Posted by admin on Jun 30, 2021 in |
A simple, accurate, and precise stability-indicating method was developed for the simultaneous estimation of the Netupitant (NTPT) and Palonosetron (PLSN) in a capsule by UPLC. Chromatographic elution was processed through an HSS C18 (100 × 2.1 mm, 1.8m) reverse phase column, and the mobile phase composition of 0.01N KH2PO4 buffer (4.0 pH) and acetonitrile in the ratio of 55:45 was pumped through a column at a flow rate of 0.3 ml/min. The column oven temperature was maintained at 30 °C, and the detection wavelength was processed at 274 nm. Retention times of NTPT and PLSN were found to be 1.682 min and 1.288 min, respectively. Repeatability of the method was determined in the form of %RSD, and findings were 0.9 and 1.0 for NTPT and PLSN, respectively. The percentage recovery of the method was found to be 99.98% and 99.61% for NTPT and PLSN, respectively. LOD, LOQ values obtained from regression equations of NTPT and PLSN were 2.174, 6.587mg/ml and 0.02, 0.05 mg/ml respectively. Regression equation of NTPT was...
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Posted by admin on Jun 30, 2021 in |
Nail plate being a formidable barrier, drug permeation through this layer is limited. Taking this as a challenging task, the present study focuses on the formulation of an antifungal topical nail lacquer using Oxiconazole nitrate. The novelty of the studies can be stated as the use of a combination of permeation enhancers like salicylic acid, thioglycolic acid, and urea for effective therapeutic treatment of topical nail infection like Onychomycosis. Results: Optimized formulation F13 was subjected for incompatibility studies followed by post-formulation studies (drying time, water resistance, etc.). Clipping of nail part was examined for in-vitro drug release and anti-microbial activity followed by stability studies of the optimized formulation. The optimized F13 formulation was found to have a thickness (57±0.04µm), folding endurance (183±0.57 mm), and tensile strength (2.62±0.02 Kg/cm2) values, respectively. The FTIR and XRD studies showed no interaction between drug-excipients. Permeation enhancer in the ratio of salicylic acid: thioglycolic acid: urea in hydrogen peroxide (1:1:1) with 5% concentration each showed in-vitro drug release rate of 96.03% at 48 hours...
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Posted by admin on Jun 30, 2021 in |
Schiff base was prepared by using 4-amino-3-hydroxy benzoic acid and 4-nitrobenzaldehyde, namely (E)-3-hydroxy-4-((4-nitrobenzylidene) amino)benzoic acid. In the preparation of rare earth complexes, nitrates of lanthanum, Cerium, and Praseodymium were used with Schiff base. Rare earth Schiff base complexes were prepared by using NaOH to maintain the pH of solvent. Synthesized Schiff base ligand and its complexes were structurally characterized by UV, IR, NMR, HRMS, TGA, and elemental analysis. Structural characterization shows 1:2 metal to ligand ratio in the complexes. The electronic absorption spectra of the ligands and their metal complexes are recorded after preparing the solution and after standing the solution for 3 weeks in DMF. No appreciable change was observed in the spectrum with time. Free ligands and their metal complexes have different electronic spectra’s and blue shift observed in complexes which support the complex formation. HRMS are in good agreement with calculated values, which confirms the proposed structure of ligand. Carboxylate group of Schiff base ligand shows bidentate the coordination to central metal and azomethine group is...
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Posted by admin on Jun 30, 2021 in |
In the present research worked aims to increase the antimicrobial activity of quinoxaline thiosemicarbazide derivatives by substitution of some acetophenones and their antimicrobial evaluation against various antimicrobial strains with molecular docking studies. Lead molecule (1E, 4E)-1-(7-chloro-3-isopropylquinoxalin-2(1H)-ylidene) thiosemicarbazide was synthesized and condensed with various substituted acetophenones to synthesize derivatives. All derivatives were characterized by IR., NMR & Mass spectroscopy. The synthesized derivatives were evaluated in-vitro for antibacterial and antifungal activities against various strains using the agar dilution method. Molecular docking studies of the derivatives (Va – Vg) were performed against E. coli DNA gyrase B and Topoisomerase IV to find out essential binding sites against target protein PDB: 1AJ6 and 1S14, respectively. Among all these compounds,Vf and Vg were found to exhibit more potent activity against Gram –Ve, Gram +Ve bacterial and fungal strains at MIC 0.19 µg/ml, 0.39µg/ml, and 0.78 µg/ml, respectively. The docking studies of all the compounds exhibit potent binding energy, but the compound Vg exhibit interactive binding energy -8.1 and -7.5 kcal/mol to the active pockets...
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Posted by admin on Jun 30, 2021 in |
Rivastigmine is used for the treatment of mild to moderate dementia of the Alzheimer’s type. Transdermal delivery of Rivastigmine is preferable to improve gastrointestinal tolerability. A novel transdermal system with zero-order release kinetics was developed following a hybrid technique in a combination of the micro reservoir and adhesive dispersion system. The transdermal system was prepared by incorporating rivastigmine in adhesive matrix layer in which rivastigmine-loaded microspheres were dispersed. Microspheres were prepared by spray drying using poly-e-caprolactone and maltodextrin (1:1 ratio) as carriers in various drug: polymer ratios. Microspheres with1:2 drug: polymer ratio (A1) showed desired particle size, yield, assay and in-vitro drug release and were found to be suitable for designing the transdermal system. A1 was dispersed into silicon adhesive layer during the preparation of the patch with a calculated amount of rivastigmine. Transdermal patch with 18 mg rivastigmine was optimized by evaluating ratios of adhesive matrix and microsphere content following DOE where 13 formulations were evaluated for various physical and chemical properties. 5 among 13 formulations were found...
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