCs (Gadade and Pekamwar, 2016) . This is commonly used in producing MCCs of phytochemicals, such as cocrystals of QUE with succinic acid (Athiyah et al, 2019) . Another method is the hot melt extrusion method, in which MCCs are formed by inducing heat during the mixing of the APIs and coformers, replacing solvents in the role of decreasing surface tension, until the API and coformer form a liquid state (Boksa et al, 2014;Gajda et al, 2019;Savjani, 2015).…”

Section: Solid-based MCC Preparation Methodsmentioning

confidence: 99%

“…However, the clinical use of QUE is limited because of its extremely low solubility in water (0.3 µg/mL) (Setyawan et al, 2018) , reducing its bioavailability (Dian et al, 2014) . In addition, QUE reportedly has a very low oral absorption capacity (only 2%) and tends to be susceptible to metabolic conjugation (Athiyah et al, 2019) which might contribute to its low bioavailability. Several techniques for improving the solubility and stability of QUE, such as solid dispersions (Li et al, 2013;Setyawan et al, 2017), lm dispersions (Dian et al, 2014) , microparticles (Silva et al, 2013) , nanoparticles (Lee et al, 2016;Pal et al, 2013), inclusion complexes (Aytac et al, 2016) , emulsions (Chen et al, 2018) , and MCCs (Athiyah et al, 2019;Setyawan et al, 2018).…”

Section: Polar Compounds 431 Quercetin (Que)mentioning

confidence: 99%

“…Cocrystals of QUE with SA were prepared in 1:1 molar ratio using the grinding liquid-assisted method to observe the enhancement of QUE solubility and dissolution rate (Athiyah et al, 2019) . Apart from being classi ed as GRAS by the FDA, SA has potential H-bonding sites which are expected to be Hbond donors for two hydroxyls (-OH) groups in QUE with two carboxylic acids (-COOH) groups of SA.…”

Section: Polar Compounds 431 Quercetin (Que)mentioning

confidence: 99%

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Crystal Engineering Approach in Physicochemical Properties Modifications of Phytochemical

Lutfiyah

Fitriani

Taher

et al. 2022

Sci. Technol. Indones

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Phytochemicals have been used to reduce the risk of diseases and maintain good health and well-being. However, most phytochemicals have a limitation in their physicochemical properties, which can be modified by reforming the shape of the crystals. Therefore, crystal engineering is a promising approach to optimize physicochemical characteristics of the active pharmaceutical ingredients (APIs) in a phytochemical without altering its pharmacological efficacy. Hence, this paper reviews current strategies for the use of crystal engineering to optimize physicochemical properties of phytochemicals, which is followed by the design of the synthesis and characterization of particular phytochemicals, including piperine (PIP), quercetin (QUE), curcumin (CUR), genistein (GEN), and myricetin (MYR). The literature indicates that crystal engineering of multicomponent crystals (MCCs) enhances phytochemical physicochemical properties, including solubility, dissolution rate, stability, and permeability. The MCCs provide a lower lattice energy and noncovalent bonding, which translate into lower melting points and weak intermolecular interactions that generate greater solubility, higher dissolution rate, and better stability of the APIs. Nevertheless, the absence of reported studies of phytochemical crystal engineering leads to a lack of variation in the selection of coformers, methods of preparation, and improvement of physicochemical properties. Therefore, more extensive evaluation of the design and physicochemical characteristics of phytochemicals using MCCs is necessary and manifests the opportunity to enhance the application of phytochemicals in the pharmaceutical industry.

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“…However, we assume that decrease in peak intensity cannot be explained by dissociation phenomenon alone since dissociation is predicted to locally occur on the tablet surface. Inadequate amount of the starting components also explains why peak loss or change in diffraction profile is not observed when change in crystal lattice is supposed to occur [21].…”

Section: X-ray Diffractionmentioning

confidence: 99%

Compression force effect on characteristics of loratadine-succinic acid cocrystal prepared by slurry method

Setyawan¹,

Paramanandana²,

Erfadrin³

et al. 2020

jrp

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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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Crystal Engineering of Quercetin by Liquid Assisted Grinding Method

Cited by 10 publications

References 22 publications

Preparation of Spray Dried Coamorphous Solids to Improve the Solubility and Dissolution Rate of Atorvastatin Calcium

Preparation of Spray Dried Coamorphous Solids to Improve the Solubility and Dissolution Rate of Atorvastatin Calcium

Crystal Engineering Approach in Physicochemical Properties Modifications of Phytochemical

Compression force effect on characteristics of loratadine-succinic acid cocrystal prepared by slurry method

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