Ternary copper(II) complexes of salicylaldehyde-histamine Schiff base (HL) and pyridyl ligands, viz. [Cu(bpy)(L)](ClO 4) (1) and [Cu(dppz)(L)](ClO 4) (2), where bpy is 2,2-bipyridine (in 1) and dppz is dipyrido[3,2-a:2 ,3-c]phenazine (in 2), were synthesized, characterized and their DNA binding, photo-activated DNA cleavage activity and photocytotoxicity studied. The 1:1 electrolytic one-electron paramagnetic complexes showed a d-d band near 670 nm in aqueous DMF (1:1 v/v). The crystal structure of complex 1 showed the metal in CuN 4 O distorted square-pyramidal geometry. Complex 2 intercalatively binds to calf-thymus (ct) DNA with a binding constant (K b) of ∼10 5 M −1. It exhibited moderate chemical nuclease activity but excellent DNA photocleavage activity in red light of 647 nm forming • OH radicals. It showed remarkable photocytotoxicity in human cervical cancer cells (HeLa) giving IC 50 of 1.6 μM in visible light (400-700 nm) with low dark toxicity. The photo-induced cell death is via generation of oxidative stress by reactive oxygen species.
A selective and sensitive novel methods were developed and validated for identification and trace level quantification (0.5 ppm) of genotoxic impurities Methyl 3‐amino‐4‐methylbenzoate, 3‐amino‐4‐methylbenzoic acid, and 3‐(4‐methyl‐1H‐imidazol‐1‐yl)‐5‐(trifluoromethyl) aniline in Nilotinib dihydrochloride active pharmaceutical ingredient by using liquid chromatography‐tandem mass spectrometry. The developed and validated methods were more accurate and capable to confirm the m/z values of parent and fragment ions through mass spectrometry and tandem mass spectrometry for further fragmentation. In addition, the developed methods were validated through current regulatory guidelines with a lower detection level of 0.15 ppm and a quantification level of 0.5 ppm for all the three genotoxic impurities. The correlation coefficient was observed as 0.9997 for Methyl 3‐amino‐4‐methylbenzoate genotoxic impurity‐I, 0.9998 for 3‐amino‐4‐methylbenzoic acid, and > 0.9999 for 3‐(4‐methyl‐1H‐imidazol‐1‐yl)‐5‐(trifluoromethyl) aniline. The recovery percentage of all the three genotoxic impurities was found to be between 93% to 105%.
A zoisite group of mineral samples from different localities are used in the present study. An EPR study on powdered samples confirms the presence of Mn(II), Fe(III) and Cr(III) in the minerals. NIR studies confirm the presence of these ions in the minerals.
A selective and sensitive novel method was established and validated for well-characterized tert-butyl ((1S, 3R)-3- acetylcyclopentyl) Carbamate (Acetyl BOC) and tert-butyl (1S, 3R)-3-hydroxycyclopentyl) Carbamate (Hydroxy BOC) genotoxic impurities in Bictegravir sodium active pharmaceutical ingredient by using liquid chromatographytandem mass spectrometry. The developed method was more accurate and capable to confirm the m/z values of parent and fragment ions, method was validated through ICH guidelines to detect 0.3 ppm and estimate up to 1.0 ppm of both impurities. The correlation coefficient was observed > 0.9993 and the recovery percentage of genotoxic impurities was found to be between 93% to 108%.
The current study mainly focused on treating cardiovascular diseases such as angina pectoris and chronic hypertension by modifying the existing commercial tablet available for Nifedipine. The limitation of Nifedipine is poor solubility, which comes under BCS class II drug category, which needs improvement in formulation to achieve better bioavailability. The objective of this research work is to enhance the oral bioavailability (first-pass metabolism in the liver (42–56%)) of Nifedipine by improving dissolution property. Sublingual fast dissolving tablets of Nifedipine formulated by sublimation method, designed to increase its disintegration time in the presence of saliva. This formulation is helpful for paediatric and geriatric patients who are unable to swallow the conventional tablet. Sublimation of camphor makes the tablet more porous and improve disintegration time as well. The direct compression method is used with different ratio of Croscarmellose Sodium (CS) and Sodium Starch Glycolate (SSG) as super disintegrants to formulate Nifedipine loaded Sublingual tablets. All formulations contain various ratio between super disintegrants and camphor, followed by the sublimation method. FTIR and DSC studies were conducted to investigate compatibility between drugs and disintegrants. Formulated tablets were subjected for precompression parameters, e.g., bulk density, tapped density, Carr’s index, Hausner’s ratio, angle of repose and for post-compression parameters, e.g. weight variation, thickness, hardness, friability, drug content, wetting time, disintegration time followed by dissolution study and found satisfactory as per IP.
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