Posted by admin on Nov 30, 2017 in |
Objective: Newly designed antipsoriatic agents which are substituted series of analogues of flavonoids (kaempferol and quercetin) that belong to the subclass flavonols were subjected to (2D-QSAR) analysis using VLIFEMDS-QSARPro software with an intention to derive and understand the possible correlation of biological activity as dependent variable and other descriptors like molecular weight, XLogP values as independent variables. It can be concluded that the current study provides better insight for designing and chemical synthesis of more potent antipsoriatic agents. Methods: Several statistical regression expressions were obtained using variable selection method as simulated annealing coupled with various model building methods like partial least squares (PLS) Regression, multiple linear regression (MLR) etc. Results: For the analogues of both quercetin and kaempferol, a total of 9 QSAR models were generated, each using test set of 15 and training set of 45 similar compounds. The best QSAR model generated by PLS model building method for quercetin was model Q4 with correlation coefficient r2 of 0.9021 and significant cross validated correlation coefficient q2 of 0.5791.Similarly,...
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Posted by admin on Nov 30, 2017 in |
A simple, precise isocratic stability indicating RP‐HPLC method was developed for the determination of isopropamide and trifluoperazine in pure and its pharmaceutical formulations. In the developed method, methanol, acetonitrile and water in the ratio of 40:30:30 (v/v) as mobile phase and Waters C-18 (250mm x 4.6mm, 5μm) column as stationary phase were used. The flow rate and detection wavelength were 0.9mL/min and 240 nm respectively. The method was validated as per ICH guidelines for specificity, linearity and range, precision, accuracy, robustness, solution stability, limit of quantification and limit of detection. The stability-indicating capability was established by forced degradation experiments. The results of all the validation parameters were well within their acceptance limits and also the degradation products formed during different stress conditions in stability studies were separated from both drugs and also from individual degradation products. This validated method was applied for the simultaneous estimation of isopropamide and trifluoperazine in commercially available formulation...
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Posted by admin on Nov 30, 2017 in |
This work investigates the effects of the surfactant system used and of spray drying temperature in physicochemical properties and retention of bioactive compounds of lipid based systems loaded with bioactive compounds of Syzygium aromaticum. Seven formulations were prepared, containing Compritol 888 ato and buriti oil as lipids and maltodextrin DE10 as wall material. The surfactants Poloxamer 188, Gelucire 50/13 and Gelucire 50/2 were employed and classified by their hydrophilic-lipophilic balance (HLB). The emulsions were homogenized by means of an ultrasonic probe and spray dried. The eugenol and eugenyl acetate content of each formulation was quantified by HPLC before and after the spray drying process. Higher eugenol retention was obtained for the composition using the amphiphilic surfactant Gelucire 50/13® (HLB of 13). Retention of bioactive marker compounds was affected by spray drying temperatures. A higher spray drying temperature (140 °C) increased eugenol loss. The particle morphology was affected by the formulation composition and the drying...
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Posted by admin on Nov 30, 2017 in |
In recent years, in silico approaches have been predicting novel drug targets. The objective of this study was to analyze the inhibitory action of canthin-6-one alkaloid by computational docking studies. For this study, natural metabolite canthin-6-one isolated from Simarouba glauca was used as ligand for molecular interaction. The crystallographic structure of molecular target Epidermal Growth Factor Receptor (EGFR) tyrosine kinase was obtained from Protein Data Bank (PDB) database (PDB ID: 1M17). Gemcitabine, Cisplatin and Thiotepa were taken as the standard for comparative analysis. Computational docking analysis was performed by using online program PATCHDOCK. The canthin-6-one showed optimum binding affinity with a molecular target (EGFR – tyrosine kinase) with the binding energy of (-248.25) as compared to the standard drugs Gemcitabine (-188.48), Cisplatin (-45.26) and Thiotepa (-190.89). These results indicated that canthin-6-one could be one of the potential ligand to treat cancer. These potential drug candidates can further be validated in wet lab studies for its proper...
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Posted by admin on Nov 30, 2017 in |
Background: A cross sectional study, to determine the endemicity, by systematic investigations in institutional settings to assess the prevalence of diseases. Methods: The study was conducted by observational method over a period of seven months regarding the prevalence of particular disease and disease with co-morbidities. Among the several diseases of distinct clinical spectrum, various risk factors may presumably be contributed. This is an epidemiological study conducted prospectively at tertiary care teaching hospital which is a 350 bedded super speciality hospital. This study was conducted for a period of seven months from August 2016 – February 2017 in order to evaluate the cases for endemicity11. Patients’ demographic and diagnostic data between 20 to 80 years of age were collected from the patient’s case survey. Objectives: The main objectives of the our study was to provide awareness about diseased non communicable endemic prevalence of conditions like Diabetes, Hypertension and habitats like alcohol consumption and smoking. The intention of this manuscript would help the clinician to intervening patient’s relevant clinical and therapeutic...
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