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Development of ketoprofen delivery systems based on aqueous polyurethane dispersions

Leite, E.; Fernandes, I.; Ayres, E.; Barreiro, M.F.; Silva-Cunha, A.
Fonte: Instituto Politécnico de Bragança Publicador: Instituto Politécnico de Bragança
Tipo: Conferência ou Objeto de Conferência
ENG
Relevância na Pesquisa
37.56%
Ketoprofen (2-(3-benzoylphenyl) propionic acid) is a non-steroidal anti-inflammatory drug (NSAID) used to treat a wide range of acute and chronic inflammatory diseases, e.g., rheumatoid arthritis, osteoarthritis and ankylosing spondylitis. Its prolonged oral administration is associated with several gastrointestinal reactions such as irritation and ulceration. In this context, ketoprofen is a good candidate for controlled release administration systems. This work aims to test the suitability of using aqueous polyurethane dispersions (PUDs) as the base vehicle for producing ketoprofen controlled release systems. Polyester (polycaprolactone, PCL) and polyether (polypropylene glycol, PPG) based PUDs have been synthesized by using a modified pre-polymer method. Two chain extenders have been assayed (ethylenediamina (EDA) and hydrazine monohydrate (HYD)).

Influence of cellulose ether polymers on ketoprofen release from hydrophilic matrix tablets

Vueba, M. L.; Carvalho, L. A. E. Batista de; Veiga, F.; Sousa, J. J.; Pina, M. E.
Fonte: Universidade de Coimbra Publicador: Universidade de Coimbra
Tipo: Artigo de Revista Científica Formato: aplication/PDF
ENG
Relevância na Pesquisa
37.56%
The present work reports the study of different ketoprofen:excipient formulations, in order to determine the effect of the polymer substitution and type of diluent on the drug-release mechanism. Substituted cellulose--methylcellulose, hydroxypropylcellulose and hydroxypropylmethylcellulose were used as polymers, while lactose monohydrate and [beta]-cyclodextrin were tested as diluents. Distinct test formulations were prepared, containing 57.14% of ketoprofen, 20.00% of polymer, 20.29% of diluent, and 1.71% of talc/0.86% of magnesium stearate as lubricants. The tablets were tested for their drug content, weight variation, hardness, thickness, tensile strength, friability, swelling and release ratio. Polymers MC25 and HPC were found not to be appropriate for the preparation of modified release ketoprofen hydrophilic matrix tablets, while HPMC K15M and K100M showed to be advantageous. The analysis of the release profiles in the light of distinct kinetic models (zero-order, first-order, Higuchi and Korsmeyer-Peppas) led to the conclusion that the type of polymer did not influence the release mechanism of the drug. The mean dissolution time (MDT) was determined, the highest MDT value being obtained for HPMC formulations. Moreover, the drug-release process was found to be slightly influenced by the type of diluent...

Bio-Dis and the Paddle Dissolution Apparatuses Applied to the Release Characterization of Ketoprofen from Hypromellose Matrices

PEZZINI, Bianca Ramos; FERRAZ, Humberto Gomes
Fonte: SPRINGER Publicador: SPRINGER
Tipo: Artigo de Revista Científica
ENG
Relevância na Pesquisa
37.56%
The purposes of this work were: (1) to comparatively evaluate the effects of hypromellose viscosity grade and content on ketoprofen release from matrix tablets, using Bio-Dis and the paddle apparatuses, (2) to investigate the influence of the pH of the dissolution medium on drug release. Furthermore, since direct compression had not shown to be appropriate to obtain the matrices under study, it was also an objective (3) to evaluate the impact of granulation on drug release process. Six formulations of ketoprofen matrix tablets were obtained by compression, with or without previous granulation, varying the content and viscosity grade of hypromellose. Dissolution tests were carried out at a fixed pH, in each experiment, with the paddle method (pH 4.5, 6.0, 6.8, or 7.2), while a pH gradient was used in Bio-Dis (pH 1.2 to 7.2). The higher the hypromellose viscosity grade and content were, the lower the amount of ketoprofen released was in both apparatuses, the content effect being more expressive. Drug dissolution enhanced with the increase of the pH of the medium due to its pH-dependent solubility. Granulation caused an increase in drug dissolution and modified the mechanism of the release process.

