ABSTRACT
This paper reports the development, characterization and
O trabalho reporta o desenvolvimento, caracterização e estudo
Subject(s)
Humans , Chemistry, Pharmaceutical , Sulfasalazine/administration & dosage , Sulfasalazine/pharmacokinetics , Sulfasalazine/pharmacology , Drug Delivery Systems , Gastroenteritis/drug therapyABSTRACT
Neste trabalho, 2 diferentes procedimentosforam utilizados para a extração de lignina a partir do licor negro, caracterizando-se quimicamente as amostras de lignina obtidas em relação a umalignina comercial, visando a aplicação no desenvolvimento de sensores voltamétricos. A análise elementar, espectroscopia na região do infravermelho, análise térmica e caracterização eletroquímica do material mostraram que, tanto a origem da lignina quanto a metodologia de obtenção da mesma, a partir do licor negro, podem fornecer materiais com propriedades químicas distintas, embora possuam comportamento eletroquímico similar. Observou-se, também, que a lignina só pode ser armazenada na forma sólida,devido à oxidação pelo oxigênio dissolvidodurante o tempo em que a solução mãe é armazenada.No entanto, a oxidação dalignina é necessária quando se tem por objetivo o desenvolvimento de sensores voltamétricos, devido a predominância de carbonos sp2na estrutura químicaoxidada, condição em que se obtém maior condutividade. Constatou-se também a necessidade de utilizar um transdutor metálico para o desenvolvimento de eletrodos qumicamente modificados com este material, visto que os eletrodos de carbono modificados com lignina oxidada ou não oxidada não apresentaram atividade eletroquímica. Devido à pequena porcentagem de enxofre existente na estrutura química, a lignina oxidada tende a se organizar pelos grupamentos SH quando na presença de ouro, expondo os grupamentos quinônicos eletroativos. A lignina oxidada ainda foi utilizada no preparo de eletrodo de pasta de carbono com nanopartículas de ouro, na qual a lignina oxidada impregnada no grafite atua como redutor "in-situ" do ouro, permitindo o preparo de um sensor voltamétrico versátil, capaz de realizar a determinação de ácido ascórbico, dopamina, nitrito e iodato. No que tange ao comportamento eletroquímico de fármacos e estudos de interação fármaco-DNA, eletrodos de carbono foram modificados com DNAdupla fita com a finalidade de monitorar a interação DNA-Gemcitabina.O fármaco não apresentou atividade eletroquímica tanto na região positiva quanto na região negativa de potencial. A interação do mesmo com o DNA promove a condensação/agregação das duplas fitas do DNA em uma primeiraetapa, seguida da clivagem do nucleosídeo guanosina, formando guanina livre. O comportamento eletroquímico de leflunomida e sulfasalazina, dois fármacos aplicados ao tratamento da artrite reumatóide, foi estudado e mecanismos de oxidação foram propostos para cada fármaco
The chemical properties of samples of lignin, which were precipitated from black liquor using two different methodologies (precipitation with CO2 and H2SO4), were studied and the results compared to those obtained from a commercial lignin sample in order to prepare voltammetric sensors. The elementary analysis, infrared spectroscopy, thermal analysis and electrochemical characterization of the material demonstrated that both, the source of lignin and the precipitation method from the black liquor, can provide lignin samples with different chemical properties, although the electrochemical behavior of all samples has been the same. Lignin could only be stored in solid form as lignin in the black liquor is slowly and quantitatively oxidized by dissolved oxygen, preventing the extraction procedures. However, the lignin as extracted from black liquor cannot be used to modify solid electrodes due its high resistivity. The previous oxidation of the all material was necessary when the aim was its application on the sensors development. The electrical conductivity in the oxidized lignin was achieved, probably due to the predominance of sp2 hybridized carbon atoms, which improved orbital overlapping in the material. In addition, it was necessary to use a metallic transducer to produce electrodes modified with films of lignin with good electrochemical activity. The films drying time was also important parameter, which suggested a specific