Dissolution profile of different brands of low solubility drugs available in the Nigerian and Brazilian pharmaceutical markets / Dissolution profile of different brands of low solubility drugs available in the Nigerian and Brazilian pharmaceutical markets

The purpose of this work was to elaborate a diagnosis of the dissolution test in Africa in comparison with Brazil, evaluating the dissolution profile of low solubility drugs such as albendazole, ibuprofen, furosemide, glibenclamide, hydrochlorothiazide and carvedilol to ascertain their quality. The dissolution profiles were evaluated by utilizing the United States Pharmacopeia (USP). The glibenclamide medicine was evaluated according to the Food and Drug Administration (FDA), while a dissolution method was developed for the carvedilol medicine. A filter selection test for all the drugs showed that cannula is suitable for all, except for carvedilol, which is centrifuged. The various brands of Nigerian and Brazilian medicines tested showed some statistical differences. The suitable conditions that allowed the dissolution of carvedilol to be determined were the USP type II apparatus at 75 rpm containing 900 mL of acetate buffer, pH 4.5. The results of the dissolution test showed that out of the 17 different brands of Brazilian medicines and 17 different products from Nigeria, 94.12% and 58.82% passed respectively

O objetivo deste trabalho foi elaborar um diagnóstico do teste de dissolução na África em comparação ao Brasil, avaliando o perfil de dissolução de medicamentos de baixa solubilidade como albendazol, ibuprofeno, furosemida, glibenclamida, hidroclorotiazida e carvedilol para verificar sua qualidade.Os perfis de dissolução foram avaliados utilizando a Farmacopeia dos Estados Unidos (USP). O medicamento glibenclamida foi avaliado de acordo com a Food and Drug Administration (FDA), enquanto um método de dissolução foi desenvolvido para o medicamento carvedilol.Um teste de seleção de filtro para todos os medicamentos mostrou que a cânula é adequada para todos, exceto para o carvedilol, que é centrifugado. As diversas marcas de medicamentos Nigerianos e Brasileiros testadas apresentaram algumas diferenças estatísticas. As condições adequadas que permitiram a determinação da dissolução do carvedilol foram o aparelho USP tipo II a 75 rpm contendo 900 mL de tampão acetato, pH 4,5. Os resultados do teste de dissolução mostraram que das 17 diferentes marcas de medicamentos brasileiros e 17 diferentes produtos da Nigéria, 94,12% e 58,82% foram aprovados, respectivamente

Solid Phase Extraction and Simultaneous Chromatographic Quantification of some Non-steroidal Anti-inflammatory Drug Residues; an Application in Pharmaceutical Industrial Wastewater Effluent

Abstract Two sensitive and selective methods were developed for the simultaneous determination of four commonly used non-steroidal anti-inflammatory drugs (NSAIDs), namely; paracetamol (PCM), diclofenac sodium (DCF), ibuprofen (IBP), and indomethacin (IND) in wastewater effluents. The first method used HPLC for the determination of the studied drugs using a mobile phase consisting of phosphate buffer (pH 3.0) and acetonitrile at a flow rate of 1 mL/min. in gradient elution mode and detection at 220 nm. The separation process was performed on BDS Hypersil Cyano column (250 x 4.6 mm, 5 µm). The second method was a TLC-densitometric one which was performed using n-Hexane: ethyl acetate: acetic acid in the ratio (6:3.5:0.5) as a developing system. The proposed chromatographic methods were successfully applied for the selective determination of the four studied drugs in simulated and real pharmaceutical wastewater samples after their solid-phase extraction

Reacciones adversas a montelukast: de la teoría a la práctica. Serie de casos / Adverse drug reactions of montelukast: from theory to practice. Case report

El montelukast se utiliza ampliamente en el tratamiento de sibilancias recurrentes y/o asma. Están descritas numerosas reacciones adversas medicamentosas (RAM) en niños relacionadas con montelukast; se destacan las neuropsiquiátricas. Realizamos un estudio observacional, retrospectivo, descriptivo, sobre RAM relacionadas con montelukast. Entre enero de 2012 y diciembre de 2017, en la Unidad de Neumonología Pediátrica se trataron con Montelukast 348 pacientes; de ellos, 20 presentaron RAM. Los síntomas más frecuentes fueron insomnio (n = 7), hiperactividad (n = 4), pesadillas (n = 3), dolor abdominal (n = 2) y parestesias en extremidades (n = 2). Se presentaron desde días hasta meses tras iniciar el tratamiento, y desaparecieron tras su suspensión. Se destacan dos pacientes con parestesias en extremidades, síntoma no descrito antes en niños. El 5,7 % de los pacientes tratados con montelukast presentaron RAM que requirieron suspender el tratamiento. Los trastornos del sueño fueron los más frecuentes.

