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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Posted by admin on Mar 1, 2016 in |
The package inserts (PI) are a valuable source of information on drugs for physicians and patients. However, the degree of awareness of PI & their perceptions at both physician and patient front has not been studied in India in current times. The study was undertaken to assess the degree of awareness regarding information in drug package inserts at a tertiary care centre in western India. A questionnaire based survey was conducted among 100 physicians and 100 patients. The questionnaire mainly focused on the level of awareness, understanding and utility of information given in PI. The responses were collated and analyzed. The results showed that 20% of the physicians admitted that they rarely or never referred to PI. 30% did not consider the PI to be important in their clinical practice & 18% did not feel the need for PI to be always available. 64% opined that the language was too technical for comprehension by lay persons. Only 10% said that they always asked their patients to read the PI....
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Posted by admin on Mar 1, 2016 in |
Terminalia paniculata Roth. (TP) is a tropical tree. Traditionally, flower juice and bark of Terminalia paniculata have been used as a remedy for cholera, for the treatment of diabetes, inflamed parotid glands and in menstrual disorders. The objective of the present study is to evaluate the antidiabetic potential of Terminalia paniculata bark extract in various in-vitro models and its safety evaluation using Wistar albino rats. The in-vitro antidiabetic activity was studied using Alpha amylase, Alpha glucosidase inhibition and Glucose diffusion assay. The nitric oxide radicals scavenging activity was determined using antioxidant assay. Acute and sub acute toxicity studies were designed as per the OECD guidelines- 423. TP extract shows maximum inhibition of 94.5 % on α-Amylase at 700 µg/ml and 94 % on α-Glucosidase at 1000 µg/ml. In glucose diffusion, it showed highest activity at a concentration of 1500 µg/ml. Also, it had excellent nitric oxide scavenging activity and maximum percentage inhibition of 86.12±1.01 was observed at 1500 µg/ml. Acute toxicity study supported the tolerance level even at the...
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Posted by admin on Mar 1, 2016 in |
High-throughput Liquid chromatography–mass spectrometry method has been developed and validated for the quantification of Linagliptin in human plasma using Linagliptin D4 as an internal standard (ISTD). Following solid phase extraction (SPE) in 96 well plate format, the analyte and ISTD were run on phenyl hexyl, 100A 100 X 4.6mm, 2.6µusing an isocratic mobile phase consisting of 10mM Ammonium formate buffer (pH 6.5 ± 0.5): Methanol 15:85 v/v. The precursor and productions of the drugs were monitored on a triple quadrupole instrument operated in the positive ionization mode. The method was validated over a concentration range of 99.532-10045.049pg/mL with relative recoveries ranging from 69.9 to 77.1%. The inter batch precision (%CV) across three validation runs was≤ 2.9%.The Inter batch accuracy determined at four QC levels (LLOQ, LQC, MQC and HQC) was between 95.2–102.7%. According to the validated results, the proposed method was found to be specific, accurate, precise and high throughput method and could be used for the estimation of Linagliptin in human plasma and can be applied for the...
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