dexibuprofen / Generic mfg. - LARVOL DELTA

Origin of phase relative stability and phase transformation in an S-ibuprofen-nicotinamide cocrystal. (PubMed, Acta Crystallogr C Struct Chem) - "The determination of the crystallographic structure of this metastable form allowed an explanation of the main mechanisms at the origin of the relative stability of the two forms of the S-ibuprofen-nicotinamide cocrystals. This also made it possible to explain the transition mechanism between the two forms with temperature."

Journal • CDKN1A

Theoretical Examination on the Chiral Separation Mechanism of Ibuprofen on Cellulose Tris(4-methylbenzoate). (PubMed, Molecules) - "Our results demonstrated that, based on the optimized geometry using the ML-T2C-ELG method, the complexation energy of S-ibuprofen with CMB obtained at B3LYP-D3(BJ)/6-311G(d) level is more negative than that of R-ibuprofen, which is caused by the greater hydrogen bonding and π-π stacking interactions between CMB and S-ibuprofen...Moreover, the ML-T2C-ELG method was found to be valuable for optimizing the geometries of such flexible and large systems, which allows for a more accurate description of interactions between soft polymers and small molecules when coupled with the docking simulation. It is anticipated that this study can provide beneficial insights for future optical resolution mechanisms of other chiral drugs."

Journal

Sustainable D-Glucose-based ibuprofen ionic liquids/salts for anti-inflammatory applications. (PubMed, Bioorg Chem) - "Cytotoxicity and anti-inflammatory evaluations were performed on the synthesized GSIS/GSIL-Ibu in comparison to ibuprofen utilizing the mouse fibroblast cell line 3T3-L1. Formulations of enantiomerically pure S-ibuprofen demonstrated superior anti-inflammatory efficacy compared to racemic ibuprofen formulations."

Journal

Evaluate the safety and efficacy of dexibuprofen in improving fever symptoms in children aged 6 months to 3 years old Multi center post marketing clinical research plan (ChiCTR) - P4 | N=586 | Recruiting | Sponsor: The Second Affiliated Hospital of Nanchang University; The Second Affiliated Hospital of Nanchang University

New P4 trial • Infectious Disease • Respiratory Diseases

Efficacy and Safety of Dexibuprofen in the Treatment of Acute Infection-Induced Fever in Children (ChiCTR) - P4 | N=135 | Not yet recruiting | Sponsor: children's hospital of fudan university; children's hospital of fudan university

New P4 trial • Infectious Disease • Respiratory Diseases

A comparative study of dexibuprofen or celecoxib for neurosurgical over-the-counter and postoperative analgesia (ChiCTR) - P4 | N=126 | Recruiting | Sponsor: Sanbo Brain Hospital of Capital Medical University; Sanbo Brain Hospital of Capital Medical University

New P4 trial

Gradient, reversed-phase HPLC method for simultaneous determination of chemical and enantiomeric impurities of dexibuprofen in a single run. (PubMed, J Chromatogr A) - "In this work, a gradient reversed-phase HPLC method is presented for the simultaneous determination of four potential chemical impurities in dexibuprofen, as well as its chiral isomer, (R)-ibuprofen. Furthermore, the stability and robustness of the gradient system were confirmed by consistent performance over one hundred consecutive injections. Following regulatory validation guidelines, the developed HPLC method was effectively applied for the quality assessment of commercially available pharmaceutical formulations."

Journal

Efficacy and Safety of Dexibuprofen Oral Suspension for Fever Treatment in Children with Acute Lower Respiratory Tract Infections: A Multicenter, Randomized Controlled Trial (ChiCTR) - P4 | N=552 | Not yet recruiting | Sponsor: Department of Pediatrics, Xijing Hospital, the Fourth Military Medical University, Xi'an, China; Shaanxi International Medical Exchange Promotion Asso

New P4 trial • Infectious Disease • Respiratory Diseases

Efficacy, Safety, Blood Kinetics, and 213Bi Distribution Studies of [225Ac]Ac-SibuDAB in Prostate Cancer Patients. (PubMed, J Nucl Med) - "225Ac-labeled (S)-ibuprofen-diaminobutyric acid-PSMA (SibuDAB) is a novel, albumin-binding compound in prostate-specific membrane antigen (PSMA)-targeted α-therapy of prostate cancer...Only limited signs of xerostomia were observed after the treatment. 213Bi generated by recoil is rapidly distributed into urine after application of [225Ac]Ac-SibuDAB."

