Disease relevance of ibuprofen

• Most of the patients with renal insufficiency showed elevated plasma (S)-ibuprofen levels, higher area under plasma concentration vs. time curve for (S)-ibuprofen and increased area under plasma concentration vs. time curves for (S)-/(R)-ibuprofen ratios as compared with their healthy counterparts [1].
• Reevaluation of some double-blind, randomized studies of dexibuprofen (Seractil): a state-of-the-art overview. Studies in patients with lumbar vertebral column syndrome, rheumatoid arthritis, distortion of the ankle joint, gonarthrosis, ankylosing spondylitis, and activated coxarthrosis [2].
• CONCLUSIONS: The active enantiomer dexibuprofen (S(+)-ibuprofen) proved to be an effective non-steroidal anti-inflammatory drug with a significant dose-response relationship in patients with painful osteoarthritis of the hip [3].
• The effect of a dexibuprofen mouth rinse on experimental gingivitis in humans [4].
• C3H/HeN mice were placed on chronic oral Ibu (CIbT; 200 and 600 micrograms/ml of water) or Indo (CIT; 10 micrograms/ml) 5 days after s.c. transplantation of 5 x 10(5) metastatic C3L5 mammary carcinoma for the prevention of spontaneous lung metastases [5].

High impact information on ibuprofen

• There were no significant differences between oral and intravenous doses for the area under the curve values, terminal rate constants, clearances, metabolite formation clearances, and serum protein binding for (R)- and (S)-ibuprofen [6].
• Although 12.5-100 mg/kg doses of DM alone produced no reliable effects, treatments with ibuprofen (IB, 50 and 100 mg/kg but not 12.5 or 25 mg/kg) produced mild analgesia in arthritic rats as determined using the Randall-Sellito test [7].
• METHODS AND MATERIALS: Nonselective COX inhibitor, ibuprofen (IB), and selective COX-2 inhibitor, SC-236, were used to determine the cytotoxicity and radiosensitization at varying pH of culture media [8].
• The most important finding was that Vv(alt mito/myocyte) was 0.09 +/- 0.16 and 0.02 +/- 0.04 in the hearts receiving PMN+PMA alone and when scavengers were added, respectively, whilst no changes in mitochondrial ultrastructure was observed after addition of IBU, BW 755C or DCM [9].
• Using a crossover study design, the renal clearance of sulfate was assessed in conscious female Lewis rats during control periods and following the infusion of two structurally dissimilar nonsteroidal anti-inflammatory drugs, ibuprofen (IBU) and indomethacin (INDO) [10].

Chemical compound and disease context of ibuprofen

• The aim of this double-blind randomized trial was to compare the isolated active enantiomer dexibuprofen (S(+)-ibuprofen) with the double dose of racemic ibuprofen and to show a dose-response relationship of dexibuprofen in painful osteoarthritis of the hip [3].
• Treatment of all five strains of Salmonella with APAP, ASA or IB under all four metabolic conditions did not induce any appreciable increases in revertant colony counts, as compared to the negative controls [11].
• At maximum erythema (8-12 h after UVB), the following approximate reductions in SBF (compared to control responses) were noted: 42-58% for combination therapies, 33-40% for IB or IN alone, and 17% for BD alone [12].

Biological context of ibuprofen

• The role of prostaglandins in the effects of IBU and INDO on sulfate homeostasis was investigated by examining the influence of concomitant intraarterial PGE2 administration (infusion of 0.1 micrograms/min) on nonsteroidal anti-inflammatory drug-induced alterations in sulfate renal clearance [10].
• 4. Interindividual variation in the pharmacokinetics of (S)-ibuprofen following administration of the racemate was similar to that following the administration of the single isomer suggesting that chiral inversion is not a major factor contributing to variability in the disposition of this drug [13].
• Water activity affects the esterification rates of (R)- and (S)-ibuprofen differently, leading to higher enantioselectivity at lower water activities [14].
• Ibuprofen (Ibu; 1,200 mg/day, to reduce PG-induced vasodilation) and placebo were administered orally for 2 days before two separate testing sessions in a double-blind manner [15].
• Resting heart rate was reduced in Ibu (52 +/- 3 beats/min) compared with placebo (57 +/- 3 beats/min) (P < 0.05) without change to MPP [15].

