Posted by admin on Dec 31, 2017 in |
Background and aim: Spiroazetidin-2-ones and furans are commonly used as anti-bacterial, anti-fungal, anti-inflammatory, cardiovascular activities, anticancer, antiparkinson agents etc. The purpose of this study was to perform virtual toxicity studies of the synthesized compounds 1-(substitutedphenyl)-3-chloro-5,9-bis(furan-2-ylmethylidene)-1-azaspiro[3.5]nonan-2-ones (3a-3h). Materials and methods: Computational toxicology and mutagenicity profiles of these compounds were generated by using TOPKAT 6.1 (Toxicity Prediction Komputer Assisted Technology version 6.1). The molecular structure of the query compound was given as a SMILES string and a desired TOPKAT predictor was selected, then TOPKAT automatically conducts analysis of the query compound. Results: According to TOPKAT 6.1 model the compounds 3a – 3h are non-mutagenic and devoid of aerobic biodegradability. The computed Rat oral LD50 values for the compounds 3a – 3h ranged from 1.1g/kg to 115.0mg/kg. These high LD50 values suggest higher safety of these compounds. The computed probability of skin irritation for all compounds was found to be 1.000 and the probability for the carcinogenicity was found to be 0.950-1.000. Conclusion: By using computerized statistical methodology, more promising molecules can...
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Posted by admin on Dec 31, 2017 in |
This study was aimed to investigate the biochemical influence of aqueous extracts of roots, stem and leaves of Zizyphus mauritiana (ZM) on silica induced toxicity in rats, with changes in inflammatory markers in liver and kidney. To test the preventive effect of extracts of Zizyphus mauritiana on development of silica induced toxicity in wistar albino rats, animals were treated simultaneously with intraperitoneal administration of silica and oral feeding of extracts, for 21 days. At the end of the experiment, blood samples were withdrawn for biochemical analysis. The results revealed that animals administered with silica and simultaneous feeding of extracts of root, stem and leaves of Zizyphus mauritiana had a significant effect and decreased serum levels of ALT, AST, ALP, urea, uric acid, creatinine and LDH, as well as pro-inflammatory cytokines TNF-α and IL-6 as compared with normal control group. Zizyphus mauritiana extracts treated groups had shown recoupment in the body weight which was found decreased in only silica treated animals. In conclusion, this study indicated that extracts of bark...
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Posted by admin on Dec 31, 2017 in |
The purpose of the study is to evaluate the effect of the granulation properties of Lactose depending upon the use of its crystalline forms and the impact of active (Acetaminophen) concentration using rheological and thermal tools. Lactose was chosen as an excipient available in different hydrate forms (anhydrous and monohydrate) and Acetaminophen (APAP) was selected as a model drug for the subject research. Preliminary research was performed to determine wet-granulation end-point utilizing a real time off-line PAT tool, thermal effusivity. Further research was continued for low-shear wet granulation for the powder blends of drug and excipients. The properties of wet and dried granulation were determined using Powder Rheometer, Thermal effusivity and DSC. The dried granules crushing strength were evaluated using Texture Analyzer. Acetaminophen is a strong cohesive active, which upon wet granulation was found to bind strongly with Lactose particles to form more flowable and compressible granular mass. The granulation prepared using anhydrous form of Lactose with APAP showed higher bulk density and permeability as compared to hydrate form...
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Posted by admin on Dec 31, 2017 in |
Cefixime trihydrate belongs to third generation cephalosporin having poor water solubility. In the present study, nanocrystal suspensions of cefixime trihydrate were prepared with the objective of providing enhanced solubility and stability with reduced particle size and thus improving the bioavailability potential. Nanocrystal suspensions were prepared by high pressure homogenization technique and evaluated for particle size, polydispersity index, zeta potential, and drug release. 23 factorial design was used for the formulation designing purpose. Particles of average size 143.5nm having PDI of 0.269 were produced. Zeta potential was found to be -36.6mV and the formulation was found stable on the basis of results obtained from differential scanning calorimetry and scanning electron microscopy studies. The drug release and ex-vivo permeation studies revealed enhanced permeation of drug, as desired, indicating its potential for an attempt towards successful nanocrystal...
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Posted by admin on Dec 31, 2017 in |
The medicinal plants are the key source in the life of human beings. The present study was aimed to evaluate the preliminary phytochemistry, pharmacognostical and antimicrobial activity of Canthium coromandelicum fruit. The fruit showed the presence of secondary metabolites like flavonoids, steroids, tannins, phenol, sterols, cardiac glycoside and saponin glycoside in various extracts. The pharmacognostical analysis of C. coromandelicum was useful in the identification of authentic samples and recognizing adulterants. The various extracts of C. coromandelicum fruit has shown antimicrobial activity against eight bacterial strains including Gram negative, Gram-positive bacteria, and three fungal strains using agar well diffusion method. The methanolic extract showed the broad spectrum antimicrobial activity compared to petroleum ether and chloroform extracts. Chloroform extract showed high cytotoxicity value with low IC50 values. The antimicrobial studies proved that Canthium coromandelicum fruit has antimicrobial activity against the selected pathogens. The Brine Shrimp Lethality Assay is an excellent predictive tool for the toxic potential of plant extracts in...
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