O ibuprofeno é um anti-inflamatório não-esteroidal (AINE) que possui propriedades analgésicas e anti-térmicas e é empregado na terapêutica em casos dores discretas e moderadas, artrite reumatóide, osteoartrite e dismenorréia primária, nas concentrações de 200, 300, 400 e 600 mg. Entretanto, a formulação contendo 200 mg não está disponível no mercado farmacêutico brasileiro. No presente trabalho, foi desenvolvida uma formulação de comprimidos de ibuprofeno 200 mg que apresentou, além de outras características físico-químicas adequadas, um ótimo perfil de dissolução. Foram testadas oito formulações, obtidas a partir de um projeto fatorial fracionado, avaliando-se diversos excipientes. Além disto, as formulações foram submetidas à temperatura ambiente, 37 ºC e 50 ºC, e analisadas à 30 e 60 dias, com o objetivo de avaliar as transformações físicas que podem ocorrer durante o armazenamento das mesmas. Os resultados das análises físico-químicas foram tratados estatisticamente, utilizando-se o programa STATGRAFCS, através de uma análise exploratória e de um estudo de efeitos. Concluiu-se, então, que a melhor formulação foi a seguinte: IBUPROFENO - 200; AMIDO - 47; LACTOSE - 72; CELULOSE MICROCRISTALINA - 23; ESTEARATO DE MAGNESIO - 8. / Ibuprofen is a non steroidal antiinflamatory drug (NSAD), that has analgesic and antipyretic properties. It is used in terapeutic cases of mild to moderant pain, rheumatoid arthritis, osteoarthritis, and primary dysmenorrhea, in the 200, 300, 400, and 600 mg of concentration. In the Brazilian pharmaceutical market the formulation of 200 mg doesn\'t exist. In this study, a formulation of ibuprofen was developed for 200 mg tablets, that has suitable physical-chemical properties and an excellent dissolution profile. The eight formulations tested were obtained from factorial designs, evaluating several excipients. These formulations also had been submitted at room temperature, 37 ºC, and 50 ºC and were analised at 30 and 60 days, with the objective to evaluate the physical transformatiom that could have occurred during that time. The results were tested statistically by the STATGRAFCS program, using the exploratory analysis and the effects study. The final results showed that the best formulation was: IBUPROFEN - 200; STARCH - 47; LACTOSE - 72; MICROCRYSTALLINE CELLULOSE - 23; MAGNESIUM STEARATE - 8.

Nonsteroidal anti-inflammatory drugs (NSAIDs) are a class of drugs prescribed to relieve pain, fever and inflammation, and are among the most commonly consumed medications in Ontario. Approximately 70% of the ingested dose is excreted unchanged or as an active metabolite, much of which reaches the surface waters of lakes and rivers. NSAIDs function through the inhibition of cyclooxygenase (COX), an enzyme present in two isoforms in the body; the constitutively expressed COX-1 and the inducible COX-2. Traditional NSAIDs like ibuprofen inhibit both isoforms with little selectivity while newer variants such as naproxen preferentially inhibit COX-2. Both COX isoforms share a high similarity between humans and fish creating a potential for off target effects to exposed aquatic organisms. This research investigated the chronic effects of waterborne exposure to 0, 0.1, 1, 10 and 100 μg/L of a nonselective and selective NSAID (ibuprofen and naproxen, respectively) on Florida flagfish (Jordanella floridae) over one complete life-cycle. Chronic exposure concentrations were selected by performing a short term experiment which examined the hatchability of flagfish eggs using continuous semi-static exposure conditions. Growth, survivability and reproductive endpoints were assessed in the life-cycle study. A concentration-response relationship for both NSAIDs was detected during the first 28 days post-hatch, resulting in increased body length for F1 fish and their offspring with increasing concentrations. Exposure to 0.1 μg/L of both ibuprofen and naproxen resulted in a decrease in egg fertilization providing an experimental LOEC (lowest observable effect concentration) of 0.1 ug/L and NOEC (no observable effect concentration) of < 0.1 ug/L for both ibuprofen and naproxen based on the reproductive endpoint. This indicates that either NSAID has the potential to affect the reproductive success of flagfish at concentrations at or below those commonly found in the environment. / UOIT

