Co-Amorphization of Ibuprofen by Paracetamol for Improved Processability, Solubility, and In vitro Dissolution

Bhandari, Mayuri S.; Wairkar, Sarika; Patil, Udaykumar; Jadhav, Namdeo

doi:10.17344/acsi.2017.3822

Cited by 9 publications

(7 citation statements)

References 36 publications

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“…For these reasons, many research groups are interested in establishing solid dosage forms of IBU with improved solubility and bioavailability. Although, the use of solid dispersions (SDs) has been reported as an effective tool to enhance IBU solubility [23,24], the large quantity of polymer increases the bulk of the final dosage form, which limits the use of these formulations at the industrial scale [25]. The toxicity aspect was recognized as a limitation of ionic liquids [26] and self-assembled mixed micelles [27] were applied to improve its solubility.…”

Section: Resultsmentioning

confidence: 99%

A Novel Approach to Optimize Hot Melt Impregnation in Terms of Amorphization Efficiency

Garbera¹,

Ciura

Sawicki

2020

IJMS

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In this study, an innovative methodology to optimize amorphization during the hot melt impregnation (HMI) process was proposed. The novelty of this report revolves around the use of thermal analysis in combination with design of experiments (DoEs) to reduce residual crystallinity during the HMI process. As a model formulation, a mixture of ibuprofen (IBU) and Neusilin was used. The main aim of the study was to identify the critical process parameters of HMI and determine their optimal values to assure a robust impregnation process and possibly the highest possible amorphization rate of IBU. In order to realize this, a DoE approach was proposed based on a face-centered composite design involving three factors. The IBU/Neusilin ratio, the feeding rate, and the screw speed were considered as variables, while the residual crystallinity level of IBU, determined using differential scanning calorimetry (DSC), was measured as the response. Additionally, the stability of IBU under HMI was analyzed using high-performance liquid chromatography to estimate the extent of potential degradation. In order to verify the correctness of the DoE model, tested extrudates were manufactured by HMI and the obtained extrudates were thoroughly examined using scanning electron micrography, X-ray powder diffraction, and DSC.

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Section: Resultsmentioning

confidence: 99%

A Novel Approach to Optimize Hot Melt Impregnation in Terms of Amorphization Efficiency

Garbera¹,

Ciura

Sawicki

2020

IJMS

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“…Pyrogallol stabilizes 5-methyl-2-[(2-nitrophenyl)amino]-3-thiophenecarbonitrile (ROY) in a 1 : 1 ratio and was identified by using a cocrystal screening method suggesting a similar process could be used to screen for coamorphous phases [31]. A paracetamol-ibuprofen coamorphous system was formed via ball milling and it showed improved processability and solubility for ibuprofen compared to the original drug [195]. Similarly, small molecule lactam dimers can act as coformers for coamorphous phases.…”

Section: Small Molecule Coamorphous Materialsmentioning

confidence: 99%

Cocrystals, Coamorphous Phases and Coordination Complexes of γ‐ andε‐Lactams

Hall

Chambers

Musa

et al. 2021

Handbook of Pyrrolidone and Caprolactam Based Materials

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The strongly interacting lactam functional group in both γand ε-lactams makes them of considerable interest in the formation of multicomponent solids including a hugely diverse range of cocrystals, coordination complexes with lactam ligands and coamorphous phases. Cocrystals are structurally homogenous crystalline substances that are comprised of two or more chemically different neutral molecules generally in stoichiometric amounts that are connected by non-ionic and non-covalent interactions [1]. The Food and Drug Administration (FDA) classifies cocrystals as crystalline materials composed of two or more different molecules, typically Active Pharmaceutical Ingredients (API) and approved, non-toxic cocrystal former (coformer), in the same crystal lattice [2].Cocrystals fall under the umbrella of multi-component molecular solids, which encompasses crystalline forms such as solvates, hydrates, and lattice inclusion compounds as well as coamorphous materials. The relationships between these various solid forms are illustrated in Figure 1. Also included under multi-component crystalline solids are solid solutions in which one component is randomly distributed in a crystal of another [4]. Salts are also multi-component molecular solids, with the main difference between a salt and a cocrystal often being proton transfer from an acid to a base that occurs to give a salt in contrast to neutral molecule cocrystals. However, the distinction is a fine one since, depending on the temperature, salts and cocrystals can interconvert [5]. Generally, true cocrystals are regarded as being formed from components that are solids at room temperature, a definition which excludes solvates and hydrates. However, this narrowing would mean that some materials involving low melting solids might be regarded as cocrystals in some labs and not others despite that fact that there is no fundamental structural difference between a cocrystal and a solvate [1,6,7].

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“…The dialysis tube was placed in vessel containing 200 ml phosphate buffer (pH 7.4 at 34 ± 0.5 °C) under a paddle speed of 50 rpm. 23,24 Aliquot of 10 ml was drawn at particular time intervals and replaced with same volume of fresh medium. The absorbance was checked in a UV-Visible spectrophotometer (JASCO V-630 UV-Visible spectrophotometer) at 274 nm.…”

Section: In Vitro Drug Release Studymentioning

confidence: 99%

Influence of TiO2 on Mucosal Permeation of Aceclofenac: Analysis of Crystal Strain and Dislocation Density

Nandi¹,

Mishra²,

Sahoo³

et al. 2020

ACSi

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Titanium dioxide can adhere with human epithelial cells and have good tolerability. Present work has been undertaken to explore the influence of TiO2 on mucosal permeation of aceclofenac. Mucosal permeation of aeclofenac solution containing TiO2 has been carried out. In fourier transform infrared spectrosopy (FTIR), the intensity of the peaks has decreased along with the increase of TiO2 content in the formulation indicating a possible binding between drug and TiO2. Melting enthalpy has been decreased with the increased content of TiO2 in the solid. The status of crystal strain and dislocation density of TiO2 and aceclofenac in the solid state formulation has also been evaluated from Xray Diffraction data using Debye-Scherrer’s equation. Mucosal permeation of aceclofenac has shown sustained effect for more than 20 h in presence of titanium dioxide. Titanium dioxide could be used in designing formulation for sustaining mucosal aceclofenac delivery after performing risk assessment study.

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Co-Amorphization of Ibuprofen by Paracetamol for Improved Processability, Solubility, and In vitro Dissolution

Cited by 9 publications

References 36 publications

A Novel Approach to Optimize Hot Melt Impregnation in Terms of Amorphization Efficiency

A Novel Approach to Optimize Hot Melt Impregnation in Terms of Amorphization Efficiency

Cocrystals, Coamorphous Phases and Coordination Complexes of γ‐ andε‐Lactams

Influence of TiO2 on Mucosal Permeation of Aceclofenac: Analysis of Crystal Strain and Dislocation Density

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