Analgesia preemptiva do cetoprofeno e do parecoxibe em cirurgia para remoção de terceiros molares inclusos; Preemptive analgesia of the ketoprofen and parecoxib in the surgery to removal of impacted third molar teeth

Arantes, Viviana Moraes Neder
Fonte: Biblioteca Digitais de Teses e Dissertações da USP Publicador: Biblioteca Digitais de Teses e Dissertações da USP
Tipo: Tese de Doutorado Formato: application/pdf
Publicado em 03/10/2006 PT
Relevância na Pesquisa
37.8%
Este trabalho prospectivo, duplo-cego randomizado, avaliou o efeito da analgesia preemptiva do cetoprofeno e do parecoxibe. Sessenta pacientes foram submetidos à cirurgia para remoção de terceiros molares inferiores bilaterais inclusos, sendo operado um lado de cada vez. O paciente foi seu próprio controle. Os pacientes foram separados em dois grupos de 30 pacientes. No grupo parecoxibe, na primeira operação foi usado o parecoxibe ou placebo, endovenoso, 30 minutos antes da cirurgia e imediatamente após a operação foi feita a administração do placebo ou parecoxibe, garantindo ao paciente receber parecoxibe antes ou após a operação. O lado oposto foi operado após duas semanas da primeira cirurgia e o paciente que havia recebido parecoxibe antes e placebo depois da operação recebeu placebo antes e parecoxibe depois da operação e o que havia recebido placebo antes e parecoxibe depois recebeu parecoxibe antes e placebo depois. Nos 30 pacientes do grupo cetoprofeno, o modelo foi o mesmo, substituindo-se apenas o parecoxibe pelo cetoprofeno. O paciente pôde utilizar como medicação resgate a dipirona, sempre que necessário para controlar a dor pós-operatória. Após a operação foi fornecido para todos os pacientes um questionário...

Transition-metal catalyzed synthesis of ketoprofen

Ramminger, Carolina; Zim, Danilo; Lando, Vanusa Regina; Fassina, Viviane; Monteiro, Adriano Lisboa
Fonte: Universidade Federal do Rio Grande do Sul Publicador: Universidade Federal do Rio Grande do Sul
Tipo: Artigo de Revista Científica Formato: application/pdf
ENG
Relevância na Pesquisa
37.56%
Reações catalisadas por complexos de metais de transição tais como carbonilação, hidrovinilação e hidrogenação foram empregadas na síntese do ácido -(3-benzoilfenil)propanóico (Cetoprofeno). Acoplamento do tipo Heck entre 3-bromobenzofenona e etileno conduziu à 3-vinilbenzofenona que na seqüência, por carbonilação catalisada por paládio, foi transformada no -(3- benzoilfenil)propanoato de isopropila com rendimento de 95% e regiosseletividade >99,5%. Hidrólise deste éster conduziu ao Cetoprofeno com 90% de rendimento. Cetoprofeno foi também obtido em duas etapas a partir da 3-vinilbenzofenona via reação de hidrovinilação catalisada por níquel que conduz seletivamente ao 3-(3’-benzoilfenil)-1-buteno (96%), seguido por oxidação desta olefina em ácido. A 3-etenilbenzofenona pôde ser sintetizada a partir da 3-bromobenzofenona via uma reação de acoplamento catalisada por paládio. Este alcino foi carabonilado em presença de paládio conduzindo regiosseletivamente (97%) ao -(3-benzoilfenil)acrilato de metila. A hidrólise do éster conduz ao ácido -(3-benzoilfenil)acrílico que foi então hidrogenado enantiosseletivamente ao (S)-Cetoprofeno (95% e.e.) usando um complexo Ru-(S)-BINAP como catalisador.; Transition metal-catalyzed reactions including carbonylations...

