Posted by admin on Nov 1, 2014 in |
Etodolac is an anti-inflammatory drug that is poorly soluble in water. This paper describes an approach to improve the dissolution rate of Etodolac by using solid dispersions (SDs) in hydrophilic polymers. The solid dispersions prepared with a Co-evaporation, kneaded method & Physical Mixture method using different concentrations of α-cyclodextrin (α-CD). The release of Etodolac from various solid dispersions was determined from dissolution studies by use of USP dissolution apparatus. The dissolution study results revealed that there was a considerable increase in solubility of all solid dispersions as compared to pure drug. Prepared solid dispersions were characterized by DSC, PXRD, IR and SEM images were evaluated for drug content, saturation solubility. Physicochemical characterization of solid dispersions suggests a reduction in drug crystallinity following dissolution enhancement. Results indicate that present % DE 30 of drug was improved from 36.01 to 58.57 by the use of Etodolac α-CD-HPMC (1:2:0.3) Kneaded...
Read More
Posted by admin on Nov 1, 2014 in |
The aim of the present study was to design the suitable culture medium and also optimize the culture conditions for enhanced production of antimicrobial metabolites by Streptomyces violaceoruber VLK-4 which exhibited a broad spectrum of activity against bacteria and fungi. Production of bioactive metabolites by the strain was high in modified yeast extract-malt extract dextrose (ISP-2) broth as compared to other media tested. Mannitol (0.4%) and asparagine (1%) were found to be the most suitable carbon and nitrogen sources for the optimum production of bioactive metabolites as well as growth. Maximum production of bioactive metabolites was found in the culture medium with an initial pH 7.0 incubated for five days at 30 ºC under shaking conditions. This is the first report on the optimization of bioactive metabolites by Streptomyces violaceoruber...
Read More
Posted by admin on Nov 1, 2014 in |
The plant selected for the activity is obtained from the ninth day young leaves of Triticum aestivum Linn. belonging to the family Poaceae. The plant is commonly known as Wheatgrass which is used for various medicinal and health benefits for many years. It is considered as a cleansing and purifying agent from ancient times and yet can be used for its healing properties because of its nutritional values. The leaves contain many chemical compositions such as proteins, flavonoids, alkaloids, glycosides, terpenoids, saponins, fibers, tannins, and phenolic compounds. Wheatgrass is also rich in chlorophyll which consists of Chlorophyllin (derivatives of chlorophyll) and posses bacteriostatic and antioxidant properties. The concentrated methanolic extract showed significant hepatoprotective effect at 500 mg/kg dose in carbon tetrachloride (CCl4) treated rats. The blood samples were collected, and the serum was estimated for biochemical parameters SGOT, SGPT, alkaline phosphatase, total and direct bilirubin content. The studies indicated that the recovery of liver from CCl4 damage after the treatment was...
Read More
Posted by admin on Nov 1, 2014 in |
Pesticide uses pose a serious threat to environment and public health owing to their persistence and tendency to accumulate in animal and plant tissues. The present investigation was conducted to analyze pesticide residues mainly HCH and DDT in field, and biological samples from the plantation areas of Northern Kerala, India and the extent of DNA damage in cattle was measured. Environmental samples mainly water and fodder and biological samples milk and blood were collected from study area. All samples were analyzed using Gas Chromatography with Electron Capture Detector and confirmed by Gas Chromatography with Mass Spectrometry (GC-MS). The extent of DNA damage was analyzed using COMET assay. Among samples analyzed, water samples revealed detectable pesticide residues. One water sample was detected with all HCH isomers, and two samples were detected with p,p’-DDD. Mean concentration (ppm) of total HCH and DDT were 8.073 × 10-4 and 3.51 × 10-5 respectively. Pesticide residues in fodder and biological samples were with below detectable level. Comet assay revealed significantly higher (p<0.05) percent DNA...
Read More
Posted by admin on Nov 1, 2014 in |
Different prokineticin receptor antagonists, based on the triazinedione scaffold, were synthesized by a new efficient method. Here we demonstrated that 5-benzyl triazinediones substituted in position para of the benzyl group with halogens provide compounds endowed with interesting selectivity for the Prokineticin receptor 1 (PKR1). BRET technology indicates that such substitution results in increased affinity for the PKR1.The affinity for PKR2, always in mM range, was never significantly affected by the para-halogen-benzyl pharmacophores. The analog bearing a para-bromobenzyl pharmacophore (PC-25) displayed the highest affinity for PKR1 (~18 times higher than the reference PC-1 that bears a para-ethyl benzyl group) and the highest selectivity (~300 times). The other halogen substituted analogs (PC-7, PC-18 and PC-35), showed selectivity for PKR1 more than 100 times higher than for PKR2. Using transgenic mice lacking one of the two PKRs we demonstrated that all these compounds were able to abolish the Bv8-induced hyperalgesia in mice still expressing the PKR1 at doses lower than those necessary to abolish hyperalgesia in mice expressing only the PKR2. The...
Read More
