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Efficacy and tolerability of a new ibuprofen 200mg plaster in patients with acute sports-related traumatic blunt soft tissue injury/contusion.
Predel, HG, Giannetti, B, Connolly, MP, Lewis, F, Bhatt, A
Postgraduate medicine. 2018;(1):24-31
Abstract
BACKGROUND Ibuprofen is used for the treatment of non-serious pain. This study assessed the efficacy and safety of a new ibuprofen plaster for the treatment of pain associated with acute sports impact injuries/contusions. METHODS In this randomised, double-blind, multi-centre, placebo controlled, parallel group study, adults (n = 130; 18-58 years of age) diagnosed with acute sports-related blunt soft tissue injury/contusion were randomized to receive either ibuprofen 200 mg plaster or placebo plaster. Plasters were administered once daily for five consecutive days. The primary assessment was area under the visual analogue scale (VAS) of pain on movement (POM) over 0 to three days (VAS AUC0-3d). Other endpoints included algometry AUC from 0 to three days (AUC0-3d) and 0 to five days (AUC0-5d), to evaluate improvement of sensitivity at the injured site, and patient and investigator global assessment of efficacy. Safety was monitored throughout the study. RESULTS The ibuprofen plaster resulted in superior reduction in AUC0-3d compared with placebo; the Least Squares (LS) mean difference was 662.82 mm*h in favour of the ibuprofen 200mg plaster (P = 0.0011). The greater improvement in VAS AUC of POM was also observed after 12 h, 24 h, and five days of therapy. Tenderness also significantly improved with the ibuprofen plaster compared with placebo; LS mean difference in algometry/tenderness AUC0-3d was 1.87 N/cm2*d and AUC0-5d was 1.87 N/cm2*d (P values ≤0.0004). At all study timepoints, a greater percentage of patients and investigators rated the effectiveness of the ibuprofen 200 mg plaster as good/excellent than the placebo plaster. Treatment-emergent adverse events for the ibuprofen plaster were few (≤1.5%) and were mild in severity. CONCLUSIONS The results of this study indicate 200 mg plaster is effective and safe for the treatment of pain due to acute sports-related traumatic blunt soft tissue injury/contusion in adults.
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Oral ibuprofen differentially affects plasma and sweat lipid mediator profiles in healthy adult males.
Agrawal, K, Bosviel, R, Piccolo, BD, Newman, JW
Prostaglandins & other lipid mediators. 2018;:1-8
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Abstract
Sweat contains a variety of lipid mediators, but whether they originate from the plasma filtrate or from the cutaneous sweat glandular tissues themselves is unknown. To explore this knowledge gap, we collected plasma and sweat from healthy men (n = 9) immediately before and 0.5, 2 and 4 h after oral administration of 400 mg ibuprofen. Of the over 100 lipid mediators assayed by liquid chromatography-tandem mass spectrometry, ∼45 were detected in both plasma and sweat, and 36 were common to both matrices. However, baseline concentrations in each matrix were not correlated and metabolite relative abundances between matrices differed. Oral ibuprofen administration altered sweat lipid mediators, reducing prostaglandin E2, linoleoylethanolamide, and oleoylethanolamide, while increasing 11-hydroxyeicosatetraenoic acid, and causing transient changes in 9-nitrooleate, N-arachidonylglycine and 20-hydroxyeicosatetraenoic acid. Meanwhile, plasma N-acylethanolamide concentrations increased with ibuprofen administration. These results suggest that sweat and plasma differentially reflect biochemical changes due to oral ibuprofen administration, and that plasma is unlikely to be the predominant source of the sweat lipid mediator profile.
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Pharmacokinetics of Cromolyn and Ibuprofen in Healthy Elderly Volunteers.
