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1.
Pak J Pharm Sci ; 35(5): 1473-1480, 2022 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-36451578

RESUMEN

Diabetes is getting a common disease and is spreading rapidly, affecting 6.6 percent world's population. Metformin HCl is an effective pharmacological treatment for type 2 diabetic patients because of its lowering blood glucose level ability, better weight-neutral effects and reduced risk of hypoglycemia. Nevertheless, gastrointestinal (GI) sensitivities are a concern in many patients using its immediate-release formulations. This study aimed to develop extended-release (ER) formulations to control the release into the body and minimize the dosage-related side effects of metformin and to develop an effective method of coating Sitagliptin immediate-release (IR) formulation over the core tablet. This study evaluated different formulations of Metformin HCl ER tablet using hydrophilic polymers. Different concentrations of Sitagliptin were used to develop immediate release coating. The dissolution profile of the designed formulation was compared with the reference 50/500mg tablet. In vitro dissolution of Metformin HCl (MT5), containing Methocel K4M and Methocel K100 polymer, showed 37.62% release at 1hr, 53.46% at 2hr, 84.75% at 6hr and 94.81% at 10hr. The Sitagliptin (ST8) with 10% excess released 103.64% in 30min. Similarity factor values suggested that developed Metformin ER and Sitagliptin IR formulation were like the reference product.


Asunto(s)
Diabetes Mellitus Tipo 2 , Metformina , Humanos , Fosfato de Sitagliptina/uso terapéutico , Metformina/uso terapéutico , Liberación de Fármacos , Comprimidos , Diabetes Mellitus Tipo 2/tratamiento farmacológico , Polímeros
2.
Polymers (Basel) ; 13(22)2021 Nov 15.
Artículo en Inglés | MEDLINE | ID: mdl-34833242

RESUMEN

A large amount of industrial wastewater containing pollutants including toxic dyes needs to be processed prior to its discharge into the environment. Biological materials such as sugarcane bagasse (SB) have been reported for their role as adsorbents to remove the dyes from water. In this study, the residue SB after fermentation was utilized for the dye removal. A combined pretreatment of NaOH and methyltrioctylammonium chloride was given to SB for lignin removal, and the pretreated SB was utilized for cellulase production from Bacillus aestuarii UE25. The strain produced 118 IU mL-1 of endoglucanse and 70 IU mL-1 of ß-glucosidase. Scanning electron microscopy and FTIR spectra showed lignin and cellulose removal in fermented SB. This residue was utilized for the adsorption of an azo dye, congo red (CR). The thermodynamic, isotherm and kinetics studies for the adsorption of CR revealed distinct adsorption features of SB. Untreated SB followed Langmuir isotherm, whereas pretreated SB and fermented SB obeyed the Freundlich isotherm model. The pseudo-second-order model fitted well for the studied adsorbents. The results of thermodynamic studies revealed spontaneous adsorption with negative standard free energy values. Untreated SB showed a 90.36% removal tendency at 303.15 K temperature, whereas the adsorbents comprised of pretreated and fermented SB removed about 98.35% and 97.70%, respectively. The study provided a strategy to utilize SB for cellulase production and its use as an adsorbent for toxic dyes removal.

3.
Environ Sci Pollut Res Int ; 28(2): 2355-2368, 2021 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-32880840

RESUMEN

Contamination of arsenic and fluoride in drinking water reservoirs is a serious health issue in the Sibi district, Balochistan, Pakistan. The contamination has already been affecting a large population of the district. Dental fluorosis and dermatitis are the most common reported illnesses in the area. This study focused on the evaluation of the root causes and pathway by which it reached to the body. Questioner analysis, simple examination, and pictorial representation were used to study the prevalence of diseases caused by As and F. People of the Sibi district were found to consume both surface and groundwater, which were highly contaminated with arsenic and fluoride. The saturation index, ranging from 1 to 7, showed high enrichment of contaminants in both types of water. Geochemical calculations and the sodium absorption ratio were evaluated. High values of the saturation index of different salts showed high saturation of salts in water. The principal component analysis grouped the data into three clusters, showing that the surface water has no resemblance with the control water. High degree of contamination was observed for most of the samples, whereas, some samples of ground water were closed to the control group; a group of samples within WHO limits. The correlation studies and other calculations also revealed that the F and As reached lethal limits in the drinking water and thus caused severe health damage to the local area population. The diseases found in the area are fluorosis, keratosis, dermatitis, and melanosis.


