Posted by admin on Mar 31, 2016 in |
This study was undertaken to evaluate the antioxidant, anti-inflammatory and anticoagulant activities of aqueous extract and organic fractions of Thymus zygis. Water, dichloromethane, ethyl acetate and methanol were used as extractant solvents. The fractions were analyzed by HPLC and screened for their antioxidant activity in vitro using different assay. In vivo, the fractions were evaluated by use of the oil croton-induced ear edema and carrageenan-induced paw edema model in mice and rat, respectively. Prothrombin Time and Partial Thromboplastin Time were used to determine the effect of aqueous extract, methanol, aqueous fractions and coumarone-rich extract on intrinsic, extrinsic and/or common pathway of the coagulation cascade. All fractions were found to possess considerable antioxidant activity and the rosmarinic acid is the major polyphenol compound in majority fractions. In comparison with the indometacin, the hydrophobic fractions presented stronger anti-inflammatory activity in the croton oil induced edema. Methanol and acetate ethyl fractions (50 mg/kg) significantly reduced the edema induced by carrageenan and their effect was comparable to the reference drug indometacin (10 mg/kg)....
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Posted by admin on Mar 31, 2016 in |
Increase in complexity and cost associated with pediatric safety and efficacy studies have reduced the interest of pharmaceutical companies to study bio-therapeutics in pediatric population. Dose recommendations are being made as per patient body weight or body surface area, with the assumption of linearity in body size dose adjustments. In the present study, newer approach i.e. flat fixed age-based dosing is explored. Stochastic simulations were performed on once-a-day (OD) and twice-a-day (BD) dosage regimens of a fixed dose combination (FDC) of ceftriaxone/sulbactam (2/1) to identify a promising dose range that can effectively evaluate exposure-response (E-R) relationships of the FDC against bacterial infection in pediatric population. Selected dose range of 60-120 mg/kg of FDC was evaluated against ESBL infection using in-vitro systems (dilution method and hollow fiber method). Effect of dose, dose frequency, severity of infection and age groups were analyzed in age-based subgroups i.e. neonates, infant, child and toddler. Recommended dose for infants, child and toddler were 75-120 mg/kg based on severity of infection. However, physiologically-induced reduction in drug’s...
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Posted by admin on Mar 31, 2016 in |
Plants served as potent sources of bioactive compounds since ages. The understanding of phytochemical constitution of each and every plant on earth is the preliminary and the most important step in drug discovery. As Operculina turpethum(L.) Silva Manso is traditionally used for various ailments, the understanding of phytochemical composition of the plant is very essential. The present study was an attempt to identify the phenolic compounds present in the leaf of the plant O. turpethum. Total phenol and flavonoid content was determined from the methanol extract of the leaf and the extract was subjected to HPLC analysis with seven standard compounds. A gradient mobile phase comprising acetonitrile and 0.1% phosphoric acid was used to get the phenolic profile. The quantity of each compound present in the extract was calculated from the peak area and expressed in mg/ ml of sample injected. The first mobile phase revealed the presence of compounds viz., coumarin, ferulic acid, catechin, salicylic acid, rutin, vanillin and gallic acid. Among the seven identified phenolics, coumarin was...
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Posted by admin on Mar 1, 2016 in |
In the present study, total fifteen compounds of 1,2,4,5-tetraoxane derivatives were docked. Two series of 1,2,4,5-tetraoxane derivatives were taken for molecular docking studies, one tetraoxaquines, a hybrid of two pharmacophores such as 4-aminoquinoline & 1,2,4,5-tetraoxane, and other dispirotetraoxanes. The docking studies were performed into the binding pocket of a falcipain-3 protein (pdb: 3bwk – hydrolase) by using the Ligand fit module within docking server. The results showed a better binding affinity of hybrid tetraoxaquines compared to dispirotetraoxanes at the active site of falcipain-3 because of very low binding energies for falcipain-3 protein (pdb: 3bwk – hydrolase). Therefore, hybrid tetraoxaquines are better Cysteine proteases (falcipains) inhibitors. They would be potent antimalarial agents. So the proposed inhibitors in the future could be more effective to treat...
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Posted by admin on Mar 1, 2016 in |
Organic solvents are integral part of chemical synthesis in pharmaceutical industry. These are commonly used as reaction media, in separation, purification of synthetic products and also for cleaning of equipment. Some of the solvents degrade to other solvents or unknown impurity either during synthesis or in analytical conditions. In this study, we have investigated formation of a trace level impurity, its identification and quantitation by successfully applying the concept of relative response factor (RRF) in GC-HS. The trace level impurity was identified as dimethyl ether (DME), formed due to interaction of strong acid and methanol. Unavailability of its commercial standard made the quantitation in drug substance challenging using gas chromatography. In this work, we have extended the concept of RRF for determination of DME in drug substances. The RRF of DME was established against other process solvents used in method of analysis. Application of RRF in quantitation of DME eliminates the requirement of its external standards during routine analysis at quality control...
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