Pharmacokinetic parameters for theophylline and dyphylline were evaluated in horse cerebrospinal fluid (csf) and plasma. Pharmacokinetic parameters did not differ significantly (p > 0.05) at the same dose for either drug when administered alone or concomitantly. Theophylline and dyphylline penetrate horse csf to produce approximately 1/2 the concentrations found in plasma. Doubling the theophylline dose from 10 mg/Kg to 20 mg/Kg doubled both csf and plasma theophylline concentrations. However, doubling the dyphylline dose from 20 mg/Kg to 40 mg/Kg tripled both csf and plasma dyphylline concentrations. Simultaneous fitting between plasma and csf drug concentrations indicates that plasma is a good indicator for predicting csf concentrations for both theophylline and dyphylline. The influence of ibuprofen input rate on antipyresis was studied in rats with yeast induced fever. In addition, a data analysis comparison was made between rat data collected from this present study and literature data from fevered children. Counterclockwise hysteresis curves (ibuprofen plasma concentration versus temperature decrement) were observed following ibuprofen oral suspension when administered to rats and children. When the collapsed hysteresis curves were plotted (mean predicted total ibuprofen effect compartment concentration versus mean predicted temperature decrement effect) the rat and children's curves were not superimposable. However, the collapsed hysteresis curves of mean predicted ibuprofen unbound effect concentration versus mean predicted temperature decrement effect were superimposable for data from the rats and children. Based on mean unbound ibuprofen effect compartment concentration versus mean predicted temperature decrement effect, the antipyretic response to ibuprofen appears to be comparable between rats and children. The apparent qualitative trend in temperature decrement, although not statistically significant, perhaps due to variability, appears to be different among ibuprofen input regimens in rats. Maximum temperature decrement appears to relate not just to the concentration of ibuprofen obtained at steady-state, but the rate at which it is obtained. / Graduation date: 1993

Dissertation submitted in partial compliance with the requirements for the Masters Degree in Technology: Chiropractic, Durban University of Technology, 2010. / The 1 year overall prevalence of Episodic Tension-Type Headache (ETTH) is 38.3%; with lifetime prevalence at 46% for TTH. Little literature exists to support the effectiveness of spinal manipulation in the treatment of ETTH. Therefore aim of this study was to determine the relative effectiveness of cervical spine manipulation and a Nonsteroidal Anti-inflammatory drug (NSAID) (Ibuprofen®) in the treatment of ETTH. Method: This study was a prospective randomised clinical trial with two intervention groups (N=32, n1=16 and n2=16). The allocation of participants to the two groups was completed by means of simple randomization. Group one were treated using cervical spine manipulation. Group two were treated using Ibuprofen. Subjective measurements included the Numerical Rating Scale 101 Questionnaire (NRS-101), Short Form McGill Pain Questionnaire (SF-MPQ), CMCC Neck Disability Index (CMCC) and Headache Diary. A p value <0.05 was considered as statistically significant. Results: The subjective measurements of the NRS-101, SF-MPQ and CMCC showed a significant time effect in both treatment groups. Several of the subjective Headaches Diary outcomes followed this trend with significant time effect in both groups. There was a significant treatment effect for the NRS-101. Several subject outcomes from the Headache Diary showed a significant treatment effect in favour of manipulation, namely frequency and duration of headaches. Conclusion: The findings in this study have shown that cervical spine manipulation is more effective than Ibuprofen® for the treatment of ETTH in terms of several subjective outcomes namely: pain intensity (NRS-101), and the frequency and the duration of headache per day.

No description available.

No description available.

Dissertation (Ph.D.)--Auburn University, 2005. / Abstract. Vita. Includes bibliographic references.

