Posted by admin on Feb 28, 2017 in |
The objective of the present study is optimization of telmisartan tablet formulation employing βCD, Primojel, and Tween 80 by 23 factorial design to achieve NLT 85% dissolution in 10 min. Eight telmisartan tablet formulations were prepared using selected combinations of the three factors as per 23 factorial design. Telmisartan tablets were prepared by direct compression method and were evaluated. Telmisartan tablet formulations Fb and Fbc disintegrated rapidly in 20 and 40 seconds and gave very rapid dissolution of telmisartan, 96.1% and 95.8% in 10 min respectively. The increasing order of dissolution rate (K1) observed with various formulations was Fc< F1< Fac< Fa< Fabc< Fab< Fbc< Fb. The polynomial equation describing the relationship between the response, percent drug dissolved in 10min (Y) and the levels of βCD (X1) , Primojel (X2) and Tween 80 (X3) based on the observed results is Y = 55.327 + 3.613(X1) + 35.072(X2) – 9.182(X1 X2) – 3.757(X3) – 3.317(X1 X3) + 2.06(X2 X3) + 1.765(X1 X2 X3). Based on the above equation, the formulation...
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Posted by admin on Feb 28, 2017 in |
Despite significant progress made in the treatment of infectious diseases, caused by bacteria and fungi, it remains a major worldwide health problem due to rapid development of resistance against the existing antimicrobial drugs. In the present investigation, a novel series of chalcones 2a–2h were synthesized by the clasein-schmidt condensation of various aldehydes with methyl ketone in the presence of KOH in ethanol which lead to the formation of new chalcones. The structures of these compounds were elucidated by, IR, 1H-NMR spectral data. The in vitro antibacterial activity of these compounds was evaluated against two Gram positive and two Gram-negative bacteria Staphylococcus aureus, Streptococcus pyogenes, Escherichia coli and Pseudomonas aeruginosa by microdilution method and then the minimum inhibitory concentration (MIC) of these compounds was determined. The results showed that compounds 2d, 2e and 2h showed most promising antibacterial activity as compared to the antibiotics ciprofloxacin in (Tables 1). Compound 2e which carries the nitro substituent appears to exhibit the highest antibacterial activity against all gram positive and gram negative...
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Posted by admin on Feb 28, 2017 in |
Understanding the mode of inhibition through the crystal structures of EGFR kinase domain complex with small molecule inhibitors provides us to search for potential ligands of EGFR. The binding mode analysis of pyridopyrimidine analog reveals that the presence of hydrogen bonds between the target protein amino acid Met 793 (i.e. the hinge region which is responsible for catalytic activity of the domain) and the ring nitrogen of the small molecule inhibitor. In addition, amino acid Asp 855 and Lys 745 were also involved in the interaction. The present work focuses on the identification of novel ligands through computational approach. By screening of pubchem database compounds, based on the bioactive and structural similarity of a pyridopyrimidine derivative (highly potent inhibitor of EGFR), 117 compounds were identified and all are having kinase inhibition activity but were not analyzed in EGFR. Using GLIDE software, the docking was done and complete analysis of the binding mode results in eleven compounds having same pattern of interactions and these compounds may be further analyzed by...
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Posted by admin on Feb 28, 2017 in |
Aegle marmelos(L.), family rutaceae is highly reputed medicinal tree commonly known as the bael. All parts of the plant have medicinal properties and extensively used by the traditional medicine practitioners of Bangladesh in different health ailments like Diabetes, Diarrhea, Jaundice, typhoid. The present study was dedicated to investigate phytochemical and pharmacological properties of ripe fruit, half-ripe fruit, leaf and seed of the plant extracted with methanol solvent. Initial phytochemical screening confirmed the presence of different phytoconstituents including alkaloid, flavonoids, carbohydrate, glycoside, saponin, tannin, glucoside and steroids in different extracts. Antioxidant potential was evaluated using total phenol and total flavonoid contents determination assays, total antioxidant capacity, DPPH (1,1-diphenyl-2-picrylhydrazyl) radical scavenging assay, NO radical scavenging assay, reducing power assessment, CUPRAC (Cupric Reducing Antioxidant Capacity), total alkaloid determination assay. All the plant parts were found to possess moderate amounts of phenolics and flavonoids, expressed as galic acid equivalent (GAE) and quercetin equivalent (QE) respectively. The methanolic extract of half-ripe fruit demonstrated highest phenolic content (6.05 mg/gm GAE) while methanol extract of seed...
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Posted by admin on Feb 28, 2017 in |
The hemoglobin uptake and transport by the malaria parasite, Plasmodium falciparum are preferable targets for antimalarial drug development. There is a need for alternative approaches to investigate the endocytic process of live and intact cells under non-disruptive conditions as previous findings were mostly based on morphological analysis of thin-section electron micrographs. In the present study, resealed erythrocytes containing TMR-dextran, the host cell cytoplasm marker, were prepared and characterized. Fresh erythrocytes were collected in EDTA anticoagulant vacutainer tubes, which proved to maintain a normal biconcave disk shape of the cells. Using a modified hypotonic dilution method, washed erythrocytes were lysed in 3 volumes of hemolysis buffer, which permitted the retention of 33.56 ± 7.84% of the original hemoglobin content of the cells. Resealed erythrocytes containing TMR-dextran were invaded by the parasites with similar efficiency to unlabeled cells, and able to support the parasite growth and development. Live cell fluorescence imaging of the endocytic process revealed the appearance of TMR-dextran-containing small endocytic vesicles with intense signals at early ring stage. These...
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