Ibuprofen Research Articles

Evaluation of physical and chemical modifications to drug reservoirs for stimuli-responsive microneedles.

Hydrogel-forming microneedle (MN) arrays are minimally-invasive devices that can penetrate the stratum corneum, the main barrier to topical drug application, without causing pain. However, drug delivery using hydrogel-forming MN arrays tends to be relatively slow compared to rapid drug delivery using conventional needles and syringes. Therefore, in this work, for the first time, different physical and chemical delivery enhancement methods were employed in combination with PVA-based hydrogel-forming MN arrays. Using a model drug, ibuprofen (IBU) sodium, the designed systems were assessed in terms of the extent of transdermal delivery. Iontophoresis (ITP) and heat-assisted drug delivery technology were investigated as physical permeation enhancement techniques. Ex vivo studies demonstrated that the ITP (0.5mA/cm2)-mediated combination strategy significantly enhanced the transdermal permeation of IBU sodium over the first 6h (~ 5.11mg) when compared to MN alone (~ 1.63mg) (p < 0.05). In contrast, heat-assisted technology showed almost no promoting effect on transdermal delivery. Furthermore, IBU sodium-containing rapidly dissolving lyophilised and effervescent reservoirs, classified as chemical modification methods, were prepared. Both strategies achieved rapid and effective ex vivo IBU sodium permeation, equating to ~ 78% (30.66mg) and ~ 71% (28.43mg) from lyophilised and effervescent reservoirs, respectively. Moreover, in vivo pharmacokinetic studies showed that the IBU sodium plasma concentration within lyophilised and effervescent groups reached a maximum concentration (Cmax) at 4h (~ 282.15µg/mL) and 6h (~ 140.81µg/mL), respectively. These strategies not only provided rapid achievement of therapeutic levels (10-15µg/ml), but also resulted in sustained release of IBU sodium for at least 48h, which could effectively reduce the frequency of administration, thereby improving patient compliance and reducing side effects of IBU sodium.

Distribution and ecological risks of pharmaceuticals and personal care products with different anthropogenic pressures in typical watersheds in China.

Due to global population growth and increased healthcare accessibility, pharmaceuticals and personal care products (PPCPs) are closely linked with human activities and have become new pollutants alongside some legacy priority pollutants, such as polycyclic aromatic hydrocarbons (PAHs). Although PPCPs have been detected in numerous river basins in recent years, a few researches have been carried out on their association with human activities. In this paper, the concentrations of PPCPs and toxicological data were compiled for over 25 representative watersheds in China in the past two decades from various sources, including PubMed, Elsevier and Springer. Comprehensive analysis of the occurrence, spatial distribution, sources and ecological risk assessment was carried out for the 30 most frequently detected PPCPs in water environments. Multivariate statistical methods, including hierarchical cluster analysis (HCA), principal component analysis (PCA) and redundancy analysis (RDA), were employed to classify PPCPs and assess their relationship with human activities. The results indicated that the concentrations of PPCPs in rivers varied significantly across studied regions, ranging from non-detect to 21,885 ng/L. Many detected compounds in PPCPs were antibiotics and their occurrence was closely linked with the economic development, effectiveness of medicines and geographical location. Household emissions were identified as the primary contributor to the occurrence of PPCPs in river basins. A strong correlation has been observed between PPCPs level and socio-economic indicators from multivariate statistical analysis. Ecological risk assessment revealed that caffeine (CAF), ibuprofen (IBU) and anhydroerythromycin (ERY) pose the greatest threat to aquatic life, particularly in the Northern China. The data compiled in this study provide insights into the impacts of PPCPs and the relationship of their ecological risks with various human activities, particularly in the typical Chinese river basins. Our results are valuable for the effective management PPCPs.

Comprehensive In Vitro and In Silico Aerodynamic Analysis of High-Dose Ibuprofen- and Mannitol-Containing Dry Powder Inhalers for the Treatment of Cystic Fibrosis.