Journal • Dental Disorders • Genito-urinary Cancer • Hematological Disorders • Oncology • Prostate Cancer • Solid Tumor • Thrombocytopenia • Xerostomia

Near-Field Terahertz Nanoscopy Spatially Resolves Chiral Drug-Cell Interactions: Toward Precision Intracellular Pharmacology. (PubMed, Anal Chem) - "We systematically analyzed morphological and biochemical compositional differences between control cells and those treated with RS-ibuprofen, (R)-(-)-ibuprofen, and (S)-(+)-ibuprofen...Quantitative analysis of spectral intensity differences within nuclear regions (p < 0.001), based on single-frequency imaging and clustering analyses at characteristic THz peak frequencies, provided direct evidence of drug-induced heterogeneity. These findings establish a novel paradigm for mapping drug-cell interactions at the nanoscale, conceptualizing these processes as spatially encoded phenomena, thereby advancing the field of subcellular chiral pharmacology."

Journal

Anticancer Activity of Phospholipid-Dexibuprofen Conjugates Loaded in Nanostructured Lipid Carriers. (PubMed, Int J Nanomedicine) - "Antiproliferative assays confirmed enhanced activity of synthesized products and their increased accumulation in cancer cells. This study describes the synthesis of new conjugates of DXI and phospholipids and their nanotechnological formulations for potential use in cancer therapy."

Journal • Oncology

Simple Quantification of Sticking Propensities of Pharmaceuticals with Mechanochemistry. (PubMed, Mol Pharm) - "For example, p-nitrobenzoic acid and (R,S)-ibuprofen were found to stick with low propensities to the milling ball (100 g/m2)...Our method is robust, nondestructive, and highly versatile and allows for fast quantification of sticking propensities of many systems with small quantities of material. The method has the potential to transform the way we study sticking tendencies of pharmaceuticals, enabling the assessment of sticking propensities significantly early in the development pipeline before manufacturing problems arise."

Journal

Binding Affinity of Synthetic Cannabinoids to Human Serum Albumin: Site Characterization and Interaction Insights. (PubMed, Pharmaceuticals (Basel)) - "Competition for site I was observed between warfarin and four synthetic cannabinoids (5F-AMB, AB-PINACA, AMB-FUBINACA, and AB-CHMINACA)...The binding affinity of all synthetic cannabinoids increased in the presence of (S)-ibuprofen...These results may improve our understanding of their toxicokinetic behavior and help in predicting possible competitive interactions that could influence HSA binding and, consequently, their activity and toxicity. This study is the first to describe the binding affinity of synthetic cannabinoids to HSA, elucidate their recognition mechanisms, identify binding sites, and characterize their interactions with the protein."

Journal

A multi-center, randomized, and positive-drug parallel controlled prospective clinical study to evaluate the efficacy and safety of dexibuprofen in the treatment of children with fever caused by influenza (ChiCTR) - P=N/A | N=586 | Recruiting | Sponsor: The Seventh Affiliated Hospital Sun Yat-sen University; The Seventh Affiliated Hospital of Sun Yat-sen University

New trial • Infectious Disease • Influenza • Respiratory Diseases • CRP

Antipyretic Effect of Dexibuprofen Versus Ibuprofen in Children With Fever Caused by Upper Respiratory Tract Infection. (PubMed, Clin Pharmacol Drug Dev) - "The incidence of adverse events did not differ between the 2 groups (all P > .05). In conclusion, dexibuprofen has a comparable antipyretic effect and safety profile to ibuprofen in Chinese children with fever caused by URTI."

Clinical • Journal • Infectious Disease • Respiratory Diseases

Synthesis of Enantiostructured Triacylglycerol Prodrugs Constituting an Active Drug Located at Terminal sn-1 and sn-3 Positions of the Glycerol Backbone. (PubMed, Molecules) - "The current paper reports the asymmetric synthesis of a focused library of enantiostructured triacylglycerols (TAGs) constituting a potent drug of the NSAID type (ibuprofen or naproxen) along with a pure bioactive n-3 polyunsaturated fatty acid (PUFA) intended as a novel type of prodrug...The most challenging key step involved the incorporation of the drugs that were activated as oxime esters by the lipase exclusively in the terminal position of glycerol that is protected as a benzyl ether. All combinations, a total of 32 such prodrug TAGs, were prepared, isolated, and fully characterized, along with 24 acylglycerol intermediates, obtained in very-high-to-excellent yields in the majority of cases."

Journal

Theoretical analysis of lipase-enzymatic DKR model for racemic (R)- and (S)- ibuprofen ester in a hollow cylindrical membrane bioreactor. (PubMed, Sci Rep) - "The agreement between semi-analytical and numerical computations demonstrates the validity of these approximation methods. The findings provide significant insights for enhancing membrane reactor design and improving the efficiency of industrial processes for racemic ibuprofen ester production."

Journal

Relative effectiveness and gastrointestinal safety of NSAIDs being prescribed for upper respiratory tract infections: an explorative cohort study in primary care. (PubMed, Int J Clin Pharm) - "Our findings indicated that various NSAIDs may exhibit differing levels of effectiveness in treating URTIs, particularly those formulated for quick onset of action. No NSAIDs-UGIBs association was found. Further prospective, larger studies are needed to confirm these findings."