Anatomical context of ibuprofen

• Furthermore, it was shown that perturbation of IB absorption from the gastrointestinal tract may serve as an important discriminative measure for identification of the inversion site [16].
• In the male trial, CFA injection (P<.01) caused TMJ swelling and chromodacryorrhea (CFA-CON); IBU eliminated these changes in the CFA+IBU group [17].
• CIbT or CIT alone reduced the number of spontaneous lung metastases and restored anti-YAC-1 killer function of splenocytes with NK-like phenotype (AGM-1+, Thy-1-, Lyt-2-); some anti-C3L5 killer function was also generated in the high dose Ibu group and the killer cell showed AGM-1+, Thy-1+ and Lyt-2+ phenotype [5].
• TA-60 did not inhibit the activity of the PG degradating enzyme, 15-hydroxy PG dehydrogenase (15-OH-PG-DH) of the gastric mucosa like the other non-steroidal anti-inflammatory drugs (NSAIDs): IP, PBZ and IM [18].

Associations of ibuprofen with other chemical compounds

• No NSAID showed significant effects on basal and IL-1beta stimulated IL-8 production, except CELE and IBUP, which slightly increased basal IL-8 production [19].
• The tablet formulation did not influence the bioavailability of the drug and dexibuprofen was well absorbed from the gastro-intestinal tract [20].
• Furthermore, taxanes binding to the serum carrier was characterized by displacement chromatography, by adding into the mobile phase selected competitors, (S)-ibuprofen and valproic acid, that are known to bind to specific binding sites on HSA [21].
• Modification of pepsinogen I levels and their correlation with gastrointestinal injury after administration of dexibuprofen, ibuprofen or diclofenac: a randomized, open-label, controlled clinical trial [22].
• The competitive binding of two ligands, ibuprofen (IBP) and salicylic acid (SAL), to human serum albumin (HSA) was studied by using nuclear magnetic resonance (NMR) relaxation measurements [23].

Gene context of ibuprofen

• Ibuprofen (IBU) and bovine serum albumin (BSA) were selected as model drugs and loaded onto the unmodified and functionalized SBA-15 [24].
• 3. No difference was found (P > 0.05) between treatments in the percentage of the dose recovered in the urine as (R)- or (S)-ibuprofen plus metabolites (S-IBU: 80.2 +/- 8.47 vs RAC: 74.1 +/- 14.0%) [13].
• Ninety-eight (41%) physicians prescribed long-term use of oral steroids for 413 (5%) patients, 103 (42%) prescribed inhaled steroids for 1,032 (12%) patients, and 108 (45%) prescribed high-dose IBU for 723 (8%) patients to control CF [25].
• A reversed-phase liquid chromatographic method was developed for 2-(4-isobutylphenyl)propionic acid (IBPP) in bulk drug and compressed tablets containing 100-600 mg of drug per tablet [26].
• Solid lipid nanoparticles (SLN) containing or not (S)-(+)-2-(4-isobutylphenyl)propionic acid (ibuprofen) were prepared with Preciol ATO 5 as lipid phase by the hot homogenization technique and characterized through particle size analyses and zeta potential measurements [27].

Analytical, diagnostic and therapeutic context of ibuprofen

• Adding 25 mg/kg DM to 25 mg/kg IB likewise increased analgesia as measured by both the Randall-Sellito and spontaneous pain behavior tests (both P < 0.05) [7].
• The obtained (S)-ibuprofen imprinted 4-VPY-EDMA materials were evaluated using aqueous eluents by HPLC [28].
• Determination of 2-(4-isobutylphenyl)propionic acid in bulk drug and compressed tablets by reversed-phase high-performance liquid chromatography [26].
• A 0.5-mL aliquot of the immunosorbent (11.5 mg of IgG/mL gel) prepared by immobilization of the antibody was capable of retaining up to 1 microg of (S)-ibuprofen [29].
• d-Ibuprofen in ocular inflammation induced by paracentesis of the rabbit eye [30].

References