Posted by admin on Sep 1, 2013 in |
A number of substituted quinazolones are well known for their pharmacological activities like anti-inflammatory, antibacterial and analgesic etc. The present work deals with synthesis of quinazolone based thiazolidinone in order to enhance the biological properties. A Series of (2-(substituted phenyl)-4-oxothiazolidin-3-yl) -4- (4-oxo-2-phenyl quinazolin-3(4H)-yl) benzamide (6a-6h) were synthesized in good yield. The structures of the compounds obtained have been established on the basis of Spectral (IR, 1H NMR, 13C NMR and Mass) data. The present study also involves in vivo anti- inflammatory activity and in vitro antibacterial activity against few strains (gram positive and gram negative) of bacteria of synthesized compounds. Derivatives 6a, 6e and 6g exhibit promising anti-inflammatory and antibacterial activity with reference to standard drug Indomethacin and Ampicillin...
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Posted by admin on Sep 1, 2013 in |
The main objective of the present study is to evaluate the effect of pH of enteric polymer [methacrylic acid ethyl acrylate copolymer dispersion (Eudragit L30 D-55)], on dissolution profile of Duloxetine HCl delayed release formulation with the Tlag of 2hrs. The said formulation was formulated using fluidized bed process in three separate layers, the drug layer, the barrier layer and the enteric layer, were coated on sugar spheres. The enteric coated pellets were top coated using a film coating material, filled in hard gelatin capsules. Eudragit L30-D55 is used as such and neutralized to different pH (pH 4.00, pH 4.25, pH 4.50, pH 4.75, pH 5.00 and pH 5.25), coated on barrier coated pellets. The formulation coated by using enteric polymer neutralized to pH 4.75 shows the maximum extent of dissolution (91.8%) in 0.1N HCl for 2 hrs followed by pH 5.5 phosphate buffer at...
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Posted by admin on Sep 1, 2013 in |
The present study was an attempt to investigate the feasibility of the matrix based sustained release unit dosage formulation of cefixime trihydrate. Matrix tablets were prepared by using xanthan gum along with the other polymer combinations (Guar gum, sodium alginate and hydroxypropylmethyl cellulose). Effect of different formulation variables like polymer concentration, ratio of polymer combination and compression force was evaluated. The Fourier transform infrared spectroscopy,differential scanning calorimeter and X ray diffraction analysis were also carried out to evaluate physico-chemical compatibility between drug and excipients. In vitro release results suggested a 24 h controlled drug release from the prepared tablet of cefixime trihydrate. Swelling and erosion studies were performed to verify the release mechanisms involved in the formulation. In vitro antimicrobial study was also performed to check the synergistic efficacy of CFT with excipients. The formulations were found to be stable up to 3 months of stability testing at 40ºC/75%...
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Posted by admin on Sep 1, 2013 in |
Oral bioavailability of Simvastatin is very low (5%) due to bad solubility and effect of first pass. The aim of this work is to enhance its solubility and reformulating it as orodispersible tablet to overcome the two problems. Simvastatin solid dispersions in β- cyclodextrin, hydroxylpropyl-β-cyclodextrin, and hydroxylbutyl-β-cyclodextrin were prepared in different drug: polymer ratios namely 1:1, 1:2, and 1:3 by kneading and solvent evaporation methods. Solid dispersion formation and mixture compatibility was investigated by DSC and FTIR. Based on the results of solubility studies; the best solid dispersion formula was selected and formulated into orodispersible tablet using Emcosoy, K-polacrillin as novel superdisintegrants and mannitol, Pullulan as water soluble diluents and evaluated. The results showed that the increase in drug solubility was dependent on polymer type, concentration and also was affected by preparation method. Simvastatin-hydroxyl-butyl-β-cyclodextrin solid dispersion mixture prepared in 1:2 drug: polymer ratio by solvent evaporation method had a higher solubility. Orodispersible tablet formula prepared by Emcosoy as superdisintegrant, Pullulan as diluent showed least wetting and disintegration times (20...
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Posted by admin on Sep 1, 2013 in |
In present work, a new vanishing cream using a natural base from palm oil and palm kernel oil and standard vanishing cream using stearic acid were prepared. The creams were o/w emulsions containing suitable combination of oil phase and aqueous phase along with preservatives. Both creams were white, non-greasy and smooth on application. They were subjected to various parameters such as; pH, viscosity, spreadability and tube extrudability. Stability studies of the prepared creams were determined at different temperatures for a period of 3 months as per ICH guidelines and the results revealed that both formulations were with good stability except the standard vanishing cream which was slightly hardened at 5oC. The pH was found to be 6.7 and 6.98, and spreadability was found to be 11.30g. cm/sec and 13.33g.cm/sec for natural base and stearic acid based creams respectively. The tube extrudability was found to be good and fair for natural base and stearic acid based cream respectively. Furthermore, the formulations were studied for primary skin irritation test on rabbits...
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