Asunto(s)
Arsénico , Agua Potable , Fluorosis Dental , Agua Subterránea , Contaminantes Químicos del Agua , Arsénico/análisis , Agua Potable/análisis , Monitoreo del Ambiente , Fluoruros/análisis , Fluorosis Dental/epidemiología , Fluorosis Dental/etiología , Humanos , Pakistán , Contaminantes Químicos del Agua/análisis
4.
Pak J Pharm Sci ; 32(3 Special): 1285-1291, 2019 May.
Artículo en Inglés | MEDLINE | ID: mdl-31551205

RESUMEN

Synthesis of new antioxidants and enzyme inhibitors is an active area of research in pharmaceutical sciences. This can be used for development of new active product ingredients which can prevent body from different diseases. This study comprises of preparation of transition metal complexes using 4-(4-bromophenyl)-2,2'-bipyridine (BPBP) and their screening for antioxidant and lipoxygenase inhibition properties. 4-(4-bromophenyl)-[2,2'-bipyridine]-6-carboxylic acid was used as starting material and its decarboxylation resulted in BPBP. Decarboxylation by conventional heating method was compared with microwave decarboxylation method. Selected metal complexes of the ligand were synthesized with Ruthenium (II), Iron (II) and Cobalt (II) ions. The complexes were characterized using UV, IR, 1H-NMR, ESI-MS and CHNS techniques. It was observed that BPBP acted as a bidentate ligand. The metal to ligand stoichiometry was 1:3 for all the synthesized complexes. The complexes had octahedral structure with C3 symmetry. The antioxidant activity was evaluated using free radical scavenging assay. BPBP showed insignificant antioxidant and lipoxygenase activities while its transition metal complexes showed promising activities. Antioxidant activity of Fe and Co-complexes was found significantly higher than the reference drug used in this study.


Asunto(s)
Antioxidantes/química , Antioxidantes/farmacología , Complejos de Coordinación/química , Inhibidores de la Lipooxigenasa/química , Inhibidores de la Lipooxigenasa/farmacología , 2,2'-Dipiridil/química , Antioxidantes/síntesis química , Cobalto/química , Complejos de Coordinación/síntesis química , Complejos de Coordinación/farmacología , Evaluación Preclínica de Medicamentos , Hierro/química , Ligandos , Inhibidores de la Lipooxigenasa/síntesis química , Espectroscopía de Resonancia Magnética , Microondas , Estructura Molecular , Rutenio/química
5.
Pak J Pharm Sci ; 32(3 (Supplementary)): 1253-1259, 2019 May.
Artículo en Inglés | MEDLINE | ID: mdl-31303598

RESUMEN

In this study, a range of oxamide ligands were synthesized by the reaction of amines with oxalyl chloride in basic medium. Spectroscopic and analytical techniques such as IR, 1H-NMR and ESI-MS techniques were used for characterization of the synthesized oxamides. The synthesized oxamides were screened for Lipoxygenase inhibition. Biological screening revealed that the oxamides possessed good lipoxygenase inhibition activities, whereas, the unsubstituted oxamide did not show any distinct lipoxygenase inhibition activity. Molecular docking studies of the oxamides were also carried out for lipoxygenase inhibition. The results obtained from molecular docking were well correlated with the empirical data.


