Posted by admin on Apr 30, 2020 in |
Sitagliptin was invented in 2006 as a DPP-4 inhibitor. It is soluble in water to the extent of 0.03 mg/mL as thus suffers bioavailability problems. It was converted into phosphate monohydrate salt with solubility 50 mg/mL, which solved bioavailability problems. In this research, an attempt is made to convert it from its crystalline form into spherical crystals. Spherical crystals have better bulk properties and can adapt to direct compression tableting. This kind of innovation saves the time needed for granulation and can be compressed directly just by adding lubricant and disintegrant. In this research sitagliptin, phosphate monohydrate was made as spherical crystals using water as a solvent, ethanol as anti-solvent, and chloroform as bridging liquid. 32 factorial designs for optimization was applied to get an optimized batch with a concentration of bridging liquid and anti-solvent as independent and Carr’s index and yield as dependent variables. Batch F7 was considered optimized with a yield of 97.5%. Spherical crystals thus obtained were characterized using X-Ray diffraction, SEM, % compressibility, and flowability....
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Posted by admin on Apr 30, 2020 in |
The kinetic of conjugated reactions of S-oxidation and perhydrolysis of Mezlocillin (Mezl) with potassium caroate in alkaline medium is studied by the increase of forming product light absorbance at 290 nm. Baypen® – powder Mezl sodium monohydrate in flacons for preparation of solution for injections (Mezl 1.0 g). Peroxomonosulfate acid as triple potassium salt 2КНSO5∙КНSO4∙K2SO4 (Oxone®) of “extra pure” qualification was used as oxidant. A scheme of peroxoacid oxidation and perhydrolysis conjugated reactions of Mezl by means of potassium caroate is proposed. A new spectrophotometric method for quantitative determination of sodium Mezl in Baypen ® preparation using potassium caroate (KHSO5) as analytical reagent was proposed. At pH 3-4 for 1 mole of penicillin, 1 mole of KHSO5 is consumed, the quantitative interaction is achieved within a time of more than 1 min (observation time). The results were obtained by the recommended procedure for seven replicate titrations of mixtures containing the three species at various concentrations. RSD = 1.32%, δ = +0.49%. It can be seen that Mezl can be...
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Posted by admin on Apr 30, 2020 in |
The present project was conducted with the objective of developing and validating a RP-HPLC method for the simultaneous estimation of aspirin, clopidogrel bisulphate, and rosuvastatin calcium in fixed-dose combination capsule. The chromatographic separation was carried out on Agilent 1260 series using Waters C18 (250 × 4.6 mm, 5 μ) column as the stationary phase and acetonitrile (ACN): phosphate buffer pH 3, gradient mode at a flow rate of 1.2 ml/min and detection at 230 nm. The validation of the developed method was conducted as per the ICH guidelines Q2 (R1). The retention time of aspirin, rosuvastatin calcium and clopidogrel bisulphate was found to be 3.2 min, 4.7 min, and 12.8 min, respectively, under the optimized chromatographic conditions. The developed method was linear in the concentration range of 6.25-400 μg/ml for aspirin, rosuvastatin calcium, and clopidogrel bisulphate. The developed method was specific, with a mean percent recovery of the three drugs in the range of 99-101%. The relative standard deviation (RSD) was less than 2 in the intraday and inter-day...
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Posted by admin on Apr 30, 2020 in |
Glioblastoma (GBM), with restricted therapy alternatives, is a catastrophic primary brain tumor. The receptor of the epidermal growth factor receptor (EGFR) in glioblastomas is recurrently enhanced, over articulated, or mutated, but up to 20 percent of GBM patients find it to be responded to kinase inhibition of EGFR. Several inhibitors of EGFR tyrosine kinase (TKI) failed clinically, due in part to acquired resistance. To automatically examine this type of resistance, we used molecular docking and swissADME approach to elucidate its putative inhibitor. We have attempted to determine a drug candidate in the current research based on the discovery of structural drugs. Docking simulation was conducted on mutated EFGR to determine the best drug candidate from Erlotinib, a renowned anti-cancer agent, derivatives. A total of 200 structures were selected for the 2D crystal structure of erlotinib based on molecular fingerprinting. Top 10 best-docked proteins were analyzed using UCSF Chimera and discovered the complicated atomic-scale properties between ligand and the target protein. SCHEMBL13087058 ligand selected based on hydrogen bonding with methionine...
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Posted by admin on Apr 30, 2020 in |
Background: Medication errors (MEs) are the potential to cause adverse clinical outcomes. The incidence of MEs is hopefully controlled with patient-centric pharmaceutical services. The present study evaluated the incidence of MEs in various departments in a multispecialty hospital in India. Methods: This prospective observational was analyzed 100 prescriptions included 749 drugs from general medicine, cardiology, renal, and endocrinology departments. The prescriptions were analyzed for medication errors as per NCCMERP criteria. The outcome was expressed as range additionally as percentages of variables. Results: A total of 217 MEs (n-105, 48.39%) were ruled out from out of these 100 cases. The applied NCCMERP criteria found 87 drug administration errors (40.09%) with higher categories A and B, but the distribution of category C (n-10) and D (n-10) was noted quite alarming. Conclusion: The study would suggest perpetual inculcation and training programs to be conducted to incorporate cognizance and practice inputs of medicos, nurses, and...
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