Posted by admin on Nov 30, 2018 in |
In the field of the preparation of chemotherapeutic agents with new mechanism distinct from currently approved drugs is important. However, the clinically effective approved small inhibitor molecule is still lacking. Previous reports indicated that 4-aryl-2-hydrazinothiazole derivatives provided a useful start point to develop HAT inhibitors (histone acetyltransferase). Consequently, preparation and biological evaluation of a focused library of 4-aryl-2-hydrazinothiazole based derivatives as useful as anti-cancer agents. Synthesis of 4-aryl-2-hydrazinothiazoles (1a-d), (2a-d), (3a-c), (4a-b), (5a-b), (6a-b) studied by either conventional method and free solvent microwave one-pot method, and the synthesized compounds were proved by spectroscopic methods (IR, 1HNMR, 13CNMR, GC-Ms, and elemental analysis). The activity against different cancer cell lines and the antimicrobial activities different organisms also studied, and all of the synthesized compounds were of high activity as an antibacterial for gram positive and gram negative; however, it showed also an antifungal activity were the most active compounds were 4a, 4b, 5b, 6a. It was found that all of the prepared thiazoles derivatives were active toward many cell lines (breast,...
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Posted by admin on Nov 30, 2018 in |
The elimination capacity of pristine powder activated charcoal PAC and powder activated charcoal modified with potassium permanganate MPAC to remove levocetirizine drug was investigated. The activated charcoal was impregnated with KMnO4 100 mg/L in order to improve the surface properties. The influence of concentration, time and pH on the adsorption of levocetirizine drug was conducted by means of UV-Vis spectroscopy. The experiments were carried out using two lines. Line 1; adsorption of the drug on pristine PAC and line 2; adsorption on MPAC. By batch experiments, the effect of levocetirizine concentrations of 25, 50, 75, and 100 mg/L, a reaction time of 15, 30, 45 and 60 min, and pH of 2, 4, 7 and 9 were investigated. The results showed that elimination capacity of both PAC and MPAC increased with increasing the drug concentration and time of contact and decreased with decreasing the pH. The elimination efficiency of MPAC found to be greater than that of...
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Posted by admin on Nov 30, 2018 in |
In response to several stressors such as intense light, fish elicit a generalized physiological stress response. Catla catla (61.3 ± 2.1 g) were exposed to five different light intensities of 983 ± 162 lx (L1), 1828 ± 324 lx (L2), 2676 ± 409 lx (L3), 3442 ± 648 lx (L4) and 114 ± 4 lx (Lc, control). Higher light intensities resulted in physiological stress, significantly (P<0.05) higher levels of heat shock protein-70 and heat shock protein-90 were found in both hepatopancreas and muscles of fish exposed at L4 treatment compared to the others to cope up with the stressor. A direct relationship was found between the light intensity and the serum glucose level. Significantly (P<0.05) higher glucose level was found in L4 exposed fish compared to the others. Fish at L4 had aggregated its pigments in the melanophores (punctate stage) to reflect intense light. This study could be useful in understanding the aspects of stress induced changes in fish skin melanophores. As a consequence of stress due to intense...
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Posted by admin on Nov 30, 2018 in |
Among different routes of drug delivery buccal route is an attractive alternate for drug administration which provides improved patient compliance and increase bioavailability of drugs undergoing extensive hepatic first pass metabolism. The present research work focussed on development, evaluation and characterization of buccal patches of losartan potassium using mucoadhesive hydrophilic polymers such as fenugreek seed mucilage (FSM), tamarind seed polysaccharide (TSP), sodium carboxy methyl cellulose (NaCMC) and propylene glycol as plasticizer. Losartan potassium is an angiotensin II type – 1(AT1) receptor antagonist used in treating hypertension. The plasma t1/2 of the drug is 1.5 to 2.5 h as it undergoes extensive hepatic first pass metabolism which reduces the bioavailability of the drug up to 33%. The mucoadhesive buccal patches were prepared by solvent casting technique and were evaluated for various physico mechanical parameters like weight variation, thickness, folding endurance, drug content, surface pH, moisture content, moisture absorption, % swelling and mucoadhesion studies. In-vitro drug release study was carried out using commercial semi permeable membrane. Ex-vivo drug permeation study was...
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Posted by admin on Nov 30, 2018 in |
Counterfeit and substandard pharmaceutical products circulate widely in developing countries, yet adequate techniques to monitor quality is lacking. We report herein a quick and reliable approach to predict the in-vitro bioequivalence and interchangeability of common antibiotics using nine model drugs; four brands of azithromycin and five brands of clarithromycin tablets marketed in Nigeria. Pharmacopoeia guidelines (British and United States) were used to assess tablet quality such as friability, disintegration and dissolution times. All the brands tested passed the British Pharmacopoeia standard for disintegration time and their hardness and friability values were also considered adequate. There were no significant differences in the dissolution profiles of the brands, however, the azithromycin brands released >70% of the active drug within 30 min. The calculated similarity factor values for the azithromycin and clarithromycin brands were between 61 to 100 and 46 to 100 respectively. Based on the in-vitro tests, all the brands of azithromycin were considered bioequivalent with the innovator brand. However, only one brand had a similarity factor very close to that...
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