Posted by admin on Nov 30, 2018 in |
A novel, sensitive and selective stability-representing RP-UPLC method was developed and validated for the quantitative determination of Erythromycin estolate in Erythromycin 250 mg capsules. The chromatographic separation was achieved on BEH C18; 50 × 2.1 mm; 1.7 µm column by using mobile phase containing a mixture of 0.002M di-potassium hydrogen phosphate and acetonitrile 53:47 v/v at a flow rate of 0.6 ml/min. The column temperature was maintained at 40 °C and detection was carried out at 210 nm. To ascertain the stability-signifying ability of the method, drug product was subjected to strain conditions of acid, base, oxidative, hydrolytic, thermal and photolytic degradation. The drug undergoes degradation at oxidative and thermal / humidity stress conditions. The resultant degrading peaks were well resolved from the drug peak. The drug was found to be stable in thermal and photolytic conditions. The proposed method was validated as per ICH guidelines with respect to specificity, linearity, accuracy, precision and robustness and the method show excellent linearity and a correlation coefficient of more than 0.99....
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Posted by admin on Nov 30, 2018 in |
We investigated the effect of vanadium citrate in the amounts of 0.125, 0.5, and 2.0 µg/mL of water on the enzymatic activity of carbohydrate metabolism, antioxidant system, and the level of lipid peroxide oxidation products in the pancreas of rats with alloxan-induced diabetes. Diabetes was detected at a glucose level of 15.14 mmol/L by measuring glucose level in the blood collected from the tail vein. In the pancreas of rats with experimentally induced diabetes, the levels of lipid hydroperoxides and TBA-positive substances increased significantly, while the level of reduced glutathione and the activity of SOD, CAT, GPx, and GR as well as carbohydrate metabolism enzymes LDH and G-6-PDH decreased as compared to the animals from the control group. With the exposure to vanadium citrate in the pancreas of rats for a month, the level of LPO products decreased and the activity of antioxidant and carbohydrate metabolism enzymes increased as compared to the diabetic animals and dose-dependently reached the level in the animals from the control group. The results obtained...
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Posted by admin on Nov 30, 2018 in |
Quantitative structure activity relationship is among the most widely used computational technology for analogue-based drug design. A molecular modelling approach using sulfadiazine- salicylaldehyde Schiff base analogue as anti-mycobacterial activity from recently reported literature were taken and was designed using MOE 2009.10. Sulfanilamide sulfa drugs have been shown to inhibit dihydropteroate synthetase. In order to develop a pharmacophoric model for this inhibition, quantitative structure-activity relationship (QSAR) for sulfa drugs active against DHPS have been studied. Multiple linear regression analysis was performed to derive quantitative structure activity relationship models which were further evaluated internally as well as externally for the prediction of activity. Accurate minimum inhibitory concentrations (µM) were collected for 19 analogs, and other parameters, such as partition coefficients, molar refractivity, dipole moment, electrostatic interactions, lowest unoccupied molecular orbital (LUMO), highest unoccupied molecular orbital (HOMO), topological polar surface area were calculated. A data set of 19 analogs, all having a common sulphadiazine moiety, provided a cross-validated correlation coefficient (r2) value of 0.5998 and root mean square error value of 0.3829....
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Posted by admin on Nov 30, 2018 in |
Diabetes mellitus relates a metabolic disorder of collective aetiology which is characterized by chronic hyperglycaemia caused due to disturbances of carbohydrate, lipid and protein metabolism due to impaired β cell function of pancreas or insulin resistance or both. Biguanides and Sulphonylureas are the most commonly prescribed drugs due to their efficacy and safety. A total of 60 patients were enclosed in the present study who met the inclusion criteria. They were divided into two groups based on their treatment plan-Group A and Group B. The Group B (P = 0.001) exhibited a significantly greater reduction in HbA1c as compared to Group A (P = 0.002). The reductions in FPG and PPG were also found to be significantly more in the Group B. In the present study, we observed that patients on Metformin-Teneligliptin exhibited better control over glycemic profile as well as lipid profile when compared to patients who are on Metformin-Glimepiride combination. Since, this study was conducted in less number of patients, to make consecutive remarks about the superiority...
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Posted by admin on Nov 30, 2018 in |
In the field of the preparation of chemotherapeutic agents with new mechanism distinct from currently approved drugs is important. However, the clinically effective approved small inhibitor molecule is still lacking. Previous reports indicated that 4-aryl-2-hydrazinothiazole derivatives provided a useful start point to develop HAT inhibitors (histone acetyltransferase). Consequently, preparation and biological evaluation of a focused library of 4-aryl-2-hydrazinothiazole based derivatives as useful as anti-cancer agents. Synthesis of 4-aryl-2-hydrazinothiazoles (1a-d), (2a-d), (3a-c), (4a-b), (5a-b), (6a-b) studied by either conventional method and free solvent microwave one-pot method, and the synthesized compounds were proved by spectroscopic methods (IR, 1HNMR, 13CNMR, GC-Ms, and elemental analysis). The activity against different cancer cell lines and the antimicrobial activities different organisms also studied, and all of the synthesized compounds were of high activity as an antibacterial for gram positive and gram negative; however, it showed also an antifungal activity were the most active compounds were 4a, 4b, 5b, 6a. It was found that all of the prepared thiazoles derivatives were active toward many cell lines (breast,...
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