Multicomponent solid forms of felodipine: preparation, characterisation, physicochemical and <i>in-vivo</i> studies

Chadha, Renu; Sharma, Mohit; Haneef, Jamshed

doi:10.1111/jphp.12685

Cited by 21 publications

(11 citation statements)

References 23 publications

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“…19,20) According to the survey of Schultheiss and Newman 51% cocrystals displayed melting points between those of the API and CCF. 21) Obviously, the screened FEL-βRA cocrystal contributed to this group. The hydrogen bond is an attractive interaction that presents in the cocrystal systems.…”

Section: Resultsmentioning

confidence: 99%

Spectroscopic Methodology and Molecular Docking Studies on Changes in Binding Interaction of Felodipine with Bovine Serum Albumin Induced by Cocrystallization with β-Resorcylic Acid

Zhou

et al. 2020

CHEMICAL & PHARMACEUTICAL BULLETIN

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In the present study, a novel cocrystal of felodipine (FEL) and β-resorcylic acid (βRA) was developed. We specially focused on the change of binding pattern with bovine serum albumin (BSA) induced by cocrystallization of FEL with βRA. The solid characterizations and density functional theory (DFT) simulation verified that FEL-βRA cocrystal formed in equimolar ratio (1 : 1 M ratio) through C O … H-O hydrogen bond between C O group in FEL and O-H group in βRA. The binding interactions between FEL-βRA system and BSA were studied using fluorescence spectral and molecular docking methods. Two guest molecule systems, including a physical mixture of FEL and βRA and FEL-βRA cocrystal were performed binding to BSA in molecular docking. According to the K b and binding energy, the supramolecular form of FEL-βRA system was retained during binding to BSA. Molecular docking simulation suggested that FEL and its cocrystal inserted into the subdomain IIIA (site II′) of BSA. The interactions between FEL and BSA including hydrogen bonding with ASN390 residue and intermolecular hydrophobic interactions with LEU429 and LEU452 residues. However, the size of supramolecular FEL-βRA better matched that of active cavity of BSA; the cocrystal is closely bound to BSA through hydrogen bonding with ASN390 residue and intermolecular hydrophobic interactions with LEU429, VAL432, LEU452 and ILE387 residues. This change on binding affinity of FEL to BSA induced by cocrystallization with βRA provided theoretical basis to evaluate the transportation, distribution and metabolism of cocrystal drug.

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Section: Resultsmentioning

confidence: 99%

Spectroscopic Methodology and Molecular Docking Studies on Changes in Binding Interaction of Felodipine with Bovine Serum Albumin Induced by Cocrystallization with β-Resorcylic Acid

Zhou

et al. 2020

CHEMICAL & PHARMACEUTICAL BULLETIN

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“…Nicotinamide has also been used as a hydrotropic agent to improve the solubility and dissolution rate for some poorly soluble drugs, such as efavirenz, ketoprofen, felodipine, and nimesulide. [13][14][15]24…”

Section: Resultsmentioning

confidence: 99%

Dissolution Rate Enhancement and Physicochemical Characterization of a Fenofibric Acid–Nicotinamide Eutectic Mixture

2021

TJNPR

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“…Also, PVP has been found to have a strong accelerating effect on the thermal decomposition of malonic acid (MA) . While not a drug, MA is used to make cocrystals with drugs as a way of improving the solubility of the latter. − Therefore, its interaction with PVP is still of pharmaceutical relevance. On the other hand, the thermal decomposition of MA is of general interest because it represents a wide class of decarboxylation reactions.…”

Section: Introductionmentioning

confidence: 99%

Accelerating Effect of Poly(vinylpyrrolidone) Matrix on Thermal Decomposition of Malonic Acid

Jelić

Liavitskaya

Paulechka³

et al. 2019

Ind. Eng. Chem. Res.

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Thermogravimetry in combination with isoconversional kinetic analysis is utilized to probe the effect of poly(vinylpyrrolidone) (PVP) on the decomposition of malonic acid (MA) in PVP matrices. The systems under study contain 4, 2, and 1 mol of PVP per 1 mol of MA. Although all systems demonstrate acceleration relative to neat MA, the strongest effect per mole of added PVP is observed in the 1:1 system. In the 4:1 system the acceleration effect weakens with the progress of decomposition and ultimately turns into deceleration. Kinetic analysis suggests that in the 1:1 and 2:1 systems, the decomposition rate at the advanced stages of the process is limited by vaporization of acetic acid. The unusual behavior of the 4:1 system at the advanced stages is proposed to be due to the decomposition rate being limited by a reversible step of dissolution of acetic acid in an excess of PVP.

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Multicomponent solid forms of felodipine: preparation, characterisation, physicochemical and in-vivo studies

Abstract: Mechanochemical approach was successful to prepare multicomponent solid forms that have the potential to improve biopharmaceutical parameters of the poorly soluble drug, FEL.

Cited by 21 publications

References 23 publications

Spectroscopic Methodology and Molecular Docking Studies on Changes in Binding Interaction of Felodipine with Bovine Serum Albumin Induced by Cocrystallization with β-Resorcylic Acid

Spectroscopic Methodology and Molecular Docking Studies on Changes in Binding Interaction of Felodipine with Bovine Serum Albumin Induced by Cocrystallization with β-Resorcylic Acid

Dissolution Rate Enhancement and Physicochemical Characterization of a Fenofibric Acid–Nicotinamide Eutectic Mixture

Accelerating Effect of Poly(vinylpyrrolidone) Matrix on Thermal Decomposition of Malonic Acid

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