Thermal and spectroscopic studies on solid Ketoprofen of lighter trivalent lanthanides

Galico, D. A.; Holanda, B. B.; Perpetuo, G. L.; Schnitzler, E.; Treu-Filho, O.; Bannach, Gilbert
Fonte: Springer Publicador: Springer
Tipo: Artigo de Revista Científica Formato: 371-379
ENG
Relevância na Pesquisa
37.56%
Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP); Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq); Processo FAPESP: 10/10931-3; Solid-state Ln(L)(3) compounds, where Ln stands for trivalent La, Ce, Pr, Nd, Sm, Eu, and L is ketoprofen have been synthesized. Thermogravimetry (TG), differential thermal analysis (DTA), differential scanning calorimetry (DSC) as well as X-ray diffraction powder (DRX) patterns, Fourier transformed infrared spectroscopy (FTIR), and other methods of analysis were used to study solid Ketoprofen of lighter trivalent lanthanides. The results provided information of the composition, dehydration, coordination mode, structure, thermal behavior, and thermal decomposition. The theoretical and experimental spectroscopic study suggests that the carboxylate group of ketoprofen is coordinate to metals as bidentate bond.

Renal histology and immunohistochemistry after acute hemorrhage in rats under sevoflurane and ketoprofen effect

Guedes Jr, Francisco Sobreira; Cruz, Deyvid Santos da; Rodrigues, Marcela Marcondes Pinto; Silva, Leopoldo Muniz da; Amorim, Renée Laufer; Vianna, Pedro Thadeu Galvão; Castiglia, Yara Marcondes Machado
Fonte: Sociedade Brasileira para o Desenvolvimento da Pesquisa em Cirurgia Publicador: Sociedade Brasileira para o Desenvolvimento da Pesquisa em Cirurgia
Tipo: Artigo de Revista Científica Formato: 37-42
ENG
Relevância na Pesquisa
37.44%
OBJETIVO: Investigar a influência do inibidor não-seletivo da ciclooxigenase, cetoprofeno (ceto) intravenoso, em alterações histológicas e dos níveis das citocinas renais - fator α de necrose tumoral (TNF- α) e interleucina 1 (IL-1) - após hemorragia de 30% da volemia (10%, três vezes, em intervalos de 10 min). MÉTODOS: Sob anestesia com sevoflurano (sevo), os grupos sevo e sevo+ceto (10 ratos cada) foram preparados cirurgicamente para leitura de pressão arterial média (PAM) e administração de solução de Ringer (5 mL/kg/h) e de cetoprofeno (1,5 mg/kg), no início da anestesia, no grupo sevo+ceto. Mediu-se temperatura retal continuamente. Os valores de temperatura e PAM foram observados antes da primeira hemorragia (T1), após a terceira hemorragia (T2) e 30 min após T2 (T3). Realizada nefrectomia bilateral nos dois grupos para análise histológica e imuno-histoquímica. RESULTADOS: Nos dois grupos, temperatura e PAM diminuíram com relação aos valores basais. Hipotermia foi mais acentuada no grupo sevo (p=0,0002). Necrose tubular foi mais frequente no grupo sevo (p=0,02). As citocinas estiveram igualmente presentes nos rins dos dois grupos. CONCLUSÃO: Cetoprofeno foi mais protetor no rim de rato durante anestesia com sevoflurano e hipovolemia...

Evaluation of adverse effects of long-term oral administration of carprofen, etodolac, flunixin meglumine, ketoprofen, and meloxicam in dogs

Luna, Stelio P.L.; Basílio, Ana C.; Steagall, Paulo V.M.; Machado, Luciana P.; Moutinho, Flávia Q.; Takahira, Regina K.; Brandão, Cláudia V.S.
Fonte: Universidade Estadual Paulista Publicador: Universidade Estadual Paulista
Tipo: Artigo de Revista Científica Formato: 258-264
ENG
Relevância na Pesquisa
37.71%
Objective - To evaluate adverse effects of long-term oral administration of carprofen, etodolac, flunixin meglumine, ketoprofen, and meloxicam in dogs. Animals - 36 adult dogs. Procedures - Values for CBC, urinalysis, serum biochemical urinalyses, and occult blood in feces were investigated before and 7, 30, 60, and 90 days after daily oral administration (n = 6 dogs/group) of lactose (1 mg/kg, control treatment), etodolac (15 mg/kg), meloxicam (0.1 mg/kg), carprofen (4 mg/kg), and ketoprofen (2 mg/kg for 4 days, followed by 1 mg/kg daily thereafter) or flunixin (1 mg/kg for 3 days, with 4-day intervals). Gastroscopy was performed before and after the end of treatment. Results - For serum γ-glutamyltransferase activity, values were significantly increased at day 30 in dogs treated with lactose, etodolac, and meloxicam within groups. Bleeding time was significantly increased in dogs treated with carprofen at 30 and 90 days, compared with baseline. At 7 days, bleeding time was significantly longer in dogs treated with meloxicam, ketoprofen, and flunixin, compared with control dogs. Clotting time increased significantly in all groups except those treated with etodolac. At day 90, clotting time was significantly shorter in flunixin-treated dogs...