Background: Cystic fibrosis is a hereditary disease, which causes the accumulation of dense mucus in the lungs accompanied by frequent local inflammation. The non-steroidal anti-inflammatory drug ibuprofen (IBU) and the mucolytic mannitol (MAN) can treat these symptoms. Compared to per os administration, a lower dose of these drugs is sufficient to achieve the desired effect by delivering them in a pulmonary manner. However, it is still a challenge to administer high drug doses to the lungs. We aim to develop two inhaled powder formulations, a single-drug product of MAN and a combined formulation containing IBU and MAN. Methods: MAN was dissolved in an aqueous solution of Poloxamer-188 (POL). In the case of the combined formulation, a suspension was first prepared in a planetary mill via wet milling in POL medium. After the addition of leucine (LEU), the formulations were spray-dried. The prepared DPI samples were analyzed by using laser diffraction, scanning electron microscopy, powder X-ray diffraction, differential scanning calorimetry, density tests, in vitro aerodynamic studies (Andersen Cascade Impactor, Spraytec® device), in vitro dissolution tests in artificial lung fluid, and in silico tests with stochastic lung model. Results: The DPIs showed suitability for inhalation with low-density spherical particles of appropriate size. The LEU-containing systems were characterized by high lung deposition and adequate aerodynamic diameter. The amorphization during the procedures resulted in rapid drug release. Conclusions: We have successfully produced a single-drug formulation and an innovative combination formulation, which could provide complex treatment for patients with cystic fibrosis to improve their quality of life.

Thermoanalytical and Kinetic Studies for the Thermal Stability of Emerging Pharmaceutical Pollutants Under Different Heating Rates.

Emerging pharmaceutical pollutants like ciprofloxacin (CIP) and ibuprofen (IBU) are frequently detected in aquatic environments, posing risks to ecosystems and human health. Since pollutants rarely exist alone in the environment, understanding the thermal stability and degradation kinetics of these compounds, especially in mixtures, is crucial for developing effective removal strategies. This study therefore investigates the thermal stability and degradation kinetics of CIP and IBU, under different heating rates. Thermogravimetric analysis (TGA) and differential thermal analysis (DTA) were employed to examine the thermal behavior of these compounds individually and in mixture (CIP + IBU) at heating rates of 10, 20, and 30 °C/min. The kinetics of thermal degradation were analyzed using both model-fitting (Coats-Redfern (CR)) and model-free (Kissinger-Akahira-Sunose (KAS), Flynn-Wall-Ozawa (FWO), and Friedman (FR)) methods. The results showed distinct degradation patterns, with CIP decomposing between 280 and 550 °C and IBU between 152 and 350 °C, while the mixture exhibited multistep decomposition in the 157-500 °C range. The CR model indicated first-order kinetics as a better fit for the degradation (except for IBU). Furthermore, CIP exhibits higher thermal stability and activation energy compared to IBU, with the KAS model yielding activation energies of 58.09 kJ/mol for CIP, 11.37 kJ/mol for IBU, and 41.09 kJ/mol for CIP + IBU mixture. The CIP + IBU mixture generally showed intermediate thermal properties, suggesting synergistic and antagonistic interactions between the compounds. Thermodynamic parameters (ΔH°, ΔG°, ΔS°) were calculated, revealing non-spontaneous, endothermic processes for all samples (except in the FWO method) with a decrease in molecular disorder and positive ΔG° values across all models and heating rates. The study found that higher heating rates led to less thermodynamically favorable conditions for degradation. These findings provide important information concerning the thermal behavior of these pharmaceutical pollutants, which can inform strategies for their removal from the environment and the development of more effective waste-treatment processes.

Cryostructuring of Polymeric Systems: 68. Evaluation of Poly(vinyl alcohol) Composite Cryogels Filled with Poly(3-hydroxybutyric acid)-Based Microspheres of Different Porous Morphology as Potential Delivery Systems for Drugs of Various Water-Solubility.