Montelukast is widely used in recurrent wheezing and/or asthma treatment. Several adverse drug reactions (ADRs) have been described in children related to montelukast. Neuropsychiatric reactions are one of the most important. We designed an observational, retrospective, descriptive study on ADRs related to montelukast in the Pediatric Pulmonology Unit, Hospital Universitario Miguel Servet, Zaragoza, Spain. Between January 2012 and December 2017, in the Pediatric Pulmonology Unit, 348 patients were treated with Montelukast; of them, 20 presented RAM. The main symptoms described were insomnia (n = 7), hyperactivity (n = 4), nightmares (n = 3), abdominal pain (n = 2) and paraesthesia in extremities (n = 2). They appeared from the first days to months after the start of treatment and disappeared after stopping it. Two patients presented limb paresthesia, not described previously in children. The 5.7 % of our patients treated with montelukast had ADRs that required treatment discontinuation. Sleep disorders were the most frequent.

Development and validation of highly selective method for the determination of imatinib mesylate and dexketoprofen trometamol combination in three different media

Imatinib mesylate is a small molecule used in cancer therapy as a thyrosine kinase inhibitor. Dexketoprofen trometamol is a non-steroidal anti-inflammatory drug that has seen use in cancer therapy in combination with an anticancer drug to minimize tumor size and to reduce pain in patients. In the present study, imatinib mesylate and dexketoprofen trometamol were selected as potential model drugs to be used in combination. A new, simple and selective Ultra Performance Liquid Chromatography method was developed and validated to determine the drug substances in distilled water, in a pH 7.4 phosphate buffer and in Dulbecco's Modified Eagle Medium. The proposed method was developed using a BEH C-18 column with isocratic elution. A mixture of methanol:acetonitrile (80:20, v/v) and pH 9.5, 0.05 M ammonium acetate were (70:30, v/v) used as a mobile phase. Detection was carried out with a flow rate of 0.3 mL/min, a column temperature of 30°C and an injection volume of 20 µL. The method was validated considering linearity, accuracy, precision, specificity, robustness, detection limit and quantitation limit values, and was found to be linear in a range from 0.05 to 20.0 µg/mL for the three different media

Montelukast Induced Hypertriglyceridemia.

Montelukast a LT4 receptor antagonist is a prophylactic agent used in chronic asthma, to improve asthma control and reduce the frequency of asthma exacerbation. Advantage of Montelukast is, it is well tolerated in both adult and children upto 6 years of age. Suspected adverse effect reported to U.K, CSM follow the launch of Montelukast are anaphylaxis, angioedema, urticaria, chest pain, vertigo, athralgia, fever. Further suspected side effects are nightmare, palpitation, and sweating and Churg Strauss syndrome. Hypertriglyceridemia associated with this agent is rarely found in any published medical report or literature. This is a case of a male patient who was suffering from chronic asthma since childhood, developed allergic rhinitis since November´10. He developed hypertriglyceridemia and associated lipid profile abnormality after taking Montelukast and was also receiving salbutamol inhalation since childhood. His lipid profile before Montelukast administration was normal. Routine investigation done 4 months following drug intake shows serum triglyceride to be 732mg/dl.Montelukast was immediately withdrawn, but salbutamol was continued The triglyceride level reaches near the base line 4 months following drug withdrawal. This case highlights a rare case of Montelukast induced hypertriglyceridemia. Physician should be vigilant of the fact that Montelukast can induce hypertriglyceridemia following therapy with it.

Ultrastructural changes in the kidney cortex of rats treated with lead acetate / Cambios ultraestructurales en la corteza renal de ratas tratadas con acetato de plomo

The purpose of this study was to investigate the ultrastructural effects of lead on the kidney cortex of rats. Wistar Albino rats (180-200g body weight) were divided into a controlled and lead acetate-exposed group. Rats received lead acetate at 500 ppm in their drinking water for 60 days. Both groups were fed with the same standard food, but lead acetate was added to the drinking water. During the experimental period, blood samples were taken from the abdominal aorta of the anesthetised animals. At the end of exposure, body weight and blood lead levels were measured. The kidney tissue samples were prepared and analyzed by light and transmission electron microscopy. Cortical renal tubules show various degenerative changes with focal tubular necrosis invaded by inflammatory cells. The ultrastructural alterations found in lead acetate-treated rats were a diminution in the amount of filtration slits, increased fusion of foot processes in epithelial cells of the glomeruli, increase of lysosomal structures and pinocytic vesicles as well as large mitochondria in proximal tubule cells.

El propósito de este estudio fue investigar los efectos ultraestructurales del plomo en la corteza renal. Ratas Wistar albinas (180-200g de peso corporal) fueron divididas en grupo control y grupo experimental. Las ratas recibieron 500 ppm de acetato de plomo en el agua potable durante 60 días. Ambos grupos fueron alimentados con el mismo alimento estándar, pero acetato de plomo se le añadió al agua potable al grupo experimental. Durante el período experimental, se tomaron bajo anestesia muestras sanguíneas desde la parte abdominal de la aorta. Al final de la exposición, fueron medidos el peso corporal y los niveles de plomo en la sangre. Fueron preparadas las muestras de tejido renal y se analizaron mediante microscopía de luz y electrónica de transmisión. Los túbulos renales corticales mostraron varios cambios degenerativos con necrosis tubular focal invadida por células inflamatorias. Las alteraciones ultraestructurales encontradas en las ratas tratadas con acetato de plomo correspondieron a una disminución en la cantidad de ranuras de filtración, aumento de la fusión de los procesos podales en las células epiteliales de los glomérulos, aumento de la estructura lisosomal y las vesículas pinocíticas, así como grandes mitocondrias en las células del túbulo proximal.

