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The aqueous methanolic extract of stem part of Berberis calliobotiys (AMEBC) was evaluated for anti-inflammatory, analgesic and antipyretic activities in albino mice. Anti-inflammatory activity was evaluated by using carrageenan and albumin induced paw edema, while the analgesic effect was assessed by using formalin-induced paw licking and acetic acid induced abdominal writhing in mice. The brewer's yeast-induced pyrexia model was used for antipyretic investigation. Ibuprofen (40 mg/kg) was used as a standard drug in all the three models. The aqueous methanolic extract at both (250 mg/kg and 500 mg/kg) doses, showed highly significant (p < 0.001) reduction in paw edema induced by carrageenan and albumin. Moreover, the aqueous methanolic extract also highly significantly (p < 0.001) reduced (87%) the formalin-induced paw licking at 500 mg/kg. The highly significant (p < 0.001) reductions (24.48% and 37.9%) was also observed in the number of writhings. Furthermore, aqueous methanolic extract also demonstrated significant (p < 0.001) antipyretic activity against yeast induced pyrexia. The maximum effect was observed in all the three parameters at 500 mg/kg dose. The results suggest a potential benefit of the aqueous methanolic extract of Berbeis calliobotrys in treating conditions associated with inflammation, pain and fever.
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Plasma ibuprofen levels peaked and declined between successive doses. Fracture callus morphology was abnormal in the rofecoxib-treated rabbits and torsional mechanical testing showed that fracture healing was impaired. Ibuprofen treatment caused persistence of cartilage within the fracture callus and reduced peak torque at 6 weeks after osteotomy as compared to the fibulas from the placebo-treated rabbits. In the specimens allowed to progress to possible healing, non-union was seen in 5 of the 26 fibulas from the rofecoxib-treated animals as compared to 1 of 24 in the placebo group and 1 of 30 in the ibuprofen treatment group.
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A novel palladium-catalyzed oxidative aminocarbonylation reaction via C(sp(3))-H activation was established, which provides a convenient and general method for the construction of arylacetamides via the carbonylation reaction of alkyl aromatics and amines. By using this protocol, the marketed drug ibuprofen could be easily obtained.
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Matrix effect is a major problem when trace level pharmaceuticals in seawater were analyzed using solid-phase extraction (SPE) combined with high-performance liquid chromatography-electrospray ionization tandem mass spectrometry (HPLC-ESI-MS-MS). Therefore, efforts should be devoted to diminish matrix effect as much as possible. The present study investigates the matrix effect during the analysis of selected pharmaceutical residues (naproxen, ibuprofen, diclofenac and gemfibrozil) in seawater samples with ultra-high-performance liquid chromatography (UHPLC)-ESI low-energy collision-induced dissociation (CID) MS-MS. Solutions to reduce matrix effect were studied through optimization of SPE procedure and the employment of isotope-labeled analogues. Results showed that 30 mL of deionized water can efficiently diminish matrix effect and satisfactory absolute mean recoveries ranging from 73.5% to 120.5% were obtained in the optimized SPE condition. Isotope-labeled analogues employed as surrogates were found to be efficient to further compensate for matrix effect, with the relative mean recoveries ranging from 85.5% to 110.5%. The optimized method has been successfully applied for the analysis of target pharmaceutical residues in different seawater samples.
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Non-steroidal anti-inflammatory drugs (NSAIDs) inhibit cyclooxygenase (COX) activity, which is the rate-limiting enzyme in the synthesis of prostaglandins. Previous studies have indicated that NSAID therapy, and in particular NSAIDs that specifically target the inflammatory cyclooxygenase (COX-2), impair bone healing. We compared the effects of ibuprofen and rofecoxib on fibula osteotomy healing in rabbits to determine whether nominal, continuous inhibition of COX-2 with rofecoxib would differentially affect fracture healing more than cyclical inhibition of COX-2 using ibuprofen, which inhibits COX-1 and COX-2 and has a short half-life in vivo.