Poly(3-hydroxybutyric acid)-based microspheres of two types, with and without macropores, were prepared; their morphology and particle size were evaluated. These microspheres were entrapped as disperse fillers into the bulk of macroporous cryogels based on poly(vinyl alcohol) (PVA). It was found that the rigidity of the resultant composite cryogels increased markedly as compared to that of unfilled cryogels of the same PVA concentration. The resulting composites were further tested for their potential to act as drug carriers. With that, simvastatin was included into the filler particles directly in the course of their preparation, followed by entrapment of such drug-loaded microspheres into the PVA cryogel. In turn, ibuprofen sodium salt was introduced into the preliminary prepared cryogels filled with the drug-free microspheres. The experimental study of drug release kinetics showed that due to the non-covalent interactions of both simvastatin and ibuprofen sodium salt with the particles of discrete phase, prolongation of the release processes was observed.

Zeolites – tabletting ibuprofen with and without zeolites as an excipient

Abstract Introduction Drug delivery via the oral route is a patient and industry-preferred approach. However, maintaining plasma concentrations of the active pharmaceutical ingredient (API) within the therapeutic window can be challenging with immediate-release (IR) tablets. To avoid the plasma peaks and troughs associated with IR tablets, sustained release (SR) formulations have been investigated. Zeolites are microporous aluminosilicate minerals that represent a novel tabletting material with the potential for modifying drug release due to their unique adsorption and ion exchange properties1. Aim This study will investigate the potential for inclusion of zeolites within orally disintegrating tablets (ODTs) and assessment of their ability to modify API release. Methods In-house, 50%w/w ibuprofen (IBU)-loaded ODTs (IHODTs) were prepared from Pearlitol® Flash, magnesium (Mg) stearate and 2 different zeolites (CP814C and CP814E), incorporated at 5%w/w each, using a manual tablet press. Formulations were prepared and mixed for 10 minutes in a cube mixer prior to direct compression (DC) into tablets. Physical characteristics of the tablets were assessed by hardness and friability measurements. Tablet quality was assessed by disintegration and dissolution analysis to British Pharmacopeia (BP) standards2. Release profiles were assessed against various models to determine the effect of zeolites on the release of IBU. Formulations were further examined and characterised using scanning electron microscopy (SEM) and energy-dispersive x-ray (EDX) spectroscopy. An ethics evaluation was completed, and the study was identified as not having any ethical considerations by the University of South Wales. Results The mean weight of blank ODTs was found to be 225.3mg, with a mean thickness of 3.65mm, diameter of 8.10mm, hardness of 43.9±9.2N (mean±SD, n=5) and friability of 0.2±0.2% (mean±SD, n=3). The hardness of IHODTs was found to be 59.98±1.6N, reducing to 54.9±4.3N and 43.4±0.7N (mean±SD, n=3) with the inclusion of CP814C and CP814E, respectively. The friability of IHODTs containing zeolites was 1.76±0.4% and 1.91±0.9N (mean±SD, n=3), for CP814C and CP814E, respectively; conforming to BP specification2. The disintegration time for all in-house tablets, both with and without a zeolite included, was found to be an order of magnitude greater than commercial ODTs (CT) controls, but all remained within the BP specification2. The release of IBU from IHODTs and CTs showed good correlation to the first-order release model (R2 = 0.96 and 0.98, respectively), indicating IR behaviour. Similarly, the release of IBU from IHODTs containing zeolites was shown to correlate best with the first-order release model, R2 = 0.91 for CP814C and R2 = 0.90 for CP814E, respectively. SEM analysis suggested a homogeneous blend of components within IHODTs, whilst EDX analysis indicated the presence of silicon and aluminium from zeolites, and Mg and carbon from Mg stearate and IBU, respectively. Discussion / Conclusion This study investigated the effect of zeolite inclusion on the release properties of ODTs containing IBU. Although the quality of ODTs containing zeolites was not compromised, this study suggests that inclusion of a zeolite by DC only, does not significantly modify the release profile. Future studies are required to ascertain whether zeolites can achieve SR from ODTs using alternative API loading approaches, such as solvent loading1.

