Posted by admin on Feb 28, 2019 in |
In the present study, comprehensive stress testing of Carfilzomib, a newly approved proteasome-inhibiting anticancer drug was carried out according to ICH guideline Q1A (R2). The drug was subjected to acid (0.1N HCl), neutral and alkaline (0.1N NaOH) hydrolytic conditions at 70 ºC, as well as to oxidative decomposition at room temperature. Photolysis was carried out in 0.1N HCl, water and 0.1N NaOH at 40 ºC. LC-PDA and LC-MS investigated the products formed under different stress conditions. The LC-PDA method that could separate all degradation products formed under various stress conditions involved a C18 column and a mobile phase comprising of ACN and phosphate buffer (pH 3). The flow rate and detection wavelengths were 1 ml/min and 220 nm, respectively. The developed method was found to be precise, accurate, specific and selective. It was suitably modified for LC-MS studies by replacing phosphate buffer with water, where pH was adjusted to 3.0 with formic acid. The drug showed instability in the solution state (under acidic, neutral, alkaline and oxidative stress conditions),...
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Posted by admin on Feb 28, 2019 in |
A series of conjugation of two heterocycles 1, 3, 4-oxadiazole and quinazolone were synthesized and screened for antimicrobial as well as antioxidant activity. Compound4-(4-oxo-2-phenyl-quinazoline-3(4H)-yl)-benzohydrazide 3 on cyclization with different aromatic acids in the presence of phosphoryl chloride (POCl3) give different 1, 3, 4-oxadiazole derivatives. Similarly, compound 3 on reaction with carbon disulphide (CS2) gives substituted oxadiazole thione which on reaction with different halides in the presence of dimethylformamide (DMF) give oxadiazole thiones analogs 6a-6c. Structural assignments of these compounds have been made by elemental analysis, UV, IR, 1H NMR, and mass spectral data. Synthesized analogs were screened for in-vitro growth inhibition activity against different strains of bacteria and fungi and compared with standard drugs ciprofloxacin and fluconazole. Compounds 4e and 4f have good activity against bacteria. All compounds have moderate activity against fungi. These compounds were screened for antioxidant activity by using radical scavenging DPPH assay by using ascorbic acid as a standard drug. Compounds 4e, 6a to 6c have good antioxidant...
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Posted by admin on Feb 28, 2019 in |
Samanea saman is a tropical avenue tree which is widely cultivated in Northern America, and Asia belongs to the family Leguminosae. It possesses a wide range of biological perspectives. Folklore claims postulated that Samanea saman is having an antiulcer, antioxidant antibacterial and anti-mycobacterial properties. In the present investigation, the methanol extract of leaves of Samanea saman has been prepared based on the polarity and subjected to column chromatography. Based on this principle, the bioactive alcoholic extract (5%) was fractioned over a Silica gel (100-200 mesh) column by eluting with solvents of increasing polarity in the order of benzene: ethyl acetate and methanol. Similar TLC fractions were being combined and characterized by spectral analysis. Spectral data are revealed the presence of phytocompounds from the methanolic fractions of the Samanea saman. It was found that the compound named Pithecolobine showed remarkable activity against Mycobacterium tuberculosis by screening through Alamar blue assay (MIC at 3.12 µg/ml) and Luciferase assay (86% inhibition at 10 µg/ml) apart from other compounds obtained. The compound was...
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Posted by admin on Feb 28, 2019 in |
Free radicals induce numerous diseases by lipid peroxidation, oxidation of monosaccharides and DNA damage. In the present study, the marine plant seagrass Halophila beccarii was exploited to detect the phytochemical constituents and its antioxidant potential. The aqueous and organic extracts of Halophila beccarii portrayed the presence of various metabolites such as phenolic compounds, flavonoids, tannins, and saponins. The antioxidant properties of extracts of Halophila beccarii (Hydrocharitaceae) were studied in four in-vitro models viz. Total antioxidant activity, radical scavenging activity by DPPH reduction Assay, Scavenging of H2O2 and reducing power. The extract was found to contain large amounts of secondary metabolites such as phenolic compounds and flavonoids. Among all the extracts the methanolic extract showed significant antioxidant activity compared with standards. The experimental data provide ample evidence to utilize Halophila beccarii as a novel dietary agent for treating chronic metabolic diseases, such as diabetes and hyperlipidemia and could be used as a potential source for natural health...
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Posted by admin on Feb 28, 2019 in |
The aim of the present research work is to validate the apixaban content in bulk and pharmaceutical dosage formulation and validate it as per ICH guidelines. A simple, rapid, precise and highly selective spectrophotometric method was developed for estimation of apixaban in tablet dosage form by the area under curve method. The area under curve method involves the measurement of absorbances of apixaban at the wavelength of 269 nm-289 nm. Methanol was used as a solvent. Linearity was observed in the concentration range of 5-25 µg/ml for apixaban. The accuracy of the method was confirmed by recovery studies of tablet dosage forms and was found to be 100% for Apixaban. The method showed good reproducibility and recovery with % RSD less than 0.988%. The LOD of apixaban was found to be 0.335 µg/ml, and LOQ of apixaban was found to be 1.015 µg/ml. Thus the proposed method was found to be rapid, specific, precise, accurate and cost-effective quality control tool for the routine analysis of Apixaban in bulk and...
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