Posted by admin on May 30, 2015 in |
Training under hypoxic conditions is known to enhance physical performance. The possible mechanism might be the stabilization of Hypoxia Inducible Factor (HIF), which otherwise is degraded under normoxia by the action of Prolyl Hydroxylase domain enzymes (PHD). Stabilization of HIF leads to upregulation of its target genes leading to improved erythropoiesis, angiogenesis and antioxidant status as an adaptation to combat training induced stress. Present study investigates efficacy of Ethyl 3, 4 Dihydroxybenzoate (EDHB) in stabilizing HIF-1α which leads to elevated levels of Vascular Endothelial Growth Factor, Erythropoetin, Hb and Hct, indicating improved angiogenesis and blood oxygen carrying capacity. In the present study we have reported 1.5 times increase in endurance performance in rats supplemented with EDHB with or without training as compared to respective controls. Significant improvement in antioxidant status as observed by increase in GSH, SOD, GST and decrease in MDA and protein oxidation, enhanced expression of anti-oxidative proteins Heme-Oxygenase, Metallothionein, Nuclear Factor Erythroid 2-Related Factor contributed in decreasing exercise training induced oxidative stress in EDHB supplemented trained...
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Posted by admin on May 30, 2015 in |
The effect of amphiphilic polyanion Poly(maleic acid-alt-octadecene)sodium salt on solubility of a zwitterionic drug (ampicillin trihydrate) in aqueous media was evaluated. This polymeric salt was obtained by an equimolar reaction of parent copolymer poly Poly(maleic acid-alt-octadecene)with an aqueous solution of NaOH. The obtained amphiphilic polyanion was purified by dialysis and lyophilization and was characterized by FTIR spectroscopy. Secondly, a method for the model drug quantification by UV spectrophotometry at 37°C was standardized. Also the grade of association drug-polymer in aqueous media using ultrafiltration methodology at three levels of temperature (20, 30 and 40°C) and two levels of pH (1.2 and 7.4) was determined. Finally, the variation of aqueous solubility of ampicillin trihydrate in ultra-pure water and two buffer media with pH of 1.2 and 7.4 with an ionic strength of 0.15 M at 37°C in presence and absence of amphiphilic polyanion was evaluated. It was found that maximum solubility is reached at a pH value of 1.2 in absence of polymeric material with a value of 36 mg/mL, which...
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Posted by admin on May 30, 2015 in |
The pharmacokinetic/pharmacodynamic indices generally predict the efficacy of antibiotics when used alone. The information related to these indices for the combination products and that too in cases of resistant bacterial infections is limited. The present study involved treatment of 12 subjects with severe complicated urinary tract infections caused by resistant extended spectrum beta lactamase bacterial strains with Elores; ceftriaxone and sulbactam combination with non-antibiotic adjuvant ethylenediamine tetracetate. In this study Elores 3g bd dose was administered and the pharmacokinetic/pharmacodynamic indices were evaluated. To see the impact of lower Elores dose on these indices, 3g od data was simulated using pharmacokinetic parameters from 3g bd dose. The pharmacokinetic/pharmacodynamic indices suggest that Elores 3g od can treat mild to moderate infection wherein minimum inhibitory concentration requirement is <16µg/mL; however for severe complicated urinary tract infections with resistant strains wherein the requirement is 16‑32µg/mL, Elores 3g bd should be the...
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Posted by admin on May 30, 2015 in |
A series of Baylis-Hillman derived N-cinnamyl substituted nitro methylene imidazole derivatives 4a-swere synthesizedfrom Baylis-Hillman acetates and nitro methylene imidazole compoundsand characterised by 1H NMR, IR, Mass and HRMS spectroscopy. Their insecticidal activities were evaluated against T. Castaneum and compared with a standard insecticide Permethrane. Preliminary biological activity tests showed that most of the compounds exhibited good insecticidal activity against T. Castaneum at 100µg/cm2 especially compounds 4b, 4g, 4i, 4l, 4n and 4r showed good insecticidal activity against T. castaneum, interestingly compound 4b with p-fluoro substitution displayed 75% activity. The structure-activity relationship showed that compounds with electron-with drawing substitutions like -F, -Br, -Cl, -NO2, -CF3 at the para position havinggood insecticidal activity and compounds with electron-with drawing groups like -F, -Br at the meta position have shown moderate activity.This work provides some hints for further structural modifications on the Baylis-Hillman derivatives and the enhancement of insecticidal...
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Posted by admin on May 30, 2015 in |
Felodipine is a member of the dihydropyridine class of calcium channel antagonists (calcium channel blockers) and is insoluble in water. To counter act above side effects, to enhance bioavailability of felodipine in blood stream and to make drug to more targeting, felodipine drug is being designed as nanosuspension formulation using hydroxyl propyl methyl cellulose and hydroxyl propyl cellulose as surfectants as well as rate controlling polymer. Drug polymers interactions were studied by FT-IR spectroscopy. Precipitation method has been used to prepare nanosuspension particles of poorly soluble drug. The prepared nanosuspensions were characterized for droplet size, pH, viscosity, polydispersity index, refractive index, surface morphology study by Scanning Electron Microscopy (SEM), drug content, percentage transmittance, zeta potential, in vitro skin permeation and drug release kinetic studies. The droplet size was in the ranges of 61.2±0.58 (F3) to 91.4±0.79 nm (F5). The polydispersity index of various felodipine nanosuspension formulations was in the ranges of 0.271±0.14 to 0.651±0.21. Most nanosuspension possesses a very low viscosity and, therefore, their application may be convenient. The...
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