Posted by admin on Dec 31, 2020 in |
The present LC-MS/MS method for estimation of Nitecapone in human plasma using Tolcapone as an internal standard is established and validated as per FDA guidelines. A good response was obtained with ZORBAX Eclipse plus C18 column (150 mm × 4.6 mm ID, 5 μm) and mobile phase with a mixture of 0.01 M Ammonium phosphate buffer with pH adjusted to 5.0 with OPA and Acetonitrile (70:30, v/v) at a flow rate of 0.8 mL/min by positive ion mode (API 4000) with an injection volume of 20 µL and a run time of 3.0 min. Detection is performed by atmospheric pressure electrospray ionization (ESI) tandem mass spectrometry in positive ion mode. The precursor to product ion transitions is m/z 266.20 to 156.20 for Nitecapone and m/z 274.20 to 183.10 for Tolcapone (Internal standard) were used for quantization. The retention time of Nitecapone and Tolcapone (Internal standard) were found to be 2.12 min and 2.58 min, respectively. Linearity established for Nitecapone in the range of 50 ng/mL to 2000 ng/mL with...
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Posted by admin on Dec 31, 2020 in |
Chlorthalidone is a long-acting diuretic recommended for treatment of oedema associated with congestive heart failure. It is oral active diuretic mainly acting on distal convoluted tubule of nephron. Chlorthalidone is poorly soluble in water at room temperature. Nanoparticles have great potential as a carrier and can improve the solubility of poorly water-soluble drugs like chlorthalidone. The aim of the present study was to formulate and optimize the chlorthalidone nanoparticles using Box-Behnken factorial design approach. Effect of three independent variables (concentration of polymer, amount of surfactant and ultrasonication frequency) on two dependent variables such as particle size and dissolution of the drug was studied. The nanoparticles of chlorthalidone were formulated by anti-solvent precipitation-ultrasonication-freeze drying technology to improve its solubility and dissolution. The samples were characterized using Horiba nanoparticles analyzer, Zeta potential analyzer, Differential Scanning Calorimetry (DSC), Fourier Transform Infrared Spectroscopy (FTIR), Powder X-ray Diffraction (PXRD), and Field Emission Scanning Electron Microscopy (FESEM). The average particle size of 342.5 nm with a Polydispersibility index 0.158 was confirmed by dynamic light scattering....
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Posted by admin on Dec 31, 2020 in |
Ruthenium(II) complexes of the type [Ru(bpy) 2(L)](PF6)2, where L= 2-{4,5-bis[(E)-2-phenylethenyl]-1H-imidazol-2-yl}-1H-benzimidazole (1), 2-{4,5-bis[(E)-2-(4-chlorophenyl)ethenyl]-1H-imidazol-2-yl}-1H-benzimi-dazole (2), 2-{4,5-bis [(E)-2-(4-fluorophenyl) ethenyl]-1H-imidazol-2-yl} -1H-benzimidazole (3), 2-{4 ,5-bis[(E)-2- (4-methylphenyl) ethenyl] -1H-imidazol-2-yl }-1H-benzimidazole (4), 2-{4, 5-bis[(E)-2-(4-methoxyphenyl) ethenyl]-1H-imidazol-2-yl}-1H-benzimidazole (5) have been synthesized and characterized by elemental analyses and spectral (IR, UV-vis, NMR, ESI-MS) techniques. The redox behavior of the complexes has been studied by cyclic and differential pulse voltammetry. In acetonitrile solution, all the complexes exhibit characteristic metal to ligand charge transfer (MLCT) absorptions and ligand-based transitions. The complexes showed efficient DNA cleavage activity in the presence of light at the wavelength of 480 nm. The complexes are also able to cleave supercoiled pUC19 plasmid DNA via guanine base oxidation in a concentration-dependent manner. In-vitro cytotoxic activity of the complexes shows that complex 1 has better anticancer activity against MCF7 human breast cancer cells with an IC50 value of 7.9 µM. The antimicrobial activities of the ligand and their metal complexes were screened by agar diffusion method and found that the metal complexes have higher antimicrobial activity than the...
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Posted by admin on Dec 31, 2020 in |
The increasing public concern on the use of synthetic fungicide and resistance development led to an increase in search for alternative control strategies. Medicinal plants serve as therapeutic agents as well as important raw materials for the manufacture of traditional and modern medicine. Considering the vast potential of plants as sources for antimicrobial drugs with reference to antifungal agents, a systematic investigation was undertaken to explore the antifungal potential of few medicinal plants. In present study, in-vitro antifungal activities of few medicinal plant extracts were evaluated against two well-known plant pathogens i.e., Fusarium oxysporum (MTCC 284) and Cladosporium herbarum (MTCC 351). Fourteen plant ethanolic extracts were prepared, and out of them, five plants; Allium sativum, Zingiber officinale, Mentha spicata, Carica papaya and Elettaria cardamomum showed good antifungal activity. A. sativum ethanolic extract showing maximum antifungal activity was further subjected to carry out other studies. MIC values of ethanolic extract of A. sativum against F. oxysporum (MTCC 284) and C. herbarum (MTCC 351) were found to be 60 mg/ml and...
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Posted by admin on Dec 31, 2020 in |
A simple, reliable, and sensitive liquid chromatography-tandem mass spectrometry (LC-MS/MS) method has been developed and validated for the determination of lacosamide, an antiepileptic drug, in human plasma. The lacosamide and internal standard (IS) have been extracted by a simple liquid-liquid extraction method and separated on C18 (50 × 4.6 mm, 5μm) column with the mobile phase of 5mM ammonium formate and methanol (50:50, v/v), pumped at flow-rate of 0.5 mL/min. The ion transitions were monitored in positive ion mode [M+H]+ at m/z 251.20 >91.10 for lacosamide and m/z 256.10>211.10 for IS. Method validation revealed excellent linearity over the concentration range of 9 – 9000 ng/mL together with satisfactory intra and inter-assay precision, accuracy, and extraction recoveries. Lacosamide was found stable throughout the various sample handling and processing conditions. It is proposed to evaluate the performance of the developed method by measurement of a plasma concentration of lacosamide versus time in four epileptic patients to monitor pharmacokinetic behavior of it. The variation in estimated pharmacokinetic parameters shows the need for...
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