Efficient Loading into and Controlled Release of Lipophilic Compound from Liposomes by Using Cyclodextrin as Novel Trapping Agent.

Lipid bilayer vesicles, liposomes are representative drug delivery carriers. High encapsulation efficiency and release control of drugs are essential for clinical application of liposomes. For efficient drug loading into liposomes, remote loading method using driving force like transmembrane gradients of pH and ions are utilized. Ions are called as "trapping agents," which are also critical for the controlled release of drugs loaded into liposomes inside. It is difficult to apply ions as trapping agents to various drugs because of limited physicochemical compatibility between drugs and ions. Cyclodextrins (CDs) with hydrophobic cavity can make inclusion complexes with various hydrophobic compounds. Therefore, we aimed to evaluate the potential of CDs as a novel trapping agent using sulfobutylether-β-cyclodextrin (SBE-β-CD) and ibuprofen (IB), a weak acid hydrophobic drug. Encapsulation efficiency of IB in liposomes with pH gradient was approximately 27%, and it was enhanced by intraliposomal SBE-β-CD inclusion in addition to pH gradient, which was SBE-β-CD concentration-dependent. In liposomes with pH gradient, a large fraction of IB was released in a short time. This early-stage rapid IB release was significantly suppressed by the inclusion of SBE-β-CD inside liposomes. Thus, novel remote loading technology by intraliposomal SBE-β-CD enabled the efficient encapsulation of the hydrophobic drug into the aqueous phase of liposomes as well as their controlled release. This technology should be applied to various drugs that can be included into CDs in order to enhance their therapeutic benefits.

Oxygen Vacancies and Lattice Distortion Synergistically Enhanced Piezocatalysis of CaZn2(BO3)2 for Nonantibiotic Pharmaceutical Degradation.

Piezocatalysis, an emerging green and advanced oxidation technology, has recently been widely researched in environmental treatment. However, the limited polarization efficiency of the piezocatalyst is a serious bottleneck for its practical application. The search for an excellent piezocatalyst with a high piezoelectric coefficient and abundant reactive sites remains an urgent task that needs to be developed. Herein, a piezocatalyst, CaZn2(BO3)2 (CZBO), obtained by quenching has an excellent piezocatalysis, which exhibited superior activity for ibuprofen (IBP) and carbamazepine (CBZ) removal with 100% and 83.8% efficiency under ultrasonic cavitation (120 W, 40 kHz) within 36 min, respectively. The outstanding piezocatalytic degradation was attributed to the strong polarization of the material under the synergistic effect of oxygen vacancies (OVs) and lattice distortion, which effectively facilitated the generation of a high concentration of reactive oxygen species (ROS). The lattice distortion induced by O-deficient [BO3] plane units can promote the e- and h+ pair separation and transportation, and the OVs with abundant electron-rich regions can significantly decrease O-O bond activation energy, thus collaboratively contributing to the high production of ROS for IBP and CBZ degradation. This work provides a simple avenue for enhancing piezoelectric polarization based on the OVs and lattice distortion and proposes insights into the reaction mechanisms for degrading nonantibiotic pharmaceuticals in wastewater.

