dexibuprofen / Generic mfg. - LARVOL DELTA

Antifebrile effects of dexibuprofen suppository on children with high fever. (PubMed, Pak J Pharm Sci) - "Dexibuprofen suppository provides rapid and effective antipyresis with better safety in pediatric emergency settings."

Journal • Retrospective data • Pediatrics

Retraction notice to "Local infiltration of the surgical wounds with levobupivacaine, dexibuprofen, and norepinephrine to reduce postoperative pain: A randomized, vehicle-controlled, and preclinical study" [Biomed. Pharmacother. 92 (2017) 459-467]. (PubMed, Biomed Pharmacother) - No abstract available

Journal • Preclinical • Pain

Simultaneous rapid structure identification and accurate quantitation of chiral drugs based on a home-built polarized Raman microscope. (PubMed, Opt Lett) - "The experimental results of the coefficients of determination (R2) are 0.957 for racemic ibuprofen and 0.988 for (S)-ibuprofen, and their root mean square error of prediction (RMSEP) values are 0.126% and 0.049%, respectively. These preliminary results give a hint that polarized Raman spectroscopy (PRS) is a powerful non-destructive analytical tool for drug applications. These preliminary results give a hint that polarized Raman spectroscopy (PRS) is a powerful non-destructive analytical tool for drug applications."

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Enhanced Anticancer Activity of Ibuprofen and 2'-Hydroxy-2,3,5'-trimethoxychalcone-Linked Polymeric Micelles in HeLa Cells. (PubMed, ACS Omega) - "We synthesized a polymeric micelle formulation incorporating (S)-ibuprofen ((S)-IP) and 2'-hydroxy-2,3,5'-trimethoxychalcone (DK143), termed (S)-IP-DK143 NP...The combination of pH-sensitive polymeric micelles and chalcone-based chemotherapy represents a promising approach for cervical cancer treatment. Further preclinical and clinical studies are warranted to validate its potential as an injectable anticancer formulation."

Journal • Cervical Cancer • Gynecologic Cancers • Hematological Disorders • Leukopenia • Oncology • Solid Tumor

Impact of Drug Hydrophilicity on Transdermal Delivery by Nanoemulsions. (PubMed, Pharmaceutics) - "Viscosity values covered broad ranges (3-9532 mPa·s for salbutamol; 13.4-9759 mPa·s for ibuprofen), with salbutamol generating an extended high-viscosity domain at 50% (w/w) surfactant and ibuprofen showing a narrower viscosity maximum at 30-40% surfactant...High surfactant levels suppressed permeation for both APIs, but the dominant positive drivers differed: balanced oil-water ratios for salbutamol and hydration-dependent diffusional resistance for ibuprofen. These findings demonstrate that API polarity and interfacial portioning behavior decisively govern NE performance, providing a framework for rational tailoring of oil-surfactant-water ratios to maximize transdermal delivery efficiency."

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Double Salts and Racemate in Mefloquine-Ibuprofen and Mefloquine-Ketoprofen Systems. A Structural and Thermochemical Analysis. (PubMed, Chirality) - "Using a drug-drug approach, we have investigated the crystallization behavior of Mefloquine (Mf), a racemic antimalarial drug, in combination with enantiopure (S)-ibuprofen and (S)-ketoprofen, as well as their racemic forms. On the other hand, the racemate with ketoprofen and the double salt with ibuprofen are the most soluble structures, suggesting that they are more stable systems than their counterparts. These findings support the view that double salt formation in such systems results from structural mimicry of racemates, emphasizing the challenges of predictable enantiomeric resolution and the importance of understanding structure-property relationships in chiral crystallization."

Journal • Infectious Disease

Ultrasensitive Fluorescent Detection of Urinary Trypsin for Early Pancreatic Disease Diagnosis: Toward Smartphone-Assisted Analysis. (PubMed, Chem Asian J) - "Its clinical applicability was further validated in the presence of acute pancreatitis (AP)-inducing factors, including aspirin, ibuprofen, dexibuprofen, acetaminophen, 6-mercaptopurine, as well as ethanol and its metabolites (acetaldehyde and acetate). In addition, urine samples were successfully analyzed using a smartphone-integrated fluorescence detection system, highlighting its practicality and clinical potential for early pancreatic disease diagnosis."

Journal • Pancreatitis • Targeted Protein Degradation

The Stereoselective Pharmacokinetics of Ibuprofen Enantiomers in Mice, Guinea Pigs, and Rats. (PubMed, Chirality) - "A chiral LC-MS/MS method was employed to simultaneously determine (R)-(-)-ibuprofen and (S)-(+)-ibuprofen in trace whole blood samples (5 μL)...Conversion rates calculated from R-IBU and S-IBU concentrations following racemic IBU administration exhibited significant interspecies differences: 54.9 ± 5.6% (rats), 76.6 ± 5.3% (mice), and 65.6 ± 6.7% (guinea pigs). In contrast, no significant species differences were observed when conversion rates were derived from S-IBU concentrations after administration of individual enantiomers (R-IBU and S-IBU), yielding values of 65.9 ± 6.5%, 76.8 ± 21.2%, and 66.3 ± 14.4% for rats, mice, and guinea pigs, respectively."

Journal • PK/PD data • Preclinical

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."

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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."

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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."

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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."

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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."

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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."

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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."

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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."

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