Spectroscopic, luminescence and in vitro biological studies of solid ketoprofen of heavier trivalent lanthanides and yttrium(III)

Galico, D. A.; Lahoud, M. G.; Davolos, M. R.; Frem, R. C. G.; Fraga-Silva, T. F. C.; Venturini, J.; Arruda, M. S. P.; Bannach, G.
Fonte: Elsevier B.V. Publicador: Elsevier B.V.
Tipo: Artigo de Revista Científica Formato: 160-166
ENG
Relevância na Pesquisa
37.64%
Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP); Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES); Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq); Processo FAPESP: 12/21450-1; Solid-state compounds of the general formulae [ML3] (M = Gd, Tb, Dy, Ho, Er, Tm, Yb, Lu, Y; L = ketoprofen) were synthesized and characterized using infrared, diffuse reflectance and luminescence spectroscopies. IR data suggested that the carboxylate group in ketoprofen is coordinated to the metals as a bidentate ligand. The triplet state energy level was determined using the Gd3+ complex, which exhibited a ketoprofen blue luminescence when excited in the UV region. The compound containing Tb3+ ion was sensitized by the ligand and emitted in the green region of the visible spectrum. On the other hand, for the analogous species containing the dysprosium ion, a competition for luminescence between the Dy3+ and the ligand levels was observed. Finally, Tm3+ complex exhibits only ligand luminescence. These optical behaviors are discussed based on rare earth energy diagrams. In addition, the compounds were evaluated for their anti-inflammatory activities. All the compounds showed a higher production of H2O2 and IL-10 than the ketoprofen...

The cytoprotective effect of a nitric oxide donor drug on gastric mucous membrane of rats treated with ketoprofen, a non-steroidal anti-inflammatory drug

Villa,Afonso Luiz; Reginaldo,Ceneviva; Viaro,Fernanda; Ramalho,Fernando; Campos,Antonio Dorival; Evora,Paulo Roberto B.
Fonte: Instituto Brasileiro de Estudos e Pesquisas de Gastroenterologia - IBEPEGE ; Colégio Brasileiro de Cirurgia Digestiva - CBCD ; Sociedade Brasileira de Motilidade Digestiva - SBMD ; Federação Brasileira de Gastroenterologia - FBG; Sociedade Brasileira de Hepatologia - SBH; Sociedade Brasileira de Endoscopia Digestiva - SOBED Publicador: Instituto Brasileiro de Estudos e Pesquisas de Gastroenterologia - IBEPEGE ; Colégio Brasileiro de Cirurgia Digestiva - CBCD ; Sociedade Brasileira de Motilidade Digestiva - SBMD ; Federação Brasileira de Gastroenterologia - FBG; Sociedade Brasileira de Hepatologia - SBH; Sociedade Brasileira de Endoscopia Digestiva - SOBED
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/09/2006 EN
Relevância na Pesquisa
37.76%
BACKGROUND: Non-steroidal anti-inflammatory drugs are considered today a very important group of medication, with a wide variety of therapeutic use, in different areas of modern medicine. Despite their beneficial effects on the patient, these drugs show a high incidence of side effects, mainly in the gastrointestinal tract. The physiopathological mechanisms of non-steroidal anti-inflammatory drugs induced lesions and the gastric mucosa defense mechanism became an important source for medical research, especially those which try to evaluate the role of nitric oxide as a cytoprotective agent. AIM: To define a possible cytoprotective effect of a nitric oxide donor, isosorbide dinitrate, on the gastric mucous of rats submitted to non-steroidal anti-inflammatory drugs ketoprofen treatment. METHODS: Adult male Wistar rats, previously submitted to starvation for 24 hours and divided in three groups: group I (standard): animals that received isotonic saline solution intragastric by gavage and intravenous. Group II (control-ketoprofen): animals that received isotonic saline solution intragastric by gavage and ketoprofen intravenous. Group III (nitrate/ketoprofen): animals that received 2mM solution of isosorbide dinitrate intragastric by gavage and ketoprofen intravenous. Later on...

