ANALYTICAL METHOD EVELOPMENT AND VALIDATION FOR ANTI ASTHAMATIC DRUG OXYMETAZOLINE HYDROCHLORIDE IN NASAL SPRAY FORMULATIONS BY RP-HPLC

A new, simple, accurate and economic reverse-phase HPLC method has been developed for quantification of Oxymetazoline Hydrochloride in nasal spray formulations. This developed method has been validated according to International Conference on Harmonization (ICH) guideline with respect to system suitability, specificity, precision, linearity, accuracy, and robustness. An isocratic condition of mobile phase Phosphate buffer (pH 3.0): Acetonitrile in a ratio of 60:40, v/v at a flow rate of 1.0 mL/minute over RP C18 (octadecylsilane (ODS), 250 × 4.6 mm, 5 µm, ECLIPSE X DB C-18) column at ambient temperature was maintained. This method is specific and showed excellent linear response with correlation coefficient (R2) values of 0.999, which was within the limit of correlation coefficient (R2 0.995). A  simple  and accurate reversed-phase  HPLC  method  for  the  analysis  of  Oxymetazoline Hydrochloride in  nasal spray formulations was developed and validated successfully

A study of method development and validation for estimation of Azelastine hydrochloride in nasal spray formulations by RP-HPLC method

A simple reverse-phase HPLC method for the estimation of Azelastine hydrochloride in nasal spray formulations has been developed. The method is simple, accurate, precise, specific and linear over the analysis range. This developed method has been validated according to International Conference on Harmonization (ICH) guideline with respect to system suitability, specificity, precision, linearity, accuracy, and robustness. An isocratic condition of mobile phase comprising Phosphate buffer (pH 3.1): Acetonitrile in a ratio of 60:40, v/v at a flow rate of 1.0 mL/minute over RP C18 (octadecylsilane (ODS), 250 × 4.6 mm, 5 µm, CHROMOSIL) column at ambient temperature was maintained. Besides, the chromatographic peak was observed sharp & symmetric. The proposed method was successfully applied for the estimation of the Azelastine hydrochloride in nasal spray formulation

Synthesis, characterization and antimicrobial screening of some novel chalcones and their derivatives

1642-1648  Synthesis of some novel 2-(4-(allyloxy)-3-methoxyphenyl)-4H-chromen-4-ones 5a-f and 2-(4-(allyloxy)-3-methoxyphenyl)-3-chloro-4H-chromen-4-ones 6a-f by oxidative cyclisation of (E)-3-(4-allyloxy)-3-methoxyphenyl)-1-(2-hydroxyphenyl)prop-2-en-1-ones using DMSO/I2 and DMSO/CuCl2 at reflux condition has been carried out. A useful and efficient synthetic strategy for the synthesis of 4-allyloxy-3-methoxyphenyl chromones has been reported. The synthesized compounds have been characterized by melting point, FT-IR, NMR and EI-MS spectral data. The synthesized compounds have been evaluated for their antibacterial and antifungal activities. Most of the compounds are found to be of comparable potency when compared with the reference standard drugs

The QUALITY BY DESIGN APPROACH FOR SIMULTANEOUS DETERMINATION OF FLUTICASONE PROPIONATE AND SALMETEROL XINAFOATE

Objective: To develop and validate a novel and simple reverse phase Ultra Performance Liquid Chromatography (UPLC) method for simultaneous determination of Fluticasone Propionate and Salmeterol Xinafoate from pharmaceutical finished product, applying Quality by design (QbD) approach. Methods: The proposed analytical method developed and validated in a linear gradient condition at a flow rate of 0.40 ml/min over Waters ACQUITY BEH Shield RP 18, 2.1*100 mm, 1.7 µm column by maintaining column oven temperature at 30 °C and Sample cooler temperature at 15 °C. Chromatograms monitored and recorded at 215 nm. Results: The proposed method has been validated as per International Conference on Harmonization (ICH) guidelines with respect to system suitability, specificity, precision, linearity, accuracy, range, solution stability and robustness. This method is qualified in all parameters in case of system suitability and specificity; precision observed within the limit of 2.0%, the excellent linear response observed with correlation coefficient (R2) for Salmeterol 0.99999 and Fluticasone Propionate 0.99999, for Accuracy within the limit of 98% to 102%. Conclusion: A selective, suitable and accurate reverse phase UPLC method for simultaneous Determination of Fluticasone Propionate and Salmeterol Xinafoate in the pharmaceutical finished product has been developed and validated successfully