Asunto(s)
Araquidonato 5-Lipooxigenasa/química , Inhibidores de la Lipooxigenasa/síntesis química , Inhibidores de la Lipooxigenasa/farmacología , Ácido Oxámico/análogos & derivados , Aminas/química , Araquidonato 5-Lipooxigenasa/metabolismo , Cloruros/química , Evaluación Preclínica de Medicamentos , Espectroscopía de Resonancia Magnética , Simulación del Acoplamiento Molecular , Oxalatos/química , Ácido Oxámico/química , Conformación Proteica , Espectrometría de Masa por Ionización de Electrospray , Relación Estructura-Actividad
6.
Water Sci Technol ; 75(5-6): 1158-1168, 2017 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-28272044

RESUMEN

Activated carbons produced from a variety of raw materials are normally selective towards a narrow range of pollutants present in wastewater. This study focuses on shifting the selectivity of activated carbon from inorganic to organic pollutants using activation temperature as a variable. The material produced from carbonization of pine shells substrate was activated at 250°C and 850°C. Both adsorbents were compared with commercial activated carbon for the sorption of lead, cadmium, methylene blue, methyl blue, xylenol orange, and crystal violet. It was observed that carbon activated at 250°C was selective for lead and cadmium whereas the one activated at 850°C was selective for the organic dyes. The Fourier transform infrared spectroscopy study revealed that AC850 had less surface functional groups as compared to AC250. Point of zero charge and point of zero salt effect showed that AC250 had acidic groups at its surface. Scanning electron microscopy depicted that increase in activation temperature resulted in an increase in pore size of activated carbon. Both AC250 and AC850 followed pseudo-second-order kinetics. Temkin isotherm model was a best fit for empirical data obtained at equilibrium. The model also showed that sorption process for both AC250 and AC850 was physisorption.


Asunto(s)
Carbón Orgánico/química , Fenómenos Químicos , Pinus/química , Temperatura , Adsorción , Cadmio/aislamiento & purificación , Colorantes/aislamiento & purificación , Difusión , Violeta de Genciana/química , Violeta de Genciana/aislamiento & purificación , Concentración de Iones de Hidrógeno , Cinética , Plomo/aislamiento & purificación , Azul de Metileno/química , Azul de Metileno/aislamiento & purificación , Microscopía Electrónica de Rastreo , Compuestos Orgánicos/aislamiento & purificación , Fenoles/química , Fenoles/aislamiento & purificación , Sales (Química)/química , Semillas/química , Espectroscopía Infrarroja por Transformada de Fourier , Sulfóxidos/química , Sulfóxidos/aislamiento & purificación
7.
Environ Monit Assess ; 182(1-4): 587-95, 2011 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-21336485

RESUMEN

The assessment of the toxicants in roadside soil on regular basis has become extremely essential with the increase in awareness for the metal toxicity in the environment. The present study investigates the presence of toxic metals along National Highway (N-5), Pakistan. Averages of about 1.3 million per month of automobile vehicles ply on this route. Lead (Pb), zinc (Zn), copper (Cu), nickel (Ni), cadmium (Cd), cobalt (Co), manganese (Mn), mercury (Hg), and iron (Fe) were analyzed by atomic absorption spectrophotometry in roadside soil at the nine selected locations along the highway. Strong Pearson correlations (α = 0.05) were found between Pb and Zn (r(2) = 0.887), Fe and Mn (r(2) = 0.880), Hg and Cd (0.864), Cu and Zn (0.838), and Cu and Pb (0.814). The correlation between the elemental compositions of the main automobile components revealed vehicular traffic as the main non-point source of roadside soil pollution. Extremely high level of mercury, 144.05 mg kg(-1), was found at S5. It was revealed that the unregulated incineration and dumping sites of hazardous waste material along N-5 were also responsible for these contaminations. Multivariate analysis on the obtained data also disclosed the same interpretation. Cluster analysis of the data grouped Pb, Zn, and Cu at 85.23% similarity, whereas, Cd, Hg, and Ni were grouped at 78.75% similarity basis. The findings need swift action against the root cause of soil pollution.


Asunto(s)
Monitoreo del Ambiente , Metales Pesados/análisis , Contaminantes del Suelo/análisis , Automóviles/estadística & datos numéricos , Análisis por Conglomerados , Contaminación Ambiental/estadística & datos numéricos , Metales Pesados/toxicidad , Pakistán , Contaminantes del Suelo/toxicidad , Emisiones de Vehículos/análisis , Emisiones de Vehículos/toxicidad
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