Novel Carbon@BaMoZrFe12O19 photocatalytic peroxymonosulfate activation for ibuprofen removal

This study reports a successful synthesis of a novel Carbon@BaMoZrFe12O19 Mhexaferrite photocatalyst (NPs) using the coprecipitation method. Afterthat, the NPs were used as an activator for peroxymonosulfate (PMS) to remove ibuprofen (IBU) from water. NPs were subjected for a thorough characterization process utilizing various analytical techniques including XRD, FTIR, UV, PL TEM, SEM/EDS, and X-ray photoelectron spectroscopy (XPS). Significantly, the utilization of NPs for PMS activation demonstrated a notable improvement in the elimination of IBU under visible light. The research conducted a thorough investigation into the effects of various parameters, such as activating systems, initial pH, inorganic salts, IBU contents, and water matrix on the efficiency of IBU degradation. The significance of reactive oxygen species, such as sulfate and hydroxyl radicals, as well as singlet oxygen, in the removal of IBU, was clarified by chemical quenching tests. In addition, NPs exhibited competent magnetic separation and reprocessing capacities. The magnetic NPs revealed excellent constancy and recyclability, by sustaining degrading productivity after five consecutive cycles. Therefore, the present study offers a significant contributions to the understanding of photocatalytic degradation for organic pollutants through the utilization of magnetic photocatalysts.

Heterogeneous Catalytic Ozonation of Pharmaceuticals: Optimization of the Process by Response Surface Methodology.

Batch heterogeneous catalytic ozonation experiments were performed using commercial and synthesized nanoparticles as catalysts in aqueous ozone. The transferred ozone dose (TOD) ranged from 0 to 150 μM, and nanoparticles were added in concentrations between 0 and 1.5 g L-1, with all experiments conducted at 20 °C and a total volume of 240 mL. A Ce-doped TiO2 catalyst (1% molar ratio of Ce/Ti) was synthesized via the sol-gel method. Response surface methodology (RSM) was applied to identify the most significant factors affecting the removal of selected pharmaceuticals, with TOD emerging as the most critical variable. Higher TOD resulted in greater removal efficiencies. Furthermore, it was found that the commercially available metal oxides α-Al2O3, Mn2O3, TiO2, and CeO2, as well as the synthesized CeTiOx, did not increase the catalytic activity of ozone during the degradation of ibuprofen (IBF) and para-chlorobenzoic acid (pCBA). Carbamazepine (CBZ) and diclofenac (DCF) are compounds susceptible to ozone oxidation, thus their complete degradation at 150 μM transferred ozone dose was attained. The limited catalytic effect was attributed to the rapid consumption of ozone within the first minute of reaction, as well as the saturation of catalyst active sites by water molecules, which inhibited effective ozone adsorption and subsequent hydroxyl radical generation (●OH).

Customizable Self-Microemulsifying Rectal Suppositories by Semisolid Extrusion 3D Printing.

Objectives: This study aims to create an innovative self-microemulsifying drug delivery system (SMEDDS) suppository for ibuprofen (IBU) using semisolid extrusion (SSE) three-dimensional (3D) printing technology. Methods: Based on solubility studies and the ability to form a transparent microemulsion upon dilution, a selected oil, surfactant, and co-surfactant were utilized to prepare SMEDDS-3DPS containing IBU. The optimal formulation consisted of 10% Triacetin, 80% Gelucire 48/16, and 10% Tetraethylene glycol. SSE 3D printing was employed to create three different-sized suppositories with varying drug contents. These suppositories were assessed for their physicochemical properties, content uniformity, and dissolution profiles. Results: The prepared mixture exhibited suitable physical properties for printing, with nano-sized emulsion droplets providing a large surface area for improved drug absorption in the rectum. Characterization techniques such as differential scanning calorimetry, powder X-ray diffraction, and Fourier transform infrared spectroscopy indicated that IBU was present in the formulation in an amorphous state. Additionally, in vitro dissolution tests demonstrated that SMEDDS-3DPS had a significantly higher initial dissolution rate compared with IBU powder. Conclusions: This research suggests that SMEDDS-3DPS, as a rectal IBU dosage form, can enhance the rectal bioavailability of IBU. It demonstrates the versatility of 3D printing as a novel manufacturing method for lipid-based suppositories and highlights the simplicity and adaptability of SSE 3D printing technology in producing customized suppositories tailored to individual patient needs, surpassing traditional methods.