organization of lignin macromolecules over the electrode surface. Due to the small percentage of sulfur in the material, the oxidized lignin tended to be organized by the SH groups in the presence of metallic substrates, exposing its electroactive quinone groups. The oxidized lignin was further used to prepare carbon paste electrodes modified with gold nanoparticles, in which the impregnated oxidized lignin on graphite acted as an "in situ" reducing agent towards HAuCl4.The resulting composite allowed the preparation of a versatile voltammetric sensor, capable of detecting ascorbic acid, dopamine, nitrite and iodate. Regarding the electrochemical behavior and drug interaction studies DNA-molecule, carbon electrodes were modified with double strand DNA with the purpose of monitoring Gemcitabine-DNA interaction. The drug showed no electrochemical activity both, in the positive and the negative potential. The Gemcitabine-DNA interaction promoted condensation / aggregation of the double strand DNA in a first step, followed by cleavage of the nucleoside guanosine in the form of free guanine. In addition, the electrochemical behavior of sulfasalazine and leflunomide, two pharmacological compounds applied to the treatment of rheumathoid arthritis, were studied and their oxidation mechanisms were proposed
Subject(s)
DNA , Lignin/analysis , DNA Cleavage , Nucleosides , Sulfasalazine/administration & dosageSubject(s)
Female , Humans , Middle Aged , Antineoplastic Agents/adverse effects , Arthritis, Rheumatoid/etiology , Quinazolines/adverse effects , Adenocarcinoma/drug therapy , Antirheumatic Agents/administration & dosage , Arthritis, Rheumatoid/drug therapy , Drug Interactions , Lung Neoplasms/drug therapy , Prednisolone/administration & dosage , Sulfasalazine/administration & dosageABSTRACT
Ulcerative colitis (UC) is uncommon in Thailand. Few reports have been published and confirmation of the diagnosis was difficult. To make a firm diagnosis of UC in Thailand, long-term follow-up and demonstration of chronic and relapsing clinical courses should help to confirm the existence of UC in Thailand. OBJECTIVE: To review the demographic data, clinical presentation and clinical courses of the diagnosed UC cases in Thailand. MATERIAL AND METHOD: Diagnosed UC patients who were followed-up for longer than 3 months at the Diarrhea Clinic, Siriraj Hospital between 1988-2000 were included. RESULTS: Forty cases of UC were followed-up. The duration of follow-up ranged from 3-75 months (mean 27 months). Male to female ratio was 19:21 and age of onset varied from 13-77 years (mean 37.7 years). Extents of the disease was left-sided colitis in 58 per cent, left and right-sided colitis in 8 per cent, pancolitis in 21 per cent, proctosigmoiditis in 13 per cent and ileal involvement in 8 per cent. At presentation, the disease was mild in 28 per cent, moderate in 60 per cent, severe in 13 per cent and fulminant in 2. Clinical presentations were diarrhea in 97.5 per cent, lower GI bleeding in 17.5 per cent, abdominal pain in 50 per cent, fever in 27.5 per cent, weight loss in 62.5 per cent and extraintestinal manifestations in 20 per cent. Diagnoses were made in all cases by sigmoidoscopy plus barium enema or colonoscopy and biopsies were taken in all cases. Histologic findings supported the diagnoses in 69 per cent of cases. Seventy per cent responded to sulfasalazine or 5-ASA with or without corticosteroid, but in 30 per cent, azathioprine was added for a period during the treatment. Clinical courses of the diseases were chronic intermittent with remission and relapse in 44 per cent, chronic continuous activity without remission in 27 per cent, single episode without relapse in 27 per cent and acute fulminating course in 6 per cent. One patient died from fulminant pancolitis with colonic perforation. There was no colonic cancer in our cases throughout the follow-up period. CONCLUSIONS: UC is very uncommon in Thailand. Firm diagnosis of UC can be made through long-term follow-up and demonstration of chronic and relapsing clinical courses. The disease severity and extent of disease involvement was slightly different from that in Western countries. Incidence of extraintestinal manifestation was 20 per cent. Most cases responded to sulfasalazine, 5-ASA or corticosteroids.