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The effect of different grades of hydroxyethyl cellulose (HEC) and hydroxypropyl methllcellulose (HPMC) on the film-formation and taste-masking ability for ibuprofen granules was evaluated. Three batches of coated ibuprofen granules were prepared using a roto-granulator, each with a different coating composition. Two grades of HEC [MW300,000 (H) and MW90,000 (L)] were combined with three different grades of HPMC [MW 11,000 (L), MW 25,000 (M) and MW 35,000 (H)] to prepare the coating solutions. Mechanical strength and physical properties of the polymer films were evaluated. Films made from HPMC (L)/HEC (H), HPMC (M)/HEC (H), and HPMC (H)/HEC (H) were stronger and more flexible than the HPMC (L) HEC (L) films. The assay, dissolution, particle size distribution, and environmental scanning electron microscopy (ESEM) data of the three batches of the coated ibuprofen granules were similar.
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Electronic tongues can produce chemical images of samples, whose changes can be correlated with general properties, e.g. taste sensations. In this work, a sensor array equipped with eight types of ion-selective electrodes was coupled with Principal Components Analysis in order to detect microencapsulation effect of two Active Pharmaceutical Ingredients (APIs), which influences their taste properties. The character of change of sensor array responses in samples modified by microencapsulation was the same in two investigated APIs (Ibuprofen and Rixithromycin), proving, that the "sensed taste" becomes similar in both formulations after Eudragit modification. The obtained results show, that the presented electronic tongue can be used for analysis of masking effects in drugs and detection of microencapsulation effect.
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Out of reviewed 51 patient charts, nineteen patients were found eligible for final comparative analysis. The daily amounts of peri-partum rescue analgesics with vs without neuraxial opioids were equianalgesic doses of parenteral hydromorphone (10.7 +/- 13.8 mg vs 2.6 +/- 0.7 mg, P = 0.45 for vaginal delivery; 16.4 +/- 21.1 mg vs 5.3 +/- 3.6 mg, P = 0.42 for elective cesarean section (CS)), oral ibuprofen (1.1 +/- 0.5g vs 0.8 +/- 0.4g, P = 0.37 for vaginal delivery; 1.1 +/- 0.2g vs 1.6 +/- 0.6g, P = 0.29 for elective CS), and acetaminophen (0.2 +/- 0.4g vs 0 +/- 0g, P = 0.56 for vaginal delivery; 0.3 +/- 0.3g vs 0.2 +/- 0.2g, P = 0.81 for elective CS). In the patients who underwent emergent CS after failed labor (all had received epidural opioids), there was clinical trend for higher daily amounts ofperi-partum rescue analgesics (parenteral hydromorphone 35.6 +/- 37.5 mg; oral ibuprofen 1.2 +/- 0.4g; oral acetaminophen 1.2 +/- 0.5g), when compared with vaginal delivery patients or elective CS patients who all had received neuraxial opioids.
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Loxoprofen (Loxonin(®), Loxonin(®) Pap, Loxonin(®) Tape) is a prodrug-type NSAID that is available in several formulations, including 60 mg tablets, 100 mg hydrogel patches and 50 or 100 mg tape. In active comparator-controlled trials, oral loxoprofen therapy (ranging from 2 days to 6 weeks' duration depending on the pain type) provided analgesic efficacy that generally did not significantly differ from that of celecoxib for postoperative pain or frozen shoulder, ibuprofen for knee osteoarthritis or naproxen for lumbar pain. In double-blind, double-dummy, multicentre trials, loxoprofen hydrogel patches were noninferior to oral loxoprofen with regard to rates of final overall symptomatic improvement over 1-4 weeks in patients with knee osteoarthritis, myalgia or trauma-induced swelling and pain. Loxoprofen hydrogel patches were also noninferior to other commercially available patches (ketoprofen and indometacin) over 2 or 4 weeks in patients with knee osteoarthritis or myalgia in open-label studies. Oral and topical loxoprofen were generally well tolerated in clinical trials. Thus, loxoprofen is a useful analgesic option for patients with pain and inflammation, with topical loxoprofen potentially reducing the risk of gastrointestinal, cardiovascular and renal complications associated with oral NSAID use.
Selective literature review, also including evidence-based guidelines and recommendations.
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A clinical audit was conducted in four primary health care centers in the Muscat region over a one-week period in April 2014. The target population included patients aged 18 years or over who attended one of the four health centers and were prescribed NSAIDs. Overall, 272 patients were recruited by systematic random sampling. The data were collected by two methods: direct face-to-face interviews and evaluations of the patient's electronic medical file. The prescribing doctors were blind to the audit. The collected information included patients demographics, past and current medical history of related comorbidities, NSAID type, dose, duration and indications for use, concomitant warfarin or/and aspirin prescriptions, and co-prescription of gastroprotective agents.