Introduction: Chronic inflammation with aging is associated with sarcopenia and osteoporosis. Bovine colostrum is the first milk secreted by cows following parturition and contains bioactive substances, while ibuprofen is a non-steroidal anti-inflammatory drug. Both target the inflammatory pathway regulated by cyclooxygenase and have potential to increase muscle and bone mass when combined with resistance training. Objectives: To determine efficacy of novel anti-inflammatory nutritional (bovine colostrum) and pharmaceutical (ibuprofen) supplementation during resistance training on muscle and bone properties and strength in older adults. Methods: Older adults (≥50y) were randomly assigned to receive 38g/d of colostrum or whey protein during a resistance training program for 8 weeks; postmenopausal women (≥60y) were randomly assigned to receive ibuprofen (400 mg) or placebo post-exercise while performing a resistance training program or stretching program (3d/wk) for 9 months. Both studies utilized dual energy x-ray absorptiometry (DXA) for body composition and predicted 1-repetition maximum for strength. The bovine colostrum study further assessed muscle thickness of the biceps and quadriceps, plasma insulin-like growth factor-1, and inflammation and bone resorption markers; the ibuprofen study further assessed bone and muscle properties and estimates of bone strength (peripheral quantitative computed tomography), and dynamic balance. Results: Bovine colostrum supplementation during resistance training increased leg press strength (21%) and reduced bone resorption (-29%) versus whey protein. Both colostrum and whey protein groups improved chest press strength, muscle thickness, and lean tissue mass. Ibuprofen alone appeared beneficial for preventing loss of areal bone density at Ward’s region (3%) and bone properties at the distal radius (0.5%) and radial shaft (1.1%), while exercise alone appeared beneficial for bone properties at the distal radius (0.6%). However, the interaction of resistance training and ibuprofen negated the benefits at the distal radius (-1.5%). Neither ibuprofen nor resistance training was effective for increasing lean tissue mass, although resistance training improved body fat percentage (-2.0%), increased upper and lower body strength (23%, 110%), and preserved muscle density of the calf (-3.1%). Conclusion: While bovine colostrum could be taken within close proximity to exercise, ibuprofen should not be as it may interfere with the effects of exercise when the two interventions are combined.

Core temperature (Tc) regulation is fundamental to mammalian survival, since hypothermia (Tc ≤ 35°C) and hyperthermia (Tc ≥ 40°C) are major risk factors for health and wellbeing. The purpose of this thesis was to determine if acetaminophen, an analgesic and antipyretic drug, increased the onset of hypothermia or hyperthermia during passive cold and heat stress, respectively. It was later investigated if acetaminophen induced inhibition of cyclooxygenase mediated these side-effects. In Study 1a, the plasma acetaminophen response to a dose of 20 mg·kg-1 of lean body mass was determined through enzyme linked immunosorbent assay. In Study 1b, the effect of acetaminophen administration on internal temperature (rectal; Tre) during a passive 2-hour mild cold (20°C, 40% relative humidity) exposure was examined. Study 1a showed that the plasma response was homogenous between subjects, reaching peak concentrations between 80-100 minutes (14 ± 4 μg·ml-1). In Study 1b, acetaminophen reduced Tre in all participants compared with baseline, and the average peak reduction was 0.19 ± 0.09°C. In contrast, Tre remained stable when participants ingested a sugar placebo. Study 1 is the first experiment which confirms a hypothermic side-effect of acetaminophen in healthy humans. Study 2 investigated whether acetaminophen augmented the rate of Tre rise during exposure to passive dry (45°C, 30% r.h.) and humid (45°C, 70% r.h.) heat stress for 2-hours and 45-minutes, respectively. This study showed that the rate of Tre rise in the dry (0.005 vs 0.006°C∙min-1) and humid (0.023 vs 0.021 °C∙min-1) conditions were similar between the acetaminophen and placebo trials (p > 0.05). Study 2 is the first experiment which confirms acetaminophen has no meaningful effect on thermoregulation during passive dry or humid heat exposure. Study 3 determined how the hypothermic effect of acetaminophen changes during exposure to a thermoneutral (25°C, 40% r.h.) and cold (10°C, 40% r.h.) environment for 2-hours. In summary, there was no hypothermic effect of acetaminophen in a thermoneutral environment (p > 0.05), whereas Tre fell by 0.40 ± 0.15°C compared with baseline during cold stress (p < 0.05). Compared with the placebo, Tre was ~0.35°C lower at 120 minutes, but was significantly lower from 70-minutes. Study 3 confirmed that there is a relationship between the level of cold stress and magnitude of the hypothermic effect of acetaminophen. Study 4 determined whether ibuprofen (400 mg), a cyclooxygenase inhibitor, reduced Tre during 2-hour passive cold stress (10°C, 40% r.h.) to a level comparable with acetaminophen. Ibuprofen administration did not influence Tre, vastus medialis shivering, or energy expenditure compared with a placebo throughout the cold exposure (p > 0.05). Taken together, this renders it unlikely that cyclooxygenase activity is required for thermogenesis induced by skin cooling. Study 4 provides evidence that acetaminophen induced hypothermia is not exclusively mediated by cyclooxygenase inhibition. In Summary, this series of experiments has shown that acetaminophen has a hypothermic side effect in healthy humans, which is amplified during acute cold stress. Ibuprofen had no such effect on thermoregulation during cold exposure, so it is unlikely that cyclooxygenase inhibition mediates the hypothermic side-effect of acetaminophen.