Preparation of Ibuprofen-Loaded Inhalable γCD-MOFs by Freeze-Drying Using the QbD Approach.

Research on cyclodextrin-based metal-organic frameworks (CD-MOFs) is still in its infancy, but their potential for use in drug delivery-expressly in the lung-seems promising. We aimed to use the freeze-drying method to create a novel approach for preparing CD-MOFs. MOFs consisting of γ-cyclodextrin (γCD) and potassium cations (K+) were employed to encapsulate the poorly water-soluble model drug Ibuprofen (IBU) for the treatment of cystic fibrosis (CF). Using the LeanQbD® software (v2022), we designed the experiments based on the Quality by Design (QbD) concept. According to QbD, we identified the three most critical factors, which were the molar ratio of the IBU to the γCD, incubation time, and the percentage of the organic solvent. light-, scanning electron microscope (SEM) and laser diffraction were utilized to observe the morphology and particle size of the samples. In addition, the products were characterized by Differential Scanning Calorimetry (DSC), X-ray Powder Diffraction (XRPD), Fourier Transform Infrared Spectroscopy (FT-IR) and nuclear magnetic resonance spectroscopy (NMR). Based on characterizations, we concluded that a γCD-MOF/IBU complex was also formed using the freeze-drying method. Using formulations with optimal aerodynamic properties, we achieved 38.10 ± 5.06 and 47.18 ± 4.18 Fine Particle Fraction% (FPF%) based on the Andersen Cascade Impactor measurement. With these formulations, we achieved a fast dissolution profile and increased IBU solubility. This research successfully demonstrates the innovative use of freeze-drying to produce γCD-MOFs for inhalable IBU delivery. The method enabled to modify the particle size, which was crucial for successful pulmonary intake, emphasizing the need for further investigation of these formulations as effective delivery systems.

Selective O2-to-H2O2 Electrosynthesis by a High-Performance, Single-Pass Electrofiltration System Using Ibuprofen-Laden CNT Membranes.

Producing H2O2 through a selective, two-electron (2e) oxygen reduction reaction (ORR) is challenging, especially when it serves as an advanced oxidation process (AOP) for cost-effective water decontamination. Herein, we attain a 2e-selectivity H2O2 production using a carbon nanotube electrified membrane with ibuprofen (IBU) molecules laden (IBU@CNT-EM) in an ultrafast, single-pass electrofiltration process. The IBU@CNT-EM can generate H2O2 at a rate of 25.62 mol gCNT-1 h-1 L-1 in the permeate with a residence time of 1.81 s. We demonstrated that an interwoven, hydrophilic-hydrophobic membrane nanostructure offers an excellent air-to-water transport platform for ORR acceleration. The electron transfer number of the ORR for IBU@CNT at neutral pH was confirmed as 2.71, elucidating a near-2e selectivity to H2O2. Density functional theory (DFT) studies validated an exceptional charge distribution of the IBU@CNT for the O2 adsorption. The adsorption energies of the O2 and *OOH intermediates are proportional to the H2O2 selectivity (64.39%), higher than that of the CNT (37.81%). With the simple and durable production of H2O2 by IBU@CNT-EM electrofiltration, the permeate can actuate Fenton oxidation to efficiently decompose emerging pollutants and inactivate bacteria. Our study introduces a new paradigm for developing high-performance H2O2-production membranes for water treatment by reusing environmental functional materials.