Subject(s)
Adolescent , Adrenal Cortex Hormones/administration & dosage , Adult , Age Distribution , Age of Onset , Aged , Aged, 80 and over , Child , Colitis, Ulcerative/diagnosis , Colonoscopy , Female , Follow-Up Studies , Humans , Incidence , Male , Middle Aged , Risk Factors , Severity of Illness Index , Sex Distribution , Sulfasalazine/administration & dosage , Thailand/epidemiologyABSTRACT
Early intervention with slow acting anti-rheumatic drugs (SAARDs) has led to improvement in substantial proportion of rheumatoid arthritis (RA) patients. The present open, controlled study was designed to assess whether a combination of SAARDs offer any added benefit. Fifty-four adult RA patients were randomly allocated to methotrexate (MTX) (n = 27) and MTX plus sulphasalazine (SSZ) (n = 27) groups. The subjects were followed-up fortnightly for four weeks then monthly for six months. The disease activity was assessed with the help of 10 clinical and four laboratory indices. The improvement was graded as: minor, mild decreases in indices, non-steroidal anti-inflammatory drugs (NSAIDs) continued, physician's global assessment (PGA) decreased by one; marked, acceptable decreases in indices, NSAIDs being taken sparingly, PGA decreased by at least 2, and complete, all indices normalised and patients discontinued NSAIDs completely. The improvement was considered clinically important when marked or complete improvement occurred. Adverse drug reactions resulted in withdrawal of 4 subjects from the MTX + SSZ group and 1 from the control groups. Four and three subjects in the combined and MTX groups respectively were lost to follow-up. Subjects in both groups showed significant decline in all indices except hemoglobin and neutrophil count. The differences between the two groups in the pre-treatment and post-treatment values were insignificant. Complete, marked, minor and no improvement occurred in 4 (21%), 12 (63%), 3 (16%) & 0 in the MTX and in 11 (48%), 7 (30%), 4 (17%) & 1 (4%) in MTX + SSZ groups respectively. The differences in the rates of complete and clinically important improvement between the two groups were insignificant (P 0.1398 and 0.7092). The incidence of side effects was insignificantly higher in the MTX + SSZ group. Most of them were mild and transient. The combination of SAARDs offered little added advantage in RA. However, the higher rate of complete improvement in the combination group justifies trials including larger samples.
Subject(s)
Adult , Anorexia/chemically induced , Anti-Inflammatory Agents, Non-Steroidal/therapeutic use , Antirheumatic Agents/administration & dosage , Arthritis, Rheumatoid/drug therapy , Chi-Square Distribution , Drug Combinations , Female , Follow-Up Studies , Hemoglobins/drug effects , Humans , Incidence , Leukocyte Count , Male , Methotrexate/administration & dosage , Nausea/chemically induced , Neutrophils/drug effects , Prospective Studies , Remission Induction , Statistics, Nonparametric , Sulfasalazine/administration & dosageABSTRACT
Four children with chronic arthritis (3 juvenile rheumatoid arthritis and 1 juvenile ankylosing spondylitis) and poorly controlled chronic uveitis, were given sulphasalazine (SASP) therapy for a mean period of 3.3 years. Three patients showed an excellent response, as evidenced by a reduction of inflammatory cells in the anterior chamber of the eyes and improvement of visual acuity. The response occurred after a mean of 7.7 weeks. These data suggested SASP therapy may have a role in the treatment of chronic anterior uveitis in children with chronic arthritis.
