A novel, safe, economic and sensitive method of spectrophotometric estimation has been developed using Azeoptropic mixture (water:methanol: 60:40, v/v) for the quantitative determination of Lornoxicam, a practically water-insoluble drug. Hence, Lornoxicam stock solution was prepared in Azeoptropic mixture. Lornoxicam showed maximum absorbance at 383 nm. Beer's law was obeyed in the concentration range 4–24 μg/mL with regression coefficient of 0.999. The method was validated in terms of linearity (R2=0.999), precision (CV for intra-day and inter-day was 0.28–0.68 and 0.12–0.92, respectively), accuracy (98.03–100.59% w/w) and specificity. This method is simple, precise, accurate, sensitive and reproducible and can be used for the routine quality control testing of the marketed formulations.
Enzymes play very important role in living organism as biocatalyst. They play vital role like secretion, metabolism, digestion, DNA functions, reproduction, conversation of molecules and many other functions of body. By inhibiting specific enzymes, we can cure numerous pathological conditions in humans like inhibiting HMG CoA reductase, we can decrease cholesterol synthesis which is very useful in atherosclerosis and also use for heart diseases. ACE inhibitors can reduce concentration of Angiotensin II and use to reduce blood pressure. Many of them use as pesticides and herbicides in agriculture field. The history says enzyme inhibitors are use as arrow poison and use to kill animals by developing paralysis in them. Using a digital technology scientist identified number of enzymes and their functions as well as their 3D structure. We can easily design their inhibitors and use as medicine to treat pathological conditions. So, enzyme inhibitors became first choice for medicinal chemist and scientist as a target and play extremely important role in future as medicinal compounds and became a safe option compared to other available options.
The main aim of present work is to identification of potency of novel quinoline-4-one derivatives as a factor Xa inhibitors by in-silico ADME study and molecular docking study. Factor Xa is enzyme which play major role in blood coagulation process by conversation of prothrombine to thrombine. Thrombine is the protein which converts fibrinogen to fibrin (clot). Inhbition of factor Xa is altimetly inhbition of blood coagulation process. Due to the abnormal blood coagulation, serious to very serious problems can create and will lead to death. Betrixaban, Rivaroxaban, Epixaban and Edoxaban which are FDA approval dugs as factor Xa inhibitors. They are very potent drugs and very few side effects compare to other available anti-coagulating drugs so they was taken as a reference molecules for current study. Some novel quinoline-4-one derivatives was design and screened for factor Xa enzyme. We design 26 compounds and first they screen for in-silico ADME parameters. Very few compounds not pass Lipinski rule. A majority compound shows excellent in-silico ADME properties. In molecular docking study almost all compound shows near binding energy to reference drug and shows almost near dock score. Q23 and Q26 show excellent inhibitory activity against Factor Xa. 13 molecules shows very near dock score compare to reference drugs. This study became a reference and provides valuable data for the synthesis, in-vitro and in-vivo evaluation of quinolone-4-on derivatives as Factor Xa inhibitors.
A rapid, specific and sensitive reverse phase high performance liquid chromatographic (RP-HPLC) method was developed for the determination of Tolperisone Hydrochloride (TOLP) in bulk and tablet dosage form. The method involved an isocratic elution of TOLP on C 18 column (250 X 4.6 mm, 5 µm) using a mobile phase composition of acetonitrile: 20 mM ammonium acetate buffer containing 0.1% triethyl amine (55:45 v/v) (pH 4.0 adjusted by glacial acetic acid), at a 1.0 ml/min flow rate. The analyte was monitored at 260 nm wavelength. The retention time for tolperisone was found to be 2.50 min. Linearity was established in range of 12.5 -100 µg/ml with correlation coefficient 0.999. The % recovery was obtained as 98.38 -101.58 %. The detection limit and quantitation limit were found to be 0.172 and 0.521 respectively. This method can be successfully employed for quantitative analysis of TOLP in bulk and pharmaceutical dosage form as its accuracy, precision, specificity and reproducibility.
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