Comprehensive evaluation of ibuprofenate amino acid isopropyl esters: insights into antioxidant activity, cytocompatibility, and cyclooxygenase inhibitory potential

Nonsteroidal anti-inflammatory drugs (NSAIDs) are widely used for pain relief and inflammation management, but there are challenges related to poor solubility and bioavailability. We explored modifications of ibuprofen (IBU) by forming ionic pairs using amino acid alkyl esters to enhance solubility without compromising the ability to inhibit cyclooxygenase (COX)-1 and COX-2). We comprehensively evaluated the pharmacological properties of the IBU derivatives, focusing on antioxidant activity (based on the ability to scavenge DPPH and ABTS), biocompatibility (using human dermal fibroblasts), and COX inhibitory potential. The antioxidant activity assays significantly enhanced DPPH scavenging activity for several IBU derivatives, particularly [l-SerOiPr][IBU], suggesting potential therapeutic benefits. There was enhanced cell viability with select derivatives, indicating possible stimulatory effects on cellular proliferation. Finally, predominant COX-1 inhibition across derivatives was consistent with IBU’s profile. This study provides insights into the pharmacological properties of IBU amino acid derivatives, highlighting their potential as therapeutic agents. Further exploration into structure–activity relationships and in vivo efficacy warranted to advance these derivatives toward clinical applications, offering prospects for novel NSAIDs with enhanced efficacy and reduced side effects.

Removal of Ibuprofen from Aqueous Solutions by Using Graphene Oxide@MgO

In this study, a new composite adsorbent, namely magnesium oxide modified graphene oxide (hereafter abbreviated GO@MgO), was prepared for the removal of Ibuprofen (IBU), a non-steroidal anti-inflammatory drug (NSAID) compound. Graphene oxide was modified with MgO to improve its properties. Several factors important for the evolution of the adsorption process were investigated, such as the dose of the adsorbent, the pH, and the initial IBU content, as well as the duration of the procedure and temperature. According to the results obtained, it was found that at pH 3.0 ± 0.1, by applying 0.5 g/L GO@MgO to 100 mg/L IBU, more than 80% was removed, reaching 96.3% with the addition of 1.5 g/L adsorbent in 24 h. After 30 min, the equilibrium was reached (77% removal) by adding 0.5 g/L of GO@MgO. This study proves that GO@MgO is capable of economical and efficient adsorption. The IBU kinetic data followed the pseudo-second-order kinetic model. Langmuir and Freundlich isotherm models were used to interpret the adsorption, but the Freundlich model described the adsorption method more accurately. The positive values of ΔH0 (14.465 kJ/mol) confirm the endothermic nature of the adsorption. Due to the increase of ΔG0 values with temperature, the adsorption of IBU on GO@MgO is considered to be spontaneous.

High throughput and cost-effective purification of small molecules using superficially porous stationary phase columns: An environment friendly approach

Over the past two decades, higher efficiencies have become the goal of most research organizations, and more so for high throughput synthesis. Consequently, there is an urgent need for an advanced purification approach to accommodate the large number of small molecules in a shorter turnaround time. To address this, an efficient and high throughput purification method was developed leveraging the superficially porous particle (SPP) column technology, which was optimized with respect to detector acquisition rate, flow rate, and gradient time. The experiments were performed using a sample mixture of six commercially available small molecules including Nicotinamide (NIC), 4-Amino benzophenone (ABP), Praziquantel (PRA), butyl‑4-hydroxybenzoate (BHB), Warfarin sodium (WAR), and Ibuprofen (IBU). The study outcomes were promising and exhibited a good separation of all six analytes with ∼83 % less turnaround time and ∼65 % less solvent consumption than the regular methods. Furthermore, it showed significant improvement in peak symmetry, capacity factor, and resolution for all six analytes and afforded superior chromatographic performance than the regular method with fully porous particle (FPP) columns. The study concludes that SPP columns provide cost-effective, eco-friendly, and high throughput purification of small molecules.