Brazier, D, Perry, R, Keane, J, Barrett, K, Elmaleh, DR
Clinical drug investigation. 2017;(11):1025-1034
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UNLABELLED BACKGROUND AND OBJECTIVES The combination of cromolyn and ibuprofen is being investigated as a treatment for early Alzheimer's disease (AD). This study investigated the pharmacokinetics, safety, and tolerability of cromolyn and ibuprofen co-administration in healthy elderly adult volunteers. METHODS In this open-labeled study, 26 subjects, aged 55-75 years, received co-administration of inhaled cromolyn (single dose 17.1 mg; double dose 34.2 mg total) and oral ibuprofen (single dose 10 mg; double dose 20 mg total). Blood sampling was performed for 6 h after co-administration in all subjects; cerebrospinal fluid (CSF) was collected in three to four subjects per cohort for 4 h following co-administration. Safety parameters, including adverse events (AEs), were monitored throughout the study. RESULTS For cromolyn, the mean (±SD) maximum observed concentration (C max) in plasma was 46.69 ± 32.97 and 96.75 ± 46.22 ng/ml after single- and double-dose inhalation, respectively [time to C max (t max) ~22 min for each; terminal elimination half-life (t ½) ~1.8 h for each]. For ibuprofen, the plasma C max was 1090.98 ± 474.64 ng/ml and 2062.96 ± 655.13 ng/ml after single- and double-dose oral administration, respectively (t max ~1.6-1.8 h; t ½ ~1.9 h for each). For cromolyn, the CSF C max was 0.24 ± 0.08 ng/ml at 3.72 ± 0.70 h after single-dose administration and 0.34 ± 0.17 ng/ml at 3.45 ± 0.95 h after double-dose administration, and for ibuprofen, the CSF C max was 3.94 ± 1.29 ng/ml at 2.55 ± 0.96 h after single-dose administration and 8.93 ± 3.29 ng/ml at 3.15 ± 1.05 h after double-dose administration. Three (12%) subjects reported mild or moderate AEs which were unlikely to be related to study drug. CONCLUSIONS The combination of cromolyn and ibuprofen was safe and well tolerated. The concentrations of cromolyn and ibuprofen observed in the CSF are considered sufficient to titrate the estimated daily amyloid production and the associated inflammatory response in patients with AD.
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Analgesic Efficacy of a New Immediate-Release/Extended-Release Formulation of Ibuprofen: Results From Single- and Multiple-Dose Postsurgical Dental Pain Studies.
Christensen, S, Paluch, E, Jayawardena, S, Daniels, S, Meeves, S
Clinical pharmacology in drug development. 2017;(3):302-312
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Analgesic effects of ibuprofen immediate-release/extended-release (IR/ER) 600-mg tablets were evaluated in 2 randomized, double-blind, placebo-controlled dental pain studies. Patients 16-40 years old with moderate-severe pain following third-molar extraction received single-dose ibuprofen 600 mg IR/ER (formulation A or B), naproxen sodium 220 mg, or placebo (2:2:2:1; study 1) or 4 doses of ibuprofen 600 mg IR/ER (formulation A) or placebo (1:1; study 2). In study 1 (n = 196), mean (standard deviation [SD]) time-weighted sum of pain intensity difference scores for placebo, ibuprofen IR/ER A, ibuprofen IR/ER B, and naproxen, respectively, were 0.05 (9.2), 16.87 (9.4), 17.34 (10.5), and 12.66 (10.0) over 0-12 hours and -0.03 (4.1), 6.57 (4.4), 7.14 (5.2), and 5.14 (5.0) over 8-12 hours (all P < .001 vs placebo). In study 2 (n = 106), mean (SD) time-weighted sum of pain relief and pain intensity difference scores were 18.2 (20.0) versus 41.5 (21.0) at 0-12 hours and 10.3 (12.0) versus 18.4 (12.1) at 8-12 hours for placebo versus ibuprofen IR/ER, respectively (P < .001 for both); efficacy was sustained over each of the four 12-hour dosing intervals with ibuprofen. Gastrointestinal adverse events predominated with placebo both after study medication administration and after rescue medication use, if applicable. Ibuprofen 600 mg IR/ER provided safe and effective analgesia after single and multiple doses.