Evaluation of the neuroprotective effect of ketoprofen on rats submitted to permanent focal brain ischemia

Silva,Manoel Nunes da; Colli,Benedicto Oscar; Coimbra,Norberto Cysne; Coutinho Netto,Joaquim
Fonte: Academia Brasileira de Neurologia - ABNEURO Publicador: Academia Brasileira de Neurologia - ABNEURO
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/12/2007 EN
Relevância na Pesquisa
37.56%
OBJECTIVE: To study the neurobehavioral, biochemical and histopathological consequences of permanent focal brain ischemia, and the putative neuroprotective action of ketoprofen. METHOD: One-hundred-and-three Wistar rats divided into groups A and B were respectively submitted to 48 hours and 15 days of ischemia. Each group was divided into 4 subgroups: ischemic not treated, ischemic treated, sham not treated, and sham treated. Ischemic animals had the left middle cerebral artery coagulated. Ketoprofen was administered to treated subgroups 15 minutes before arterial coagulation (manipulation in the sham group). RESULTS: Exploratory activity and defecation were reduced in all ischemic animals in the first postoperative days and constant histopathological changes were observed in each group. The total brain glutamate levels were higher in treated animals 48 hours after surgery. CONCLUSION: No clear parallelism among behavioral, biochemical and histopathological findings was observed. Ketoprofen demonstrated no neuroprotective effect on the behavioral or histopathological aspects of focal permanent brain ischemia.

A randomized, double blind comparison of pethidine and ketoprofen as adjuvants for lignocaine in intravenous regional anaesthesia

Desai,Sameer N.; Santhosh,M.C.B.
Fonte: Sociedade Brasileira de Anestesiologia Publicador: Sociedade Brasileira de Anestesiologia
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/08/2014 EN
Relevância na Pesquisa
37.64%
BACKGROUND AND OBJECTIVES: A review of all the adjuncts for intravenous regional anaesthesia concluded that there is good evidence to recommend NonSteroidal Anti-Inflammatory agents and pethidine in the dose of 30 mg dose as adjuncts to intravenous regional anaesthesia. But there are no studies to compare pethidine of 30 mg dose to any of the NonSteroidal Anti-Inflammatory agents. METHODS: In a prospective, randomized, double blind study, 45 patients were given intravenous regional anaesthesia with either lignocaine alone or lignocaine with pethidine 30 mg or lignocaine with ketprofen 100 mg. Fentanyl was used as rescue analgesic during surgery. For the first 6 h of postoperative period analgesia was provided by fentanyl injection and between 6 and 24 h analgesia was provided by diclofenac tablets. Visual analogue scores for pain and consumption of fentanyl and diclofenac were compared. RESULTS: The block was inadequate for one case each in lignocaine group and pethidine group, so general anaesthesia was provided. Time for the first dose of fentanyl required for postoperative analgesia was significantly more in pethidine and ketoprofen groups compared to lignocaine group (156.7 ± 148.8 and 153.0 ± 106.0 vs. 52.1 ± 52.4 min respectively). Total fentanyl consumption in first 6 h of postoperative period was less in pethidine and ketoprofen groups compared to lignocaine group (37.5 ± 29.0 mcg...

Presurgical ketoprofen, but not morphine, dipyrone, diclofenac or tenoxicam, preempts post-incisional mechanical allodynia in rats

Prado,W.A.; Pontes,R.M.C.
Fonte: Associação Brasileira de Divulgação Científica Publicador: Associação Brasileira de Divulgação Científica
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/01/2002 EN
Relevância na Pesquisa
37.64%
The treatment of pain before it initiates may prevent the persistent pain-induced changes in the central nervous system that amplify pain long after the initial stimulus. The effects of pre- or postoperative intraperitoneal administration of morphine (2 to 8 mg/kg), dipyrone (40 and 80 mg/kg), diclofenac (2 to 8 mg/kg), ketoprofen (10 and 20 mg/kg), and tenoxicam (10 and 20 mg/kg) were studied in a rat model of post-incisional pain. Groups of 5 to 8 male Wistar rats (140-160 g) were used to test each drug dose. An incision was made on the plantar surface of a hind paw and the changes in the withdrawal threshold to mechanical stimulation were evaluated with Von Frey filaments at 1, 2, 6 and 24 h after the surgery. Tenoxicam was given 12 or 6 h preoperatively, whereas the remaining drugs were given 2 h or 30 min preoperatively. Postoperative drugs were all given 5 min after surgery. No drug abolished allodynia when injected before or after surgery, but thresholds were significantly higher than in control during up to 2 h following ketoprofen, 6 h following diclofenac, and 24 h following morphine, dipyrone or tenoxicam when drugs were injected postoperatively. Significant differences between pre- and postoperative treatments were obtained only with ketoprofen administered 30 min before surgery. Preoperative (2 h) intraplantar...

