Correlating Single Crystal Structure, Nanomechanical, and Bulk Compaction Behavior of Febuxostat Polymorphs

Yadav, Jayprakash Amarpal; Khomane, Kailas S.; Modi, Sameer R.; Ugale, Bharat; Yadav, Ram Naresh; Nagaraja, C. M.; Kumar, Navin; Bansal, Arvind K.

doi:10.1021/acs.molpharmaceut.6b01075

Cited by 50 publications

(52 citation statements)

References 35 publications

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“…Tabletability measures the capacity of powdered material to be transformed into tablets of specified strength under the effect of compression pressure [23,27]. The tabletability of a material is a function of its mechanical properties and is governed by the compressibility and compactibility of the material [28]. Tabletability profiles of formulations II & III granules, as seen in Fig.…”

Section: Compaction Propertiesmentioning

confidence: 99%

Quantifying the effect of glidant on the compaction and tableting properties of paracetamol granules

Apeji¹,

Olowosulu²

2020

jrp

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Glidants play a vital role in tablet formulation. This study aimed to examine the impact of glidants on the compaction and tableting properties of paracetamol granules prepared by wet granulation. Three formulations of paracetamol granules were prepared to consist of either talc, colloidal silicon dioxide (CSD) or a combination of both in equal proportion (1:1) as glidants added extragranularly. The granules were characterised by measuring the particle size, angle of repose, bulk and tapped densities, true densities, and moisture content. Compaction studies on the granules were carried out using the Heckel, Kawakita, Walker, and compressibility-tabletability-compactibility (CTC) models. Tablets were prepared from the granules for each formulation and evaluated according to USP requirements. The results of the granule analysis revealed that granule properties were similar across the formulations irrespective of the type of glidant used. Compaction studies revealed that talc granules exhibited a greater degree of plasticity and compressibility compared to the other formulations. However, CSD granules and granules containing the two glidants in equal proportion were found to have better compactibility and tabletability, resulting in tablets with relatively better properties. This study has underscored the impact of glidants on the compaction and tableting properties of paracetamol granules.

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Section: Compaction Propertiesmentioning

confidence: 99%

Quantifying the effect of glidant on the compaction and tableting properties of paracetamol granules

Apeji¹,

Olowosulu²

2020

jrp

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“…Tabletability is the capacity of a powdered material to be transformed into a tablet of specified strength under the effect of compaction pressure (Ghori and Conway, 2016;Joiris et al, 1998;Upadhyay et al, 2013;Yadav et al, 2017). It is represented by a plot of tensile strength against compaction pressure (Fig.…”

Section: Fig 5 Ctc Plots For Sas-cd Sas-cf and Sas-cg (A) Compresmentioning

confidence: 99%

Comparative analysis of co-processed starches prepared by three different methods

Apeji¹,

Aluga²,

Olayemi³

et al. 2017

British Journal of Pharmacy

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Co-processing is currently of interest in the generation of high-functionality excipients for tablet formulation. In the present study, comparative analysis of the powder and tableting properties of three co-processed starches prepared by three different methods was carried out. The co-processed excipients consisting of maize starch (90%), acacia gum (7.5%) and colloidal silicon dioxide (2.5%) were prepared by co-dispersion (SAS-CD), co-fusion (SAS-CF) and co-granulation (SAS-CG). Powder properties of each co-processed excipient were characterized by measuring particle size, flow indices, particle density, dilution potential and lubricant sensitivity ratio. Heckel and Walker models were used to evaluate the compaction behaviour of the three co-processed starches. Tablets were produced with paracetamol as the model drug by direct compression on an eccentric Tablet Press fitted with 12 mm flat-faced punches and compressed at 216 MPa. The tablets were stored at room temperature for 24 h prior to evaluation. The results revealed that cogranulated co-processed excipient (SAS-CG) gave relatively better properties in terms of flow, compressibility, dilution potential, deformation, disintegration, crushing strength and friability. This study has shown that the method of coprocessing influences the powder and tableting properties of the co-processed excipient.

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“…FEB is classified as a BCS II drug due to its low solubility (12.9 mg/L) and high permeability [14]. In recent years, several FEB polymorphs [15], solvates [16][17][18], cocrystals [19,20], and salts [21,22] have been reported. All salts feature increased dissolution rates and enhanced solubility compared with FEB.…”

Section: Introductionmentioning

confidence: 99%

Febuxostat-Minoxidil Salt Solvates: Crystal Structures, Characterization, Interconversion and Solubility Performance

et al. 2018

Crystals

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Three febuxostat-minoxidil salt solvates with acetone (ACE), tetrahydrofuran (THF) and isopropanol (IPA) are synthesized by solvent-assisted grinding and characterized by infrared (IR), nuclear magnetic resonance ( 1 H-NMR), single crystal and powder X-ray diffraction (PXRD), thermogravimetry (TG) and differential scanning calorimetry (DSC). These febuxostat-minoxidil salt solvates feature isostructural with the same stoichiometries (1:1:1 molecule ratio). The proton transfers from the carboxylic group of febuxostat (FEB) to imino N atom of minoxidil (MIN), which forms the motif with combined R 2 2 (9) R 2 4 (8) R 2 2 (9) graph set in the three solvates. The solvents occupy the different positions related to the motif, which results in the apparent differences in PXRD patterns before/after desolvation although they are isostructures. The FEB-MIN·THF was more thermostable than FEB-MIN·ACE and FEB-MIN·IPA relative to solvent removal from DSC patterns, which is different from the results from the solvent-exchange experiments in chemical kinetics. All three salt solvates exhibit increased equilibrium solubility compared to FEB in aqueous medium.

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Correlating Single Crystal Structure, Nanomechanical, and Bulk Compaction Behavior of Febuxostat Polymorphs

Cited by 50 publications

References 35 publications

Quantifying the effect of glidant on the compaction and tableting properties of paracetamol granules

Quantifying the effect of glidant on the compaction and tableting properties of paracetamol granules

Comparative analysis of co-processed starches prepared by three different methods

Febuxostat-Minoxidil Salt Solvates: Crystal Structures, Characterization, Interconversion and Solubility Performance

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