1. | UV SPECTROPHOTOMETRY METHOD FOR THE ESTIMATION OF AMINOPHYLLINE IN BULK AND PHARMACEUTICAL FORMULATIONS |
| Sonja Jose*, Ajith Kumar A, Rathana K |
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The main objective was to develop and validate the UV spectrophotometric method for the estimation of aminophylline in bulk and its tablet dosage formulations as per ICH guidelines. Distilled water is used as a solvent. the λ max of the Aminophylline was found to be 272 nm. The linearity in the concentration range 5-30 µg/ml with correlation co efficient of 0.9996. The accuracy studies of proposed method was performed at three different levels, 20%, 40%, 60% and recovery was found to be in the range of 100.82%. The limit of detection and limit of quantification were found to be 0.0383 and 0.1160 (µg/ml respectively. The % RSD less than 2 which indicates the accuracy and precise of the method the above method was a rapid tool for routine analysis of aminophylline in the bulk and its tablet dosage forms.
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2. | SYNTHESIS, CHARACTERIZATION & ?-LACTAMASES ACTIVITY OF 4-THIAZOLIDINE DERIVATIVES |
| Bharat Kumar Tyagi and Chandra Kishore Tyagi |
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Some novel 4-thiazolidinone derivatives have been synthesized by the condensation of isatin/5-chloroisatin with thiosemicarbazide to yield thiosemicarbazones, which were then cyclized to form corresponding thia-3,4, 9-triaza-fluoren-2- ylamines. These were reacted with substituted aldehydes to give corresponding Schiff bases, which were cyclized using thioglycolic acid in the presence of zinc chloride to obtain the 4-thiazolidinone derivatives. All the synthesized compounds were characterized by spectral (IR, MS and NMR) and elemental analysis. The compounds were screened for their antibacterial activity against Gram-positive bacteria (B. subtilis, S. aureus, B. pumilus and M. luteus), Gram-negative bacteria (P. aeruginosa, E. coli and P. fluorescens) and for antifungal activity against A. niger and P. chrysogenum by agar-diffusion method. The minimum inhibitory concentrations of these compounds were also determined by tube dilution method. The antimicrobial effectiveness of all the compounds was found to be concentration dependent. Two compounds—2- methyl-3- (1-thia-3, 4, 9-triaza-fluoren-2-yl)-thiazolidin-4- one (7aI) and 2-naphthalen-1-yl-3-(1-thia-3, 4, 9-tri aza-fluoren-2-yl)- thiazolidin-4-one (7aII)—exhibited good antibacterial activity. The antibacterial activity of all the compounds was found to be better than the antifungal activity.
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3. | DEVELOPMENT AND VALIDATION OF RP-HPLC METHOD OF SIMULTANEOUS ESTIMATION FOR DONEPEZIL AND MEMANTINE TABLET DOSAGE FORMS |
| Sonja jose, Ishwarya.P.J, Monisha.R, Sonu.S, Vignesh sharma.G |
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To develop a simple, cheap, accurate, and rapid Reverse Phase High Performance Liquid Chromatographic (RPHPLC) method and validate as per ICH guidelines for estimation of donepezil and memantine in pharmaceutical dosage forms. The separation was conducted by using mobile phase consisting of phosphate buffer: methanol in the ratio (70:30). The wavelength was found at 273nm. HPLC alliance with empower software is used for chromatographic determination. The separation was conducted by using inertsil C-18 (4.6×250mm×5μm) at the flow rate of 1.0 ml/min using variable wavelength detector. The developed method resulted in donepezil and memantine eluting at 5.067 min and 2.003min. The method was found to be linear over the concentration range 25-125μg/ml with coefficient regression R2-0.999. Mean recovery was found to be in the range of 99.8%, during accuracy studies. The limit of detection (LOD) was found to be 2.75mg/ml and 3.14mg/ml. The limit of quantitation (LOQ) was found to be 9.96mg/ml and 10.05 mg/ml respectively. A cheap, accurate, precise, linear and rapid RP-HPLC method was developed and validated for the quantitative estimation of Donepezil and memantine as per ICH guidelines.
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4. | STRUCTURE BASED MOLECULAR DOCKING ANALYSIS OF QUINAZOLINE DERIVATIVES AGAINST Mycobacterium tuberculosis |
| Vismaya KV* and Vijayakumar B |
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Tuberculosis remains a worldwide public health problem despite the fact that the causative organisms was discovered more than 100 years ago and highly effective drugs and vaccines are available making tuberculosis a preventable and curable disease. In this paper we report the molecular docking studies of 30 quinazoline derivatives having antitubercular activity. The derived compounds were analyzed for drug likeliness based on the Lipinski’s rule of Five and docking study was performed between receptor and ligands by Autodock vina with PyRx and visualized by Biovia Discovery studio 2020 client. Docking studies have shown that the quinazoline derivatives interacts and bind efficiently with 1P44 (enoyl-acyl carrier protein reductase (InhA)) enzyme which resulted in antitubercular activity.
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5. | METHOD DEVELOPMENT FOR THE ESTIMATION OF LUPEOL IN ITS GEL FORMULATION |
| Srikanth A*, M.Purushothaman, Shiva Kumar Tejavath, R. Shankar Sheshu, S. Selva Kumar |
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Lupeol is a triterpenoid pentacyclic compound that is known for its anti-inflammatory and anti-cancer properties. Its activities are based on its anti-oxidant potential. Lupeol has been found to have a contraceptive effect due to its inhibiting effect on the calcium channel of sperm (CatSper). Lupeol has also been shown to exert anti-angiogenic and anti-cancer effects via the downregulation of TNF-alpha and VEGFR-2. Famous anti-inflammatory ethno-medicinal plant Camellia japonica contains anti-inflammatory component lupeol in its leaf. In order to determine the drug in biological fluid or in pharmaceutical preparations, there are no. of methods available, that is HPTLC, HPLC, and spectrophotometery. It can be concluded that the proposed method is simple, rapid, accurate, precise, economic and reproducible for UV spectrophotometric estimation of lupeol from pharmaceutical formulation. This method can be successfully applied for routine estimation of lupeol in bulk and pharmaceutical dosage form.
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