Posted by admin on Mar 31, 2021 in |
In the view of an extensive literature survey that revealed the anticonvulsant profile of 1,4-dihydropyridines and 1,3,4-Thiadiazole, we have coupled these two moieties with the aim of achieving an enhanced anticonvulsant effect. In present investigation some of ethyl-1-((5-amino-1, 3, 4-thiadiazol-2-yl) methyl)-5-ethyl-2, 6-dimethyl-4-substituted phenyl-1, 4-dihydro-pyridine-3-carboxylate derivatives are synthesized through four steps. A greener approach is employed by using Chloramine-T as an efficient and safer oxidative catalyst for the synthesis of Thiadiazole and the use of the Microwave technique for accelerating the chemical reactions. The structures of the newly synthesized compounds were confirmed on the basis of IR, 1H-NMR, and Mass analyses. An acute toxicity study was done to determine LD50 of the newly synthesized compounds. Some of the synthesized compounds were evaluated for their anticonvulsant effect by PTZ induced convulsions method. Statistical testing was done by one-way ANOVA followed by Dunnett’s test. The compounds F123 and showed the highest percentage of protection against convulsions at the dose of 15 mg/kg among the evaluated compounds compared to...
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Posted by admin on Mar 31, 2021 in |
Objective: This research article aims to formulate and evaluate orodispersible tablets (ODTs) for Vinpocetine, a nootropic drug used for improving brain functions and cerebral blood flow. This will provide a convenient way for taking medication for dysphagia patients and therefore improve compliance. Methods: Vinpocetine ODTs were prepared by using superdisintegrants. A full mixed 31×41 factorial design was applied to evaluate the effect of two independent variables, namely superdisintegrant type (crospovidone, croscarmellose sodium and sodium starch glycolate) and superdisintegrant concentration (2.5, 5, 7.5, and 10%) on four responses namely friability, disintegration time, wetting time and dissolution percent after 5 min. Compatibility study was carried out using differential scanning calorimetry. Various physico-chemical properties were measured, and in-vivo pharmaco-kinetic study for a selected formula was performed against a conventional tablet market product. Results: Results showed that formulae ingredients were compatible. Crospovidone showed the shortest disintegration time and wetting time. Friability was less than 1%in all formulae, and dissolution percent after 5 min was greater than 80% in all formulae. Statistical evaluation of...
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Posted by admin on Mar 31, 2021 in |
This study was conducted to evaluate gastroretentive metronidazole tablets formulated using Brachystegia eurycoma gum as a matrix. The gum was isolated from powdered dried Brachystegia eurycoma seeds. Gastroretentive metronidazole tablets were produced by direct compression technique using Brachystegia eurycoma gum, sodium carboxymethylcellulose, or their combination as the matrix. Sodium bicarbonate was used as a gas generating agent. The tablets were evaluated based on hardness, friability, weight uniformity, drug content, swelling studies, buoyancy lag time, and total buoyancy time. Hardness ranged from 4.57 ± 0.053 to 11.81 ± 0.90 Kgf. None of the tablets deviated from the mean tablet weight by more than ± 5%. The friability of the tablets was within 0.28 to 1.00% except for formulation MF1 that was 1.93%. Drug content was between 91.51% and 109.53%. The buoyancy lag time was between 2.35 and 20.15 min, and tablets from all the formulations maintained a total buoyancy time of above 12 h. Eighty percent (80%) of metronidazole was released from formulations MF1 to MF5 after 6, 9, 7,...
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Posted by admin on Mar 31, 2021 in |
Objective: Ethyl para toluene sulfonate is a genotoxic impurity and the current work’s primary objective is to develop a hyphenated and highly sensitive LC-MS method for the determination (EPTS) in Perindopril tert-butylamine. Method: EPTS was determined by LC-MS method in selective ion monitoring mode (SIM) using Atlantis T3 (150×4.6mm) 3.0 µm column. 0.01M ammonium acetate is utilized as buffer. Gradient elution was employed and the Mobile phase A is composed of mixture of buffer and methanol in 70:30 (v/v) ratio along with Mobile phase B made up of buffer and methanol in 5:95 (v/v) ratio. The gradient program (T/%B) was set as 0/5, 2.50/5, 7.00/50, 12.00/70, 18.00/95, 21.00/95, 24.00/5, 30.0/5. Results: The LOD and LOQ values found for EPTS were 0.018 µg/mL and 0.054 µg/mL. The method has accuracy within 98.1-103.5% for the analyte. Developed method validated as per International Conference on Harmonization guidelines. Conclusion: Developed LC-MS method in SIM mode can be applied as a good quality control tool for quantitation of EPTS impurity at very low levels...
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Posted by admin on Mar 31, 2021 in |
A new stability indicating Ultra-Fast Liquid Chromatography (UFLC) method was validated for the simultaneous estimation of Metformin hydrochloride (MET) and Vildagliptin (VILDA) in bulk and tablet dosage form as per the International Council for Harmonization guidelines. Chromatography developed on Shimatzu UPLC, X-Bridge C18 column equipped with PDA detector. Mobile phase composed of phosphate buffer (25 mM) pH 3.0: acetonitrile: methanol (85:13:2). Sodium 1-octanesulfonate monohydrate (0.25 g/L) added in aqueous buffer. The effluent was passing through the column 1.0 ml/min at 40 ºC. The retention time of MET and VILDA were found to be 2.964 min and 6.358 min. The specificity study was determined by the addition of known impurities 1-cynoguanidine and vildagliptin amide of MET and VILDA, respectively. The forced degradation studies indicated that MET was stable while VILDA was susceptible to alkaline hydrolysis and peroxide oxidation. The degradation product peaks were well resolved from the MET and VILDA peaks. Purity angle and purity threshold of the MET and VILDA peak showed spectral homogeneity over the entire peak region...
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