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Effects of acetaminophen and ibuprofen in children with migraine receiving preventive treatment with magnesium.
Gallelli, L, Avenoso, T, Falcone, D, Palleria, C, Peltrone, F, Esposito, M, De Sarro, G, Carotenuto, M, Guidetti, V
Headache. 2014;(2):313-24
Abstract
AIM: The purpose of this study was to evaluate both the effects of ibuprofen and/or acetaminophen for the acute treatment of primary migraine in children in or out prophylactic treatment with magnesium. METHODS Children ranging from the ages of 5 to 16 years with at least 4 attack/month of primary migraine were eligible for participation the study. A visual analog scale was used to evaluate pain intensity at the moment of admission to the study (start of the study) and every month up to 18 months later (end of the study). RESULTS One hundred sixty children of both sexes aged 5-16 years were enrolled and assigned in 4 groups to receive a treatment with acetaminophen or ibuprofen without or with magnesium. Migraine pain endurance and monthly frequency were similar in the 4 groups. Both acetaminophen and ibuprofen induced a significant decrease in pain intensity (P < .01), without a time-dependent correlation, but did not modify its frequency. Magnesium pretreatment induced a significant decrease in pain intensity (P < .01) without a time-dependent correlation in both acetaminophen- and ibuprofen-treated children and also significantly reduced (P < .01) the pain relief timing during acetaminophen but not during ibuprofen treatment (P < .01). In both acetaminophen and ibuprofen groups, magnesium pretreatment significantly reduced the pain frequency (P < .01). CONCLUSIONS Magnesium increased the efficacy of ibuprofen and acetaminophen with not age-related effects.
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Comparison of effects of ginger, mefenamic acid, and ibuprofen on pain in women with primary dysmenorrhea.
Ozgoli, G, Goli, M, Moattar, F
Journal of alternative and complementary medicine (New York, N.Y.). 2009;(2):129-32
Abstract
OBJECTIVES To compare the effects of ginger, mefenamic acid, and ibuprofen on pain in women with primary dysmenorrhea. METHODS This was a double-blind comparative clinical trial conducted from September 2006 to February 2007. Participants were 150 students (18 years old and over) with primary dysmenorrhea from the dormitories of two medical universities who were alternately divided into three equal groups. Students in the ginger group took 250 mg capsules of ginger rhizome powder four times a day for three days from the start of their menstrual period. Members of the other groups received 250 mg mefenamic acid or 400 mg ibuprofen capsules, respectively, on the same protocol. A verbal multidimensional scoring system was used for assessing the severity of primary dysmenorrhea. Severity of disease, pain relief, and satisfaction with the treatment were compared between the groups after one menstruation. RESULTS There were not significant differences between groups in baseline characteristics, p > 0.05. At the end of treatment, severity of dysmenorrhea decreased in all groups and no differences were found between the groups in severity of dysmenorrhea, pain relief, or satisfaction with the treatment, p > 0.05. No severe side effects occurred. CONCLUSION Ginger was as effective as mefenamic acid and ibuprofen in relieving pain in women with primary dysmenorrhea. Further studies regarding the effects of ginger on other symptoms associated with dysmenorrhea and efficacy and safety of various doses and treatment durations of ginger are warranted.
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The effect of systemic administration of ibuprofen in the experimental gingivitis model.