Subcutaneous administration of ketoprofen delays Ehrlich solid tumor growth in mice

Souza,C.M.; Auler,P.A.; Reis,D.C.; Lavalle,G.E.; Ferreira,E.; Cassali,G.D.
Fonte: Universidade Federal de Minas Gerais, Escola de Veterinária Publicador: Universidade Federal de Minas Gerais, Escola de Veterinária
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/10/2014 EN
Relevância na Pesquisa
37.71%
Ketoprofen, a nonsteroidal anti-inflammatory drug (NSAID) has proven to exert anti-inflammatory, anti-proliferative and anti-angiogenic activities in both neoplastic and non-neoplastic conditions. We investigated the effects of this compound on tumor development in Swiss mice previously inoculated with Ehrlich tumor cells. To carry out this study the solid tumor was obtained from cells of the ascites fluid of Ehrlich tumor re-suspended in physiological saline to give 2.5x106 cells in 0.05mL. After tumor inoculation, the animals were separated into two groups (n = 10). The animals treated with ketoprofen 0.1µg/100µL/animal were injected intraperitoneally at intervals of 24h for 10 consecutive days. Animals from the control group received saline. At the end of the experiment the mice were killed and the tumor removed. We analyzed tumor growth, histomorphological and immunohistochemical characteristics for CDC47 (cellular proliferation marker) and for CD31 (blood vessel marker). Animals treated with the ketoprofen 0.1µg/100µL/animal showed lower tumor growth. The treatment did not significantly influence the size of the areas of cancer, inflammation, necrosis and hemorrhage. Moreover, lower rates of tumor cell proliferation were observed in animals treated with ketoprofen compared with the untreated control group. The participation of ketoprofen in controlling tumor malignant cell proliferation would open prospects for its use in clinical and antineoplasic therapy.

Renal histology and immunohistochemistry after acute hemorrhage in rats under sevoflurane and ketoprofen effect

Guedes Jr,Francisco Sobreira; Cruz,Deyvid Santos da; Rodrigues,Marcela Marcondes Pinto; Silva,Leopoldo Muniz da; Amorim,Renée Laufer; Vianna,Pedro Thadeu Galvão; Castiglia,Yara Marcondes Machado
Fonte: Sociedade Brasileira para o Desenvolvimento da Pesquisa em Cirurgia Publicador: Sociedade Brasileira para o Desenvolvimento da Pesquisa em Cirurgia
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/01/2012 EN
Relevância na Pesquisa
37.44%
PURPOSE: To investigate the influence of intravenous nonselective cyclooxygenase inhibitor, ketoprofen (keto), on kidney histological changes and kidney cytokines, tumor necrosis factor-α (TNF-α) and interleukin-1 (IL-1), levels after hemorrhage of 30% of volemia (three times 10%, intervals of 10 min) in rats. METHODS: Under sevoflurane (sevo) anesthesia, sevo and sevo+keto groups (10 rats each) were instrumented for Ringer solution (5mL/kg/h) administration and mean arterial pressure (MAP) evaluation, plus keto (1.5mg/kg) administration in sevo+keto group in the beginning of anesthesia. Rectal temperature was continuously measured. The baseline data of temperature and MAP were collected at the first hemorrhage (T1), the third hemorrhage (T2) and 30min after T2 (T3). Bilateral nephrectomy was achieved for histology and immunohistochemistry. RESULTS: In both groups, temperature and MAP diminished from initial values. Hypothermia was greater in sevo group (p=0.0002). Tubular necrosis was more frequent in sevo group (p=0.02). The studied cytokines were equally present in the kidneys of both groups. CONCLUSION: Ketoprofen was more protective to the rat kidney in condition of anesthesia with sevoflurane and hypovolemia, but it seems that TNF-α and IL-1 were not involved in that protection.