Baker’s yeast: An efficient, green, and reusable biocatalyst for the one-pot synthesis of biologically important <i>N</i>-substituted decahydroacridine-1,8-dione derivatives

<p>A green approach for one-pot three-component synthesis of <i>N</i>-substituted decahydroacridine-1,8-diones is offered for the first time using baker’s yeast (<i>Saccharomyces cerevisiae</i>) as a biocatalyst under ultrasonication. Due to growing safety and environmental concerns, enzymatic methods were constantly investigated as an attractive alternative to toxic and nonspecific chemical approaches. This method is relatively simple, efficient, inexpensive, and environment-friendly. The catalyst was recovered and reused and also the recyclability of baker’s yeast resulted in excellent yields of products without loss of any catalytic activity.</p

Synthesis and Antimicrobial Activity of New Carbohydrazide Bearing Quinoline Scaffolds in Silico ADMET and Molecular Docking Studies

In search of a more potent and new series of fluorine-containing quinoline, hybrid Schiff bases (6a–o) analogues were synthesized by a facile and efficient conventional method. They were developed via condensation of quinoline-4-carbohydrazide intermediate and aromatic aldehydes in presence of ethanol. All compounds viz., 6a–o were efficiently synthesized in good yields in ranges of 76–84%, respectively. All synthesized compounds were well characterized by using various spectroscopic techniques such as FT-IR, 1H NMR, 13C NMR, Mass spectroscopy. Moreover, all newly synthesized hybrid Schiff bases (6a–o) have been screened for their antifungal and antibacterial activity. Among these compounds (6a–d) shows good antibacterial activity, while compound 6b was found to be effective against a fungal pathogen Aspergillus niger and compound 6a was found to inhibit the visible growth of Staphylococcus aureus ATCC 6538 at low concentration with MIC 340 µg/.</p

Synthesis and Antitubercular Activity of New Benzo[<i>b</i>]thiophenes

<i>In vitro</i> and <i>ex vivo</i> efficacies of four series of benzo­[<i>b</i>]­thiophene-2-carboxylic acid derivatives were studied against <i>Mycobacterium tuberculosis</i> H37Ra (MTB). Benzo­[<i>b</i>]­thiophenes were also tested <i>in vitro</i> against multidrug resistant <i>Mycobacterium tuberculosis</i> H37Ra (MDR-MTB), and <b>7b</b> was found to be highly active against A- and D-MDR-MTB/MTB (MIC ranges 2.73–22.86 μg/mL). The activity of all benzo­[<i>b</i>]­thiophenes against <i>M. bovis</i> BCG (BCG) was also assessed grown under aerobic and under conditions of oxygen depletion. Compounds <b>8c</b> and <b>8g</b> showed significant activity with MICs of 0.60 and 0.61 μg/mL against dormant BCG. The low cytotoxicity and high selectivity index data against human cancer cell lines, HeLa, Panc-1, and THP-1 indicate the potential importance of the development of benzo­[<i>b</i>]­thiophene-based 1,3-diketones and flavones as lead candidates to treat mycobacterial infections. Molecular docking studies into the active site of DprE1 (Decaprenylphosphoryl-β-d-ribose-2′-epimerase) enzyme revealed a similar binding mode to native ligand in the crystal structure thereby helping to understand the ligand–protein interactions and establish a structural basis for inhibition of <i>MTB</i>. In summary, its good activity in <i>in vitro</i> and <i>ex vivo</i> model, as well as its activity against multidrug-resistant <i>M</i>. <i>tuberculosis</i> H37Ra in a potentially latent state, makes <b>7b</b> an attractive drug candidate for the therapy of tuberculosis