Sekino, S, Ramberg, P, Lindhe, J
Journal of clinical periodontology. 2005;(2):182-7
Abstract
BACKGROUND Studies in humans have indicated that systemically administered flurbiprofen and ibuprofen may reduce gingivitis. De novo plaque formation is enhanced at tooth surfaces adjacent to inflamed gingivae. OBJECTIVE The aim of the present clinical trial was to evaluate the effect of systemic administration of ibuprofen on gingivitis and plaque build-up. MATERIAL AND METHODS Eleven subjects were recruited for the study and were given oral hygiene instruction, scaling and professional mechanical tooth cleaning (PTC). At the end of a preparatory period (Day 0), the participants were told to abstain from all mechanical plaque control measures during a 2-week experimental period but to rinse with an assigned mouth rinse (positive control: 0.1% chlorhexidine digluconate; negative control: saline) or administer ibuprofen (tablets of 200 mg twice daily). Mouth rinsing was performed twice a day (after breakfast and in the evening), for 60 s with 10 ml. Re-examination was performed after 14 days of experiment. After a 2-week "wash-out" period, the participants received a new PTC and a second 14-day experimental period was initiated. The experimental and "wash-out" periods were repeated until all volunteers had been involved in all three regimens. Dental plaque was scored using the Quigley & Hein Plaque Index system and gingivitis according to the Gingival Index (GI) system. Supragingival plaque was collected and prepared for dark-field microscopy. One hundred bacterial cells were counted and classified into six different groups: coccoid cells, straight rods, filaments, fusiforms, spirochetes and motile rods. Gingival crevicular fluid (GCF) was collected from the same sites that were sampled for plaque. The volume of GCF collected in each strip was measured and analysed regarding content of lactoferrin and albumin. RESULTS During the period when the panelists rinsed with saline they accumulated large amounts of plaque and developed marked signs of gingivitis. When they rinsed with chlorhexidine digluconate, small amounts of plaque formed and few sites received GI score > or =2. After the 2 weeks of ibuprofen administration, the panelists presented with significantly fewer sites that scored GI > or =2 but had formed similar amounts of plaque as during the negative control period. CONCLUSION It is suggested that ibuprofen administered via the systemic route has an effect on gingivitis but not on de novo plaque formation.
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Effects of ibuprofen on molecular markers of cartilage and synovium turnover in patients with knee osteoarthritis.
Gineyts, E, Mo, JA, Ko, A, Henriksen, DB, Curtis, SP, Gertz, BJ, Garnero, P, Delmas, PD
Annals of the rheumatic diseases. 2004;(7):857-61
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OBJECTIVE The aim of this study was to evaluate the effect of ibuprofen on the urinary excretion of C-terminal crosslinking telopeptide of type II collagen (CTX-II) and urinary glucosyl galactosyl pyridinoline (Glc-Gal-PYD), two new molecular markers of cartilage and synovial tissue metabolism, respectively, in patients with knee osteoarthritis (OA). METHODS We studied 201 patients with knee pain and radiographic evidence of knee OA who were on treatment with non-steroidal anti-inflammatory drugs (NSAIDs) prior to study initiation. After an initial screening visit, patients were withdrawn from their pre-study NSAID and, following a flare of their OA symptoms, were randomised to ibuprofen (2400 mg/day) or placebo. Urinary CTX-II and Glc-Gal-PYD levels were measured at time of randomisation (baseline) and after 4-6 weeks of treatment. RESULTS After 4 to 6 weeks, urinary CTX-II (+17%, p = 0.023) and Glc-Gal-PYD (+10%, p = 0.020) increased significantly from baseline in the placebo group whereas marginal or no increase was observed in the ibuprofen group (CTX-II +2%, NS and Glc-Gal-PYD +4%, p = 0.045). For urinary CTX-II, the difference in the change from baseline between placebo and ibuprofen treated groups was significant (13%, p = 0.017). At baseline, urinary levels of CTX-II and Glc-Gal-PYD were higher in patients with knee swelling (n = 127) than in those without (n = 74) (p<0.02 for both markers). When patients were stratified according to presence or absence of knee swelling at baseline, the increases over 4-6 weeks of urinary CTX-II and Glc-Gal-PYD in the placebo group were restricted to patients with knee swelling (+22% from baseline, p = 0.001 and +12%, p = 0.011, for urinary CTX-II and Glc-Gal-PYD respectively). In patients with knee swelling who were treated with ibuprofen this increase was not observed and the difference from placebo was significant for urinary CTX-II (p = 0.014). CONCLUSION In patients with a flare of knee OA, specifically in patients with evidence of joint inflammation documented by knee swelling, there was a significant increase in markers reflecting cartilage and synovium metabolism that could partly be prevented by high doses of ibuprofen. These data suggest that patients with a flare of knee OA are characterised by increased cartilage and synovial tissue degradation, which may be partly prevented by high doses of NSAIDs.