Desenvolvimento e caracterização de sistemas multiparticualdos de liberação prolongada para o antiinflamatório cetoprofeno; Development and characterization of systems multiparticualdos of extended release for the anti-inflammatory ketoprofen

OLIVEIRA, Rodinelli Borges de
Fonte: Universidade Federal de Goiás; BR; UFG; Mestrado em Ciências da Saúde; Ciências da Saúde - Medicina Publicador: Universidade Federal de Goiás; BR; UFG; Mestrado em Ciências da Saúde; Ciências da Saúde - Medicina
Tipo: Tese de Doutorado Formato: application/pdf
POR
Relevância na Pesquisa
37.86%
Ketoprofen is a nonsteroid anti-inflammatory drug (NSAID) which is used in rheumatic disorders and in mild to moderate pain. Ketoprofen has a short biological half life and the commercially available conventional release formulations require dosages to be administered at least 2-3 times a day. Due to these characteristics, ketoprofen is a good candidate for the preparation of controlled release formulations. In this work, a multiparticulate sustained release dosage form containing ketoprofen in a carnauba wax matrix was developed. Particles were prepared by emulsion congealing technique, spray drying, fluidized bed and conventional granulation. Hydroxypropylmethylcellulose (HPMC) and carnauba wax were used in the formulations as the main ingredients to promote sustained release. Particles were evaluated for their rheological properties, morphology and drug release characteristics. For the emulsion congealing technique, system variables were optimized using fractional factorial and response surface experimental design in order to obtain spherical particles with high drug load and sustained drug release profile. The optimized particles had an average diameter of approximately 200 μm, 50% (w/w) drug load, good flow properties and a prolonged release profile (up to 24 hours) for ketoprofen. Particles prepared with HPMC 2208 by spray drying...

Desenvolvimento de comprimidos contendo pellets revestidos para liberação cólon específica de cetoprofeno; Development of tablets contain coated pellets for colon specific release of ketoprofen

Alencar, Rodrigo Gomes de
Fonte: Universidade Federal de Goiás; Brasil; UFG; Programa de Pós-graduação em Ciências Farmacêuticas (FF); Faculdade Farmácia - FF (RG) Publicador: Universidade Federal de Goiás; Brasil; UFG; Programa de Pós-graduação em Ciências Farmacêuticas (FF); Faculdade Farmácia - FF (RG)
Tipo: Dissertação Formato: application/pdf
POR
Relevância na Pesquisa
37.76%
Ketoprofen is a nonsteroidal anti-inflammatory drug used for the treatment of mild to moderate pain in chronic inflammatory conditions. Due to its superior potency ketoprofen can be used in the treatment of inflammatory bowel disease (IBD). The treatment of IBD becomes safer and more effective when the drug is incorporated into colon-specific drug delivery systems. Pellets are multiparticulate solid dosage forms extensively investigated as colon-specific drug delivery systems. Pellets can be introduced into capsules or compressed into tablets. The industrial production of tablets containing pellets has several advantages when compared to the production of capsules. However, the compression of the pellets should not affect the release of the drug and the tablets should quickly disintegrate following administration. Therefore, the aim of this study was to develop tablets containing ketoprofen coated pellets for colon-specific drug release. For this, pellets were produced by extrusion and spheronization technique containing 40% (w / w) ketoprofen. Ketoprofen pellets obtained were coated with two different pH - dependent polymers derived from methacrylic acid (Opadry ® k 94 or Eudragit ® FS 30D) with weight gains of 10 or 20% (w / w). The coated pellets were then compressed under different pellets’ amounts and different compression forces. An extra- granular mixture of lactose and microcrystalline cellulose was used as compression aid. The in vitro release of ketoprofen from the systems obtained was evaluated in Bio Dis ® apparatus. The morphological and physical properties of pellets and tablets were assessed. The Eudragit ® FS 30 D coated pellets with weight gains of 10 or 20% showed higher efficiency of colon-specific delivery (94 %)...