Core-shell tablets designed for modified and sequential release of ibuprofen and rabeprazole

In this study, core–shell tablets comprising an ibuprofen (IBU) enteric-coated core for modified release and a rabeprazole (RAB) shell for immediate release were developed using wet granulation method. The primary aim was to produce a sequential release of RAB and IBU with pharmacokinetic profiles comparable to those of the respective single tablets, thereby reducing the potential for IBU-associated gastrointestinal (GI) side effects. The composition of the IBU/RAB core–shell tablets was finalized on a comparative basis by evaluating various trial formulations. IBU/RAB core–shell tablets (400/20 mg) were assessed for physicochemical attributes, storage stability, and in vivo pharmacokinetics in beagle dogs. IBU/RAB core–shell tablets showed immediate RAB release (99.5 % in 1 h at pH 1.2) and delayed IBU release (3.4 % and 88 % in the acid and buffer stages, respectively). IBU/RAB core–shell tablets produced either comparable or improved plasma concentrations in dogs (Cmax; 1163.3 vs. 1160.0 ng/mL for RAB and 27,370 vs. 24,170 ng/mL for IBU) compared to those of the respective single tablets. The IBU/RAB core–shell tablets also demonstrated long-term and accelerated storage stability. In conclusion, the core–shell design could be a promising strategy for the co-administration and sequential release of IBU and RAB to relieve inflammatory conditions and reduce GI complications.

Material-Sparing Approach to Predict Tablet Capping Under Processing Compression Conditions Based on Mechanical and Molecular Properties Derived from Compaction Simulation and Crystal Structural Analysis.

Present study evaluates the usability of compaction simulation-based mechanical models as a material-sparing approach to predict tablet capping under processing compression conditions using Acetaminophen (APAP) and Ibuprofen (IBU). Measured mechanical properties were evaluated using principal component analysis (PCA) and principal component regression (PCR) models. PCR models were then utilized to predict the capping score (CS) from compression pressure (CP). APAP formulations displayed a quadratic correlation between CS and CP, with CS rank order following CP of 200MPa < 300MPa < 100MPa, indicating threshold compression pressure (TCP) limit between 200 and 300 MPa, resulting in higher CS at 300 than 200 MPa regardless of increased CP. IBU formulations displayed a linear correlation between CS and CP, with CS rank order following CP of 100MPa < 200MPa < 300MPa, indicating TCP limit between 100 and 200 MPa, resulting in higher CS at 200 and 300 than 100 MPa regardless of increased CP. Molecular models were developed as validation methods to predict capping from CP. Measured XRPD patterns of compressed tablets were linked with calculated Eatt and d-spacing of slip planes and analyzed using variable component least square methods to predict TCP triggering cleavage in slip planes and leading to capping. In APAP and IBU, TCP values were predicted at 245 and 175 MPa, meaning capped tablets above these TCP limits regardless of increased CP. A similar trend was observed in CS predictions from mechanical assessment, confirming that compaction simulation-based mechanical models can predict capping risk under desired compression conditions rapidly and accurately.

Study on mixed association behaviour of sodium salt of ibuprofen (IBF) and TX-165 mixture in different media

Study on mixed association behaviour of sodium salt of ibuprofen (IBF) and TX-165 mixture in different media

Can natural zeolite improve the removal of micropollutants in a nitrifying sequencing batch reactor? Insights on bioreactor performance, kinetics, and microbial community using Ibuprofen and Diclofenac as model micropollutants

This study presents the effect of natural zeolite (NZ) on a nitrifying sequencing batch reactor for removing ibuprofen (IBP) and diclofenac (DFC) in the long term, including kinetics and microbial community. The research was conducted in two 2 L liquid-volume bioreactors, one with 5 g/L of NZ. Nitrogen load rates ranging between 5.8 and 8.5 mg N/L h were studied. Bioreactors were operated for 217 days, with IBP and DFC concentrations ranging between 20 and 2000 μg/L. The results showed that using NZ in a nitrifying SBR only improves IBP removal at low concentrations (40 μg/L). IBP and DFC do not affect the nitrification efficiency or kinetic of ammonia removal. In the presence of IBP and DFC, NZ also favored a higher relative abundance in the genus Nitrosomonas and the Bradyrhizobiaceae family (responsible for nitrite-oxidizing activity), allowing higher IBP degradations at low IBP concentrations. Finally, IBP and DFC stimulated heterotrophic nitrification.