A quitosana tem se mostrado muito atrativa para a indústria farmacêutica, visando principalmente matrizes de liberação controlada com fármacos amplamente utilizados pela população em altas dosagens ou em períodos prolongada tal como o Ibuprofeno. O uso de combinado de polímeros e materiais como a argila é uma opção interessante, unindo as propriedades de ambos os materiais, minimizando o efeito colateral do fármaco. No presente trabalho descreve-se a preparação de um complexo iônico contendo quitosana e ibuprofeno por meio de uma reação ácido base entre ambos. Em uma segunda etapa, foi preparado um nanocompósito de montmorilonita/quitosana contendo o fármaco ibuprofeno. As matrizes foram caracterizadas por diferentes técnicas, incluindo análise elementar, ressonância magnética nuclear (RMN) de 13C e 1H, termogravimetria (TG), calorimetria exploratória diferencial (DSC), difração de raios X (DRX) e espectroscopia de infravermelho com transformada de Fourrier (FTIR). O grau de desacetilação (GD) da quitosana obtido por titulação potenciométrica foi de 80,0%. Esses resultados foram confirmados por medidas de RMN 1H e RMN 13C. O estudo dissociação do fármaco, na presença e na ausência de argila, foi avaliado por cromatografia líquida de alta eficiência (CLAE) e por espectroscopia de absorção eletrônica UV-VIS. A dissociação do fármaco em meio aquoso foi avaliada em pH 2 e 7, que correspondem aos valores encontrados no estômago e no intestino, respectivamente. Os resultados indicaram que a dissociação do ibuprofeno das matrizes é dependente do pH e que a presença da argila retarda a dissociação do fármaco na matriz. / Due to its interesting properties chitosan has attracted interest regarding several applications including drug carrier in pharmaceutical industry, mainly for actives consumed in high doses for long periods, as Ibuprofen. The combined use of materials such as polymers and the clay is an interesting option, combining the properties of both materials while minimizing the side effects of the drug. A chitosan-ibuprofen ionic complex had been prepared from the acid-base reaction between both of them. In a second step a montmorilonite/chitosan nanocomposite containing ibuprofen was also prepared. The complex and the nacomposite containing ibuprofen had been characterized by several techniques including elemental analysis, 13C e 1H, nuclear magnetic resonance (NMR), thermogravimetry (TG), differential scanning calorimetry (DSC), X-ray diffraction (XRD) and Fourrier transform infrared spectroscopy (FTIR). The chitosan degree of deacetylation (DD) was determined by potentiometry as 80.0%. These results were confirmed by 13C e 1H NMR. The dissociation of the pharmaceutical from the complex and nanocomposite was investigated by high performance liquid chromatography (HPLC) and electronic spectroscopy in the UV-vis (UV-vis). The dissociation of the pharmaceutical from the complex in aqueous media was evaluated in pH 2 and 7, corresponding to the stomach and intestines respectively. Results revealed that such dissociation is dependent of the pH of the medium as well as that release of Ibuprofen from the matrices is dependent on the pH and the presence of the clay slows the dissociation of the drug from the matrix.