Evaluation of digital optical density of bone repair in rats medicated with ketoprofen

Martins,Márcia Valéria; Silva,Marcos André dos Santos da; Medici Filho,Edmundo; Moraes,Luiz Cesar de; Castilho,Julio Cezar de Melo; Rocha,Rosilene Fernandes da
Fonte: Fundação Odontológica de Ribeirão Preto Publicador: Fundação Odontológica de Ribeirão Preto
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/12/2005 EN
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37.76%
The purpose of this study was to evaluate the influence of ketoprofen on bone repair process in tibiae of rats by means of analysis of the digital optical density. Twenty Wistar rats were assigned to two groups: an untreated control group and a group treated with ketoprofen. The experimental procedures comprised the following stages: general anesthesia, preparation of a unicortical bone defect on the left tibia of each rat, medication with ketoprofen and radiographic examination. Digital radiographic images were acquired using Visualix GX-S-HDI™ digital sensor and an x-ray equipment. Radiographs were taken at baseline, 7, 14, 21 and 30 days postoperatively and the optical density (OD) was evaluated using the Vix winTM 1.4 system. The mean values of OD readings were analyzed statistically by ANOVA and Tukey's test with significance level set at á=5%. The control group showed a statistically significant correlation (p=0.001) between time and optical density, while the ketoprofen group exhibited a weak and not statistically significant correlation (p=0.100). The control group presented the smallest OD ratios at days 1 and 7, and the greatest OD ratios at days 14, 21 and 30, with statistically significant difference (p=0.001). There was no significant differences (p=0.100) among the OD ratios in the ketoprofen group...

Transition-metal catalyzed synthesis of Ketoprofen

Ramminger,Carolina; Zim,Danilo; Lando,Vanusa R.; Fassina,Viviane; Monteiro,Adriano L.
Fonte: Sociedade Brasileira de Química Publicador: Sociedade Brasileira de Química
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/04/2000 EN
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Transition metal-catalyzed reactions including carbonylations, hydrovinylations and hydrogenations have been applied in the synthesis of alpha-(3-benzoylphenyl)propanoic acid (Ketoprofen). 3-Vinylbenzophenone was obtained from 3-bromobenzophenone by a Pd-catalyzed Heck coupling reaction. Pd-catalyzed carbonylation of this olefin gave the isopropyl alpha-(3-benzoylphenyl) propionate in high yield (95%) and with high regioselectivity (>99.5%). Ketoprofen was obtained in 90% yield by hydrolysis of the isopropyl ester. It was also obtained in two steps from 3-vinylbenzophenone by a Ni-catalyzed hydrovinylation selectively affording 3-(3'-benzoylphenyl)-1-butene, followed by an oxidation. 3-Ethynylbenzophenone was obtained from 3-bromobenzophenone by Pd-catalyzed coupling reaction. By means of a Pd-catalyzed carbonylation, this alkyne was converted regioselectively (97%) into methyl alpha-(3-benzoylphenyl) acrylate (93% yield). Hydrolysis of the ester afforded the alpha-(3-benzoylphenyl)acrylic acid. Asymmetric hydrogenation of this acid to give (S)-ketoprofen in 95% optical yield was achieved using a chiral Ru-(S)-BINAP catalyst.

Enantioselective extraction of ketoprofen enantiomers using ester alcohol R, R-di-tartarates or S, S-di-tartarates as chiral selector

Huang,K.; Jiao,F.; Liu,S.; Li,X.; Huang,D.
Fonte: Latin American applied research Publicador: Latin American applied research
Tipo: Artigo de Revista Científica Formato: text/html
Publicado em 01/07/2006 EN
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Distribution behavior of ketoprofen enantiomers was examined in a two-phase system containing R, R-di-tartarates or S, S-di-tartarates. The influences of different alkyl chain of R, R-di-tartarates or S, S-di-tartarates, concentrations of R, R-di-tartarate, organic solvent and content of methanol on partition coefficient and separation factor were investigated, respectively. The experimental results show that R, R-di-tartarates studied all form more stable diastereomeric complexes with ketoprofen S-enantiomer than with R-enantiomer. The partition coefficients and enantioselectivity generally increase with the addition of length of alkyl chain of alcohol. The concentration of chiral selector and methanol also have bigger influences on enantioselectivity.