Subject(s)
Adolescent , Adult , Antirheumatic Agents/administration & dosage , Arthritis, Juvenile/complications , Child , Chronic Disease , Female , Humans , Iridocyclitis/diagnosis , Male , Retrospective Studies , Spondylitis, Ankylosing/complications , Sulfasalazine/administration & dosageABSTRACT
Actualmente se dispone de fármacos de primera línea y de probada eficacia, como son los corticoesteroides, la sulfaslazina y el metronidazol; de 2a. línea como la azatioprina y la 6-mercaptopurina, cuya utilidad ya está demostrada y aún de 3a. línea que están comenzando a perfilarse, pero acerca de los cuales se requiere acumular mas experiencia. Es el caso del metotrexato y la ciclosporina. Estos recursos farmacológicos actualmente disponibles han modificado substancialmente la evolución, las complicaciones y el pronóstico de las enfermedades inflamatorias intestinales. En efecto, por una parte son capaces de inducir remisiones en un alto porcentaje de casos (probablemente mayor de 80 porciento) y lo que es tanto o más importante aún, mantener las remisiones obtenidas mediante tratamientos de largo plazo, con dosis reducidas, inductoras de bajos porcentajes de efectos adversos. Los resultados obtenidos con la sulfasalizina y especialmente con la azatioprina y la 6-mercaptopurina han sido particularmente satisfactorios en el tratamiento de la enfermedad de Crohn y muy especialmente en algunas de sus complicaciones, como las fístulas y las lesiones perianales que, hasta no hace mucho, constituían verdaderos desafíos médicos y quirúrgicos
Subject(s)
Humans , Colitis, Ulcerative/drug therapy , Crohn Disease/drug therapy , Enteritis/drug therapy , Mercaptopurine/administration & dosage , Adrenal Cortex Hormones/administration & dosage , Azathioprine/administration & dosage , Metronidazole/administration & dosage , Sulfasalazine/administration & dosageSubject(s)
Child , Colonoscopy , Enema , Female , Humans , India , Rectal Diseases/diagnosis , Sulfasalazine/administration & dosage , Ulcer/diagnosisABSTRACT
La sulfasalazina es un fármaco auxiliar en el tratamiento de la colitis ulcerativa crónica inespecifíca, enfermedad de Crohn, artritis reumatoide y psoriásica. Ha demostrado su utilidad en el tratamiento de lesiones cutáneas de psoriasis. Reportamos 20 pacientes con psoriasis en placas tratadas con 3-4 g/d de sulfasalazina durante 8 semanas. Nueve pacientes mostraron desaparición de sus lesiones y mejoría de más del 50 por ciento. Los efectos secundarios fueron náuseas en 8 pacientes y erupción macular en uno. La sulfasalazina es un fármaco que puede considerarse de elección en el tratamiento inicial de la psoriasis en placas
Subject(s)
Humans , Male , Female , Adult , Psoriasis/drug therapy , Sulfasalazine/therapeutic use , Psoriasis/physiopathology , Skin Diseases/drug therapy , Skin Diseases/physiopathology , Sulfasalazine/administration & dosageABSTRACT
La salazosukfapiridina (SASP) tiene una acción efectiva en la colitis ulcerosa (CU), al desdoblarse en el ciego en sulfapiridina (SP) y 5 aminosalicilato (5 ASA), siendo este último el que actúa por contacto sobre la mucosa colónica. El objetivo fué conocer los niveles séricos efectivos de la droga con eventual presencia o no de efectos colaterales, y también verificar fluctuaciones de los mismos en el intervalo de dosificación. Se estudiaron 10 niños de 6 a 16 años con CU, a quienes se les suministraba SASP de 0.50 a 2 gramos por día y cada 12 horas. Los niveles de SASP y SP en sangre se realizaron a las 6 y 12 horas de administrada la droga, y en materia fecal se cuantificó en recolección de 24 horas. Estos dosajes se realizaron por el método de Hansson y Sandberg. Los niveles lasmáticos de SP fueron a las 6 horas de 6.8 a 36.3 microng/ml (x 17.7-9.0 microng/ml) y a las 12 horas de 5.7 a 25.0 microng/ml (x 14.1 -7.2 microng/ml los de SASP fueron de 2.1 a 53.4 microng/ml (x 15.5-15.4microng/ml) a las 6 horas, y 3.9 a 70.7 microng/ml (x 14.0 -20.4 microng/ml) a las 12 horas. La excreción en materia fecal de SASP durante 24 horas fué de 17.4 a 236 mg., observándo-se una correlación significativa (r: 0.88) con la dosis administrada calculada en gramos por metro cuadrado de superficie corporal en 24 horas. Los niveles de SP y SASP no se correlacionaron con la dosis. Los niveles plasmáticos de SASp y SP no tuvieron diferencia significativa entre las 6 y 12 horas. Los niveles de SP no alcanzaron los mínimos ee toxicidad, no detectándose manifestaciones clíncias ni humorales adversas. Estos hallazgos sugieren que conociendo los niveles en plasma de la droga, la dosis puede ser modificada con mayor amplitud