Journal • Gastroenterology • Gastrointestinal Disorder • Infectious Disease • Inflammation • Pain • Respiratory Diseases

RS, S (+) - and R (-)-ibuprofen cocrystal polymorphs: Vibrational spectra, XRD measurement and DFT calculation studies. (PubMed, Heliyon) - "In this paper, cocrystal polymorphs of RS-ibuprofen (RS-IBU), S (+)-ibuprofen (S(+)-IBU), R (-)-ibuprofen (R(-)-IBU) with nicotinamide (NIC) were synthesized by different methods...We found that the melt recrystallization method can generate cocrystal form A, while the solvent drop grinding method and solution evaporation method can generate cocrystal form B. In addition, in order to verify the successful preparation of them, we used density functional theory (DFT) to optimize and simulate the theoretical structures of the RS-IBU: NIC cocrystal polymorphs, and compared the simulated results with the experimental results. These research results provide a reference for the analysis and preparation of pharmaceutical cocrystal polymorphs and help to distinguish the cocrystal polymorphs."

Journal

Chemically Specific Coherent Raman Imaging of Liquid-Liquid Phase Separation and Its Sequelae. (PubMed, Anal Chem) - "In doing so, we also discovered and partially characterized a new polymorph of (S)-ibuprofen. Our results demonstrate the potential of correlative SRS and SHG for monitoring phase separation and crystallization in real time, giving mechanistic insights into the spatial distribution, chemical composition and structure of phase-separated domains and newly formed crystals. Such insights could benefit not only pharmaceutical development, but also the biomedical, food and chemical sectors."

Journal

Evaluation of the safety and efficacy of dexibuprofen in improving fever symptoms in children aged 6 months to 3 years, multicenter post marketing clinical trial protocol (ChiCTR) - P4 | N=586 | Sponsor: The Second Affiliated Hospital of Nanchang University; The Second Affiliated Hospital of Nanchang University

New P4 trial • Infectious Disease • Respiratory Diseases • CRP

Enantioselective Toxicity of Ibuprofen to Earthworms: Unraveling the Effect and Mechanism on Enhanced Toxicity of S-Ibuprofen Over R-Ibuprofen. (PubMed, Environ Sci Technol) - "The findings of this study highlight that S-IBU poses a higher risk than R-IBU to soil organisms under wastewater reuse scenarios and that the chirality of chemical pollutants in wastewater deserves more attention when implementing wastewater reuse. In addition, our study underscores that the differences in bioavailability and bioactivity may account for the enantioselective toxicity of chiral pollutants."

Journal

Dexibuprofen loaded into nanoemulsion based gel for topical application - In vitro characterization and in vivo anti-inflammatory evaluation. (PubMed, Colloids Surf B Biointerfaces) - "DEX-SE-T loaded nanoemulgel has improved in vivo anti-inflammatory activity as compared to ibuprofen gel. DEX-SE-T could be a promising option for effective topical treatment of inflammatory conditions."

Journal • Preclinical • Back Pain • Immunology • Inflammation • Inflammatory Arthritis • Musculoskeletal Pain • Pain • Rheumatoid Arthritis • Rheumatology • Women's Health

Molecular mechanisms of sulforaphane in Alzheimer's disease: insights from an in-silico study. (PubMed, In Silico Pharmacol) - ""Amyloid precursor protein catabolic process", "regulation of apoptotic signaling pathway", and "positive regulation of nitric oxide biosynthetic process" were the main pathways, while NFKB1, SP1, RELA, hsa-miR-17-5p, hsa-miR-16-5p, and hsa-miR-26b-5p were transcription factors and miRNAs implicated in sulforaphane In AD treatment, miRNA sponges, dexibuprofen, and sulforaphane may be effective...Further work is needed to elucidate its therapeutic effects based on our findings, including genes, miRNAs, molecular pathways, and transcription factors. The online version contains supplementary material available at 10.1007/s40203-024-00267-4."

IO biomarker • Journal • Alzheimer's Disease • CNS Disorders • Gastrointestinal Disorder • Inflammation • APP • BCL2 • MIR16 • MIR17 • RELA

Preparation of two new chiral metal-organic frameworks for lipase immobilization and their use as biocatalysis in the enantioselective hydrolysis of racemic naproxen methyl ester. (PubMed, Int J Biol Macromol) - "In this work, two new chiral MOFs (UiO-66@Np and UiO-66@Ib) were prepared by the covalent attachment of the chiral compounds (S-naproxen and S-ibuprofen) to the amine-functionalized Zr-MOF (UiO-66-NH2). In addition, it was observed that the catalytic activity, conversion rate and ees value of this composite (UiO-66@Np@CRL) remained almost unchanged in reuse after 6 months. The results showed that in enantioselective reactions, the highest conversion and enantioselectivity could be achieved when the chiral compound bound to the MOF and the model compound used are the same."

Journal