Solid-state interaction of ibuprofen with magnesium stearate and product characterization thereof

Pecova, Monika Stojanovska; Geškovski, Nikola; Petrushevski, Gjorgji; Chachorovska, Marina; Krsteska, Liljana; Ugarković, Sonja; Makreski, Petre

doi:10.1080/03639045.2020.1788067

Cited by 7 publications

(7 citation statements)

References 24 publications

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“…Surprisingly, FH, FI and FJ showed the highest solubility of IBF (247.2–252.8 µg/mL) among all formulations due to the presence of 2.5% MgSt. While MgSt disperses in basic conditions (PBS, pH 7.4) at a certain temperature and humidity, MgO from the MgSt reacts with carboxyl acid group from IBF, which might cause an acid–base reaction to form magnesium salt of ibuprofen [ 39 ]. This result significantly increased the drug solubility (at 24 h of mixing), which could be attributed to the improvement of the drug particle dispersion which helps in drug solubilization [ 40 ].…”

Section: Resultsmentioning

confidence: 99%

“…While MgSt is dispersed in basic conditions such as PBS, faster release or increase in the drug solubility at 24 h could be attributed to improvements in the drug particle dispersion which helped in solubilizing the drug [ 40 ]. MgSt might play an important role in enhancing the solubility and dissolution of IBF particles by forming a complex mixture of the drug, such as the Mg salt of IBF that dissociates in the solvent and improves the solubilization [ 39 ]. Additionally, faster drug release could be due to the presence of both excipients which reduced the particle–particle cohesion and increased the drug–solvent interactions, thus enhancing the solubility of IBF.…”

Section: Resultsmentioning

confidence: 99%

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Impact of Leucine and Magnesium Stearate on the Physicochemical Properties and Aerosolization Behavior of Wet Milled Inhalable Ibuprofen Microparticles for Developing Dry Powder Inhaler Formulation

et al. 2023

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This study investigated the development and characterization of leucine and magnesium stearate (MgSt) embedded wet milled inhalable ibuprofen (IBF) dry powder inhaler (DPI) formulations. IBF microparticles were prepared by a wet milling homogenization process and were characterized by SEM, FTIR, DSC, XRD and TGA. Using a Twin-Stage Impinger (TSI), the in vitro aerosolization of the formulations with and without carrier lactose was studied at a flow rate of 60± 5 L/min and the IBF was determined using a validated HPLC method. The flow properties were determined by the Carr’s Index (CI), Hausner Ratio (HR) and Angle of Repose (AR) of the milled IBF with 4–6.25% leucine and leucine containing formulations showed higher flow property than those of formulations without leucine. The fine particle fraction (FPF) of IBF from the prepared formulations was significantly (p = 0.000278) higher (37.1 ± 3.8%) compared to the original drug (FPF 3.7 ± 0.9%) owing to the presence of leucine, which enhanced the aerosolization of the milled IBF particles. Using quantitative phase analysis, the XPRD data revealed the crystallinity and accurate weight percentages of the milled IBF in the formulations. FTIR revealed no changes of the structural integrity of the milled IBF in presence of leucine or MgSt. The presence of 2.5% MgSt in the selected formulations produced the highest solubility (252.8 ± 0.6 µg/mL) of IBF compared to that of unmilled IBF (147.4 ± 1.6 µg/mL). The drug dissolution from all formulations containing 4–6.25% leucine showed 12.2–18.6% drug release in 2.5 min; however, 100% IBF dissolution occurred in 2 h whereas around 50% original and dry milled IBF dissolved in 2 h. The results indicated the successful preparation of inhalable IBF microparticles by the wet milling method and the developed DPI formulations with enhanced aerosolization and solubility due to the presence of leucine may be considered as future IBF formulations for inhalation.

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Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

Impact of Leucine and Magnesium Stearate on the Physicochemical Properties and Aerosolization Behavior of Wet Milled Inhalable Ibuprofen Microparticles for Developing Dry Powder Inhaler Formulation

et al. 2023

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“…This approach can be used to characterize the thermodynamic properties of the solid phase and screen for intermolecular interactions between two solids. 16 A binary phase diagram was constructed using DSC thermal analysis. The endothermic peaks for FA, NIC, and an FA-NIC binary mixture in various molar ratios were determined using a DSC apparatus (Fig.…”

Section: Resultsmentioning

confidence: 99%

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

2021

TJNPR

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“…starch paste) that can be contaminated if stored prior to utilization in production (22). Several studies have indicated incompatibilities between IBU and boundary lubricants, in terms of identified changes in crystallinity and formation of eutectic mixtures of IBU and excipients such as stearic acid and magnesium stearate (23)(24). Traditionally, IBU tablets are sugar (sucrose) coated in order to mask their unpleasant taste, as well as due to the acidity of IBU.…”

Section: Solid Dosage Formsmentioning

confidence: 99%

Application of text-mining techniques for extraction and analysis of paracetamol and ibuprofen marketed products' qualitative composition

Đuriš¹,

Pilović²,

Džunić³

et al. 2022

Arhiv za farmaciju

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Text mining (TM) applications in the field of biomedicine are gaining great interest. TM tools can facilitate formulation development by analyzing textual information from patent databases, scientific articles, summary of products characteristics, etc. The aim of this study was to utilize TM tools to perform qualitative analysis of paracetamol (PAR) and ibuprofen (IBU) formulations, in terms of identifying and evaluating the presence of excipients specific to the active pharmaceutical ingredient (API) and/or dosage form. A total of 152 products were analyzed. Web-scraping was used to retrieve the data, and Python-based open-source software Orange 3.31.1 was used for TM and statistical analysis (ANOVA) of the obtained results. The majority of marketed products for both APIs were tablets. The predominant excipients in all tablet formulations were povidone, starch, microcrystalline cellulose and hypromellose. Povidone, stearic acid, potassium sorbate, maize starch and pregelatinized starch occurred more frequently in PAR tablets. On the other hand, titanium dioxide, lactose, shellac, sucrose and ammonium hydroxide were specific to IBU tablets. PAR oral suspensions more frequently contained dispersible cellulose; liquid sorbitol; methyl and propyl parahydroxybenzoate, glycerol and acesulfame potassium. Specific excipients in other PAR dosage forms, such as effervescent tablets, hard capsules, oral powders, solutions and suspensions, as well as IBU gels and soft capsules, were also evaluated.

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Solid-state interaction of ibuprofen with magnesium stearate and product characterization thereof

Abstract: Figure S1. 2950 -2920 cm -1 IR spectral region (SNV normalized) colored according to the MgS content (a) and stress conditions (b) Figure S2. VIP plot of the DSC curves PLS model (a), DSC curves colored according to the MgS content (b) and stress conditions (c)

Cited by 7 publications

References 24 publications

Impact of Leucine and Magnesium Stearate on the Physicochemical Properties and Aerosolization Behavior of Wet Milled Inhalable Ibuprofen Microparticles for Developing Dry Powder Inhaler Formulation

Impact of Leucine and Magnesium Stearate on the Physicochemical Properties and Aerosolization Behavior of Wet Milled Inhalable Ibuprofen Microparticles for Developing Dry Powder Inhaler Formulation

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

Application of text-mining techniques for extraction and analysis of paracetamol and ibuprofen marketed products' qualitative composition

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