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In vitro and in vivo pharmacoscintigraphic evaluation of ibuprofen hypromellose and gelatin capsules.
Cole, ET, Scott, RA, Cade, D, Connor, AL, Wilding, IR
Pharmaceutical research. 2004;(5):793-8
Abstract
PURPOSE To evaluate the in vitro and in vivo characteristics of hypromellose (HPMC) capsules prepared using a gellan gum and potassium gelling system compared to conventional hard gelatin capsules. METHODS The in vitro dissolution of ibuprofen gelatin and HPMC capsules was determined using the USP and TRIS buffers at pH 7.2. The effect of pH and composition of the media was determined using a model drug that is soluble throughout the pH range 1.2 to 7.2. In an 11 subject four-way crossover study, the gastrointestinal performance of ibuprofen gelatin and HPMC capsule formulations was evaluated using scintigraphy and pharmacokinetics following fasted and fed dosing. RESULTS Acid conditions and the presence of K+ cations hinder HPMC capsule opening, whereas in water, dissolution is identical to that of gelatin. These effects are related to the nature of the gel network that is formed in the presence of cations. No significant difference in esophageal transit was observed. Although the in vivo opening times of HPMC capsules were longer than for their gelatin counterparts, no significant difference in the regulatory important pharmacokinetic metrics of C(max) and AUC was found between ibuprofen, gelatin and HPMC capsules. CONCLUSIONS The in vitro performance of HPMC capsules differ from gelatin, which will require modification to dissolution testing methodology for certain drugs. However, for the class II BCS drug ibuprofen, the two capsule types were not statistically different when comparing AUC and C(max) values, which suggests that the in vitro differences have reduced in vivo relevance.
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Efficacy of nonsteroidal anti-inflammatory medications for prevention of atrial fibrillation following coronary artery bypass graft surgery.
Cheruku, KK, Ghani, A, Ahmad, F, Pappas, P, Silverman, PR, Zelinger, A, Silver, MA
Preventive cardiology. 2004;(1):13-8
Abstract
This study was designed to test whether nonsteroidal anti-inflammatory medications could reduce the frequency of atrial fibrillation after coronary artery bypass graft surgery. The study was designed as an open-label, randomized trial. Patients undergoing first-time coronary artery bypass graft surgery were considered eligible. Patients with a history of atrial fibrillation, serum creatinine >2.0 mg/dL, on antiarrhythmic treatment, and those undergoing concomitant valvular surgery were excluded. The study was conducted in a single, university-affiliated community hospital. The researchers' role in the study was restricted to randomizing the patients and collecting data. The primary clinical care team made all decisions regarding patient care. One hundred patients were randomized to two groups: one received 30 mg ketorolac intravenously every 6 hours until able to take oral medications, at which point the patients were switched to 600 mg ibuprofen orally three times a day; the other group received conventional treatment. The primary end point of the study was incidence of atrial fibrillation in the immediate postoperative period. Atrial fibrillation occurred in 14 patients (28.6%) in the conventional treatment group vs. five patients (9.8%) in the ibuprofen group (p<0.017). Nonsteroidal anti-inflammatory medications were relatively safe and effective in significantly reducing the incidence of atrial fibrillation after coronary artery bypass graft surgery.