Posted by admin on Jan 1, 2016 in |
The objective of the present study was to prepare gum Cordia myxa-g-polyacrylonitrile using microwave irradiation and to evaluate its mucoadhesive applications. The graft co-polymerization of poly(acrylonitrile) on gum Cordia myxa was carried out employing 3- level 4-factor central composite experimental design. It was observed that the concentrations of ammonium persulphate and concentrations of acrylonitrile exerted a significant synergistic and antagonistic influence on grafting efficiency and percent swelling respectively. Graft co-polymer was characterized by fourier transform infrared spectroscopy, X-ray diffraction and differential scanning calorimeter. Mucoadhesive properties of the graft-copolymer were evaluated by formulating tablets employing captopril as the model drug. On comparative evaluation the gastroretentive tablets of captopril formulated using graft co-polymer (20%) showed ex vivo mucoadhesive time of 12 h whereas the tablets formulated using native Cordia myxa gum and carbopol 934 showed ex vivo mucoadhesive time of 6 h and 8 h respectively. According to the results obtained it was concluded that grafting of poly(acrylonitrile) on gum Cordia myxa enhances its mucoadhesion and thus, the grafted Cordia myxa...
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Posted by admin on Jan 1, 2016 in |
There are more than 40% of drugs which are poorly soluble and 90% of the drugs from the pipeline are from BCS class II and IV. Application of techniques like computers, robotics, high-throughput screening, combinatorial chemistry have resulted in database of huge drug-like molecules which are generally derived solely based on the affinity of the molecule with the target physiological bodies viz. enzymes, receptors etc. These new chemical entities or drug-like substances having poor biopharmaceutical properties exhibiting poor pharmacological properties. Poor biopharmaceutical properties like poor solubility poses many difficulties and delay in drug development process as the these molecules show satisfactory performance in-vitro or in-silico but in-vivo they fail to exhibit pharmacological response thereby have low bioavailability. Drug dissolution is rate limiting step in majority of the cases hence increasing solubility leads to increased dissolution rate and thereby likely to increase the bioavailability. By doing so the drug is available in a solubilized form at site of action and is efficacious at lower doses. In the present work dissolution...
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Posted by admin on Jan 1, 2016 in |
The use of herbal medicines for the betterment of mankind is well practiced from centuries. Triphala is a well known Rasayana drug used in Indian systems of medicine. Due to its wide spread usage in herbal medicine it drives the attention of regulatory bodies for its safety and efficacy and hence quality become major concern. In the present study we have standardized herbs by Pharmacognostical evaluation and selected chemical markers as part of quality control tool. Gallic acid and total tannins are selected as stability indicating assay for triphala caplet. The drug was subjected to short time accelerated stability study (400C/75%RH) as per ICH guidelines. Presence of stone cells, starch grains and calcium oxalate crystals are noted for differentiate along with the xylem elements (fibers and vessels) based on their structure. The content of these active constituents were monitored throughout the study and were found to be stable (Gallic acid: 3.72 to 5.24 %w/w, Total tannins: (17.16%w/w to 23.49%w/w). The HPTLC chromatographic fingerprint was also found to be complying...
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Posted by admin on Jan 1, 2016 in |
New tetradentate Schiff base and its Co(II), Ni(II), Cu(II), Zn(II), Cd(II) and Hg(II) complexes formed by the condensation of 5-fluoro-3-hydrazonoindolin-2-one with isophthalaldehyde. The coloured complexes were prepared of [MLX2], Where L = Schiff base hydrazone, M = Co(II), Ni(II), Cu(II), Zn(II), Cd(II) and Hg(II), X = Cl-. Physico-chemical characterization has been carried out to determine the structure of the complexes. All the synthesized compounds, were studied for their in vitro antibacterial, and antifungal activities, against two Gram-negative (Shigella flexneri and Enterococcus aerogens) and one Gram-positive (Micrococcus luteus,) bacterial strains and against three fungal strains (Candida krusiae Candida parasilopsis and Malassesia pachydermatis) by using cup-plate method. The DNA cleavage capacity of all the complexes was analysed by agarose gel electrophoresis...
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Posted by admin on Dec 31, 2015 in |
Docking is a method which predicts the preferred orientation of one molecule to a second when bound to each other to form a stable complex and is frequently used to predict the binding orientation of small molecule drug candidates to their protein targets and plays an important role in the rational design of drugs. The present study has been focused on the Docking studies of 1,3-disubstituted ureas derivatives as anti-tubercular agents that can explore the binding affinity of ligands to that of the epoxide hydrolase with the help of Schrodinger molecular modelling software. The G-score of the ligand 6s was found to be -8.03 as comparable with the G-score of co-crystallized ligand i.e. -3.77. The carbonyl oxygen of urea moeity of the ligand 6s showed a H-bond interaction with the phenolic oxygen of TYR381 and TYR465 amino acid of the protein residue with distances 2.24Å and 1.67Å respectively and the carbonyl oxygen of urea moeity of the co-crystallized ligand also showed a H-bond interaction with the phenolic oxygen of...
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