[Evaluation of lead acetate side effects on rat hippocampus and the effects of vitamin C on these]

To investigate the effect of ascorbic acid against lead-induced neurotoxicity in the rat hippocampus. The heads of 40 male Sprague-Dawley rats were divided into 4 groups: normal, control, lead-treated and lead plus ascorbic acid-treated. Lead acetate [20mg/kg] was administered intraperitonealy to rats for 7days in third and fourth groups. During this period, rats in the fourth group received 500 mg ascorbic acid, in drinking water daily. At the end of the treatment, all rats were sacrified and their hippocamps were excluded. Using TEM the samples were examined in terms of natural and apoptotic cells. Histopathological evaluation showed that apoptosis was attenuated significantly in the ascorbic acid group but not in the lead group. Simultaneous administration of ascorbic acid and lead increased the level of Bcl-2 and decreased Bax protein compared with lead-treated only. It seems that ascorbic acid may reduce the lead-induced toxicity in central nervous system

Effectiveness of montelukast in the treatment of atopic dermatitis.

Leukotriene receptor antagonist ( montelukast) are recommended for the treatment of asthma, and have proved anecdotally successfully even in atopic dermatitis.In this open randomized clinical trial, the efficacy and safety of montelukast were assessed in the atopic dermatitis. Out of 31 enrolled patients all completed the study among which 16 in the montelukast group and 15 in the control group. No patient dropped from the study. Statistically significant SCORAD improvement (P = 0.003) was observed in montelukast group but in the control group SCORAD improvement was not statistically significant (P = 0.088).According to the patients impression pruritus was the most influenced SCORAD item by montelukast group immediately followed by sleep loss and inflammatory signs. On the contrary montelukast seemed to be completely devoid of activity on xerosis. No adverse effect of montelukast was observed in the present study.

New antiepileptic drugs. II. Clinical use

No abstract available.

Aspectos morfológicos da colite difusa induzida pelo ácido acético a 10 por cento via retal e tratada com enemas de ácido 5-amino-2-higroxibenzóico: estudo experimental da linhagem Sprague-Dawley / Morphological aspects of diffuse colitis induced by acethic acid at 10 per cent by rectum and treated with enemas of 5-amino-2-hydroxibenzoic acid: experimental study in Sprague-Dawley rats

O objetivo do estudo foi avaliar do ponto de vista morfológico a resposta terapêutica do enema do ácido 5-amino-2hidroxibenzóico (5-ASA) na colite difusa experimental (CDE) induzida pelo ácido acético a 10 por cento via retal. O experimento foi desenvolvido segundo um modelo randômico controlado. Foram utilizados 500 ratos machos da linhagem Sprague-Dawley com colite difusa experimental induzida pelo ácido acético a 10 por cento, divididos em cinco subgrupos: 1) subgrupo de teste-dose A; 2) subgrupos de teste-dose B; 3) subgrupo de teste-dose C; 4) subgrupo de teste-dose D e 5) subgrupo de controle da CDE. Os subgrupos de tese-dose foram tratados diariamente com enemas de 1ml de 5-ASA nas concentraçoes de 2,0; 4,0; 6,0 e 12,0g/ml, respectivamente. O subgrupo de controle da CDE recebeu enemas diários de 1ml de soluçao salina isotônica a 0,9 por cento. Foram sacrificados 10 animais de cada subgrupo mediante a inalaçao de éter nos dias 1,2,3,5,7,9,16,21,36 e 60 do experimento. Para avaliar a eficácia do enema de 5-ASA no tratamento dessa colite experimental, utilizaram-se os seguintes critérios histológicos: erosoes do epitélio de superfície, presença de pseudomembranas, ulceraçoes, produçao de muco, alteraçao na arquitetura e número de criptas, tipo de infiltrado inflamatório, epitélio glandular regenerativo, reepitelizaçao da superfície mucosa com incorporaçao de áreas hialinas e fibrose residual. Além desses critérios, houve recurso no experimento à endorcopia e ao exame coprológico (parasitológico e bacteriológico). O ácido 5-amino-2hidroxibenzóico através de enemas mostrou eficácia no tratamento da colite difusa experimental induzida pelo ácido acético a 10 por cento. A análise dos critérios modificaçao do padrao histológico, tempo para o início do reparo e tempo para retorno a padroes histológicos normais indica as dosagens de 4,0 e 6,0/ml de ácido 5-amino-2hidroxibenzóico como mais eficazes do que a de 2,0g/ml. A dosagem de 12,0g/ml de ácido 5-amino-2-hidroxibenzóico foi a que determinou resposta terapêutica mais eficaz no tratamento dessa colite experimental, porque determinou menor modificaçao do padrao histológico, menor tempo para início do repouso (3(dias) e menor tempo para retorno aos padroes histológicos normais (16(dia).