Posted by admin on Sep 1, 2014 in |
Mycobacterium leprae, the causative agent of the disease, leprosy develops resistance against most of the drugs, so novel drug targets are required to design new drugs. Present work is aimed at understanding the inhibition of enoyl-acyl carrier protein reductase (Enoyl-ACP reductase), which is one of the receptor proteins used in drug discovery for screening anti-leprosy agents by virtually designed sulfone class of compounds. The crystal structure of the inhibited M. leprae InhA complex (2NTV) provides the details of protein-ligand interactions. The virtually designed series of compounds having sulfone moiety have docked well in the active site region of the protein. The prediction of ADME properties was also performed by Qikprop software. Mycobacterium leprae, the causative agent of the disease, leprosy develops resistance against most of the drugs, so novel drug targets are required to design new drugs. Present work is aimed at understanding the inhibition of enoyl-acyl carrier protein reductase (Enoyl-ACP reductase), which is one of the receptor proteins used in drug discovery for screening anti-leprosy agents by virtually...
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Posted by admin on Sep 1, 2014 in |
Kaempferia galanga (Family: Zingiberaceae) has immense importance in the traditional health care system as a carminative, cholera, anti-inflammatory, abdominal pain, dyspepsia, and stomachic as well as in the diseases of coughs, pectoral affections, and stoppage of the nasal blocks. Grewia paniculata (Family: Malvaceae) has been used in traditional medicine for the treatment of indigestion, eczema, itch, small-pox, typhoid fever, dysentery and syphilitic ulceration of the mouth. Leaves of this plant used along with turmeric and shell of snail for the treatment of jaundice. This study was aimed to investigate the antidiarrhoeal activity of the acetonic extract of Kaempferia galanga and ethanolic extract of Grewia paniculata. The acetone extract of rhizome (ACR), as well acetone extract of the leaf (ACL), ethanol extract of bark (EEB) and ethanol extract of the leaf (EEL) were subjected to antidiarrhoeal activity test. The antidiarrhoeal activity was performed by castor oil-induced diarrhea in mice. In this study, both plant extracts exhibited significant inhibition (p < 0.05-0.001) and a dose-dependent decrease in the total number of...
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Posted by admin on Sep 1, 2014 in |
The present investigation aimed to design and evaluate solid dispersions of Atorvastatin and Fenofibrate combination, to enhance the solubility and bioavailability. When used in combination, these drugs show additive beneficial effect and comparatively fewer side effects, in the treatment of Hyperlipidemia. Being members of BCS Class-II, these drugs exhibit low aqueous solubility and high permeability. The solubility of the above drug combination is increased using solid dispersions with PEG 4000 and PEG 6000 in different concentrations, using the solvent evaporation method. The in-vitro release profiles of prepared solid dispersions were found to exhibit better dissolution characteristics compared to that of a branded market formulation, Atocor-F. The prepared solid dispersions were evaluated concerning, percent practical yield, drug content, and characterized using Fourier Transform Infra-red (FTIR) spectroscopy, X-Ray Diffraction (XRD) and Scanning Electron Microscopy (SEM). FT-IR spectra data showed the absence of drug-polymer incompatibility. Drug-polymer interaction was investigated using X-Ray diffraction (XRD) and Scanning Electron Microscopy (SEM). The formulation F4, containing Atorvastatin: Fenofibrate: PEG 4000: PEG 6000: 1:1:2:4 was found to...
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Posted by admin on Sep 1, 2014 in |
Objective: This study aims to develop an enteric coated (coated with Eudragit S-100) matrix tablet of Mesalamine to improve the bioavailability by targeting the drug to the colon for the treatment of ulcerative colitis. Materials and Methods: Matrix tablets were prepared by wet granulation technique by applying 32 full factorial designs for optimization. The independent variables used were the amount of guar gum, and amount of starch paste, each at three different levels and dependent variables was hardness, percent cumulative drug release (% CDR) study at 5th hr. and time required for 90% of drug release (t90%). The prepared matrix tablets were coated with Eudragit S-100. Result and Discussion: The prepared tablets were characterized for physical parameters, in-vitro drug release (with and without 2% rat ceacal contents) and stability on storage. The optimized formulation was subjected to in-vivo roentgen graphic studies to analyze the in-vivo behavior of the prepared tablet. The optimized formulation consisting of guar gum (20% w/w) and starch paste (15% w/w) released a negligible amount of...
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Posted by admin on Sep 1, 2014 in |
The present work was undertaken to develop and validate a rapid and consistent UPLC method in which the peaks will appear in a short period as per ICH Guidelines. The UPLC separation was achieved on a Symmetry C18 (2.1 × 100mm, 1.7mm, Make: BEH) or equivalent in an Isocratic Mode. The mobile phase was composed of Phosphate Buffer (60%) [pH 3.0] & Methanol (40%) [UPLC Grade] The flow rate was monitored at 0.25 ml per min. The wavelength was selected for the detection was 280 nm. The run time was 3 min. The retention time found for the drugs Lamivudine, Abacavir, and Zidovudine was 1.019 min, 1.271 min & 1.617 min respectively. The % recovery was found to be 98.0%- 99.0% for the drug Abacavir. The % recovery was found to be 98.0% – 99.6% for the drug Lamivudine. The % recovery was found to be 98.2% – 98.6% for the drug Zidovudine. The linearity was established in the range of 20 to 60 ppm for the drug Abacavir...
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