Posted by admin on Nov 30, 2023 in |
Androgenic hormones such as testosterone and dihydrotestosterone are essential for the progression of the prostate gland. Overexpression of androgenic receptors is responsible for the proliferation of prostate tumours and androgenic receptors are an essential target in prostate cancer therapy. Flutamide was the first Nonsteroidal androgen receptor antagonist used to treat prostate cancer, but it causes side effects such as hepatotoxicity. This study aims to develop less toxic compounds using a bioisosteric approach by replacing groups such as nitro, trifluoromethyl and aryl of Flutamide drug and to improve pharmacokinetic and toxicity prediction as well as docking studies of newly generated bioisosteres. The Lipinski rule of five was followed. In the docking study, docking scores were obtained in the range of -7.76 to -9.75 Kcal/mol. All ligands docked inside the binding pocket region share a shape that is complementary to the androgen receptor. Among the selected bioisosteres and flutamide, the common amino acid residue 746Val plays a key role in the activity and binding affinity. Based on their QED score, toxicity...
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Posted by admin on Nov 30, 2023 in |
Climbazole is a topical antifungal agent commonly used to treat human fungal skin infections such as dandruff and eczema. The goal of research work was to develop and validate a simple, precise, quick, and highly efficient UV spectrophotometric approach for quantifying Climbazole in bulk and shampoo dosage form. The quantification was completed using a twin beam UV spectrophotometer at 222 nm and ethanol (99.9%) as the solvent for the estimate. The Climbazole calibration curve exhibit strong correlation coefficient (R2=0.9938) and high linearity in the range of 5–25 µg/ml concentrations. The accuracy was found to be between 98.21%- 99.83%. The accuracy of the approach was proved by the percent relative standard deviation being less than 2.0%. It was observed that the intraday and interday precision found within acceptable ranges. The method’s sensitivity was assessed using the detection limit and quantification limit, which were discovered to be 2.37 µg/ml and 7.20 µg/ml, respectively. In this paper, we introduce a UV-spectrophotometric technique for investigating Climbazole using ethanol as solvent. The suggested method demonstrated excellent...
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Posted by admin on Nov 30, 2023 in |
A highly sensitive, simple, accurate and precise HPLC-ESI-MS/MS method was developed and validated for the quantitative determination of talazoparib in biological matrices. The present study describes the determination of Talazoparib using validated protein precipitation method from human plasma employing Talazoparib 13C D4 as internal standard by electron spray ionization technique. Combination of 0.1% v/v formic acid and methanol (25:75) % v/v was used as mobile phase. Ascentis Express C18 (50 mm × 4.6 mm, 2.7 µm) column was employed for the separation and the run time was 3 minutes. Flow rate was set at 0.6 ml/min and column oven temperature at 40°C for the chromatographic separation method. 10µl injection volume was selected for mass spectrometer to obtain good ionisation. Parent (Q1) and Product (Q3) ion mass transitions for Talazoparib and Talazoparib-13C-D4 were found at m/z 381.5®180.5 and 386.4®180.5 respectively. The linear regression data for the calibration plot showed a good relationship with high correlation coefficient. Correlation coefficient (r2) value from the standard curve (5-10000 pg/ml) found to be more...
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Posted by admin on Nov 30, 2023 in |
Hydrophobic medications that are taken orally having poor bioavailability due to permeability issues. They experience a chemical and enzymatic breakdown in the digestive system and exhibit a significant amount of hepatic first-pass metabolism. Similar obstacles prevent the development of effective therapeutic molecule delivery systems and the discovery of new drugs. It has been revealing that curcumin, a key active lipophilic constituent of Curcuma longa (Zingiberaceae), has a variety of pharmacological properties, including cholagogues, anticancer, and anti-inflammatory properties. Based on its organoleptic characteristics, solubility, loss on drying, partition coefficient, infrared spectroscopy, and differential scanning calorimetry, Curcumin was physically and chemically characterized. The drug sample Curcumin was found to be genuine and pure based on the tests. For the purpose of determining in-vitro release and permeation study, an analytical method utilizing RP-HPLC was created and validated. Ionic gelation was used to create chitosan nanoparticles. The study includes the evaluation of various processing conditions, including surface morphology, particle size, particle size distribution, surface charge, percentage yield, entrapment efficiency, and drug loading, as...
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Posted by admin on Nov 30, 2023 in |
Introduction: Adverse drug reactions (ADRs) poses an unforeseeable menace associated with all the prescribed medicines. Thus, ADRs are monitored and assessed on a large scale in our country by the Pharmacovigilance Programme of India through adverse drug reaction monitoring centres (AMCs). Objectives: This study was done to assess the pattern of ADRs reported in a tertiary care teaching hospital in Haryana by applying various aspects of ADR monitoring such as clinical presentation, causality, and severity assessment in various Inpatient departments at SHKM GMC. Material and Methods: A Prospective, Observational study was conducted in all the inpatient clinical departments of SHKM Govt. Medical College, Haryana for a duration of 12 months. ADRs were recorded in pre-designed proforma along with ADR reporting form “Version 1.3”. Processing & analysis of data was done using SPSS version 20. Results: A total of 189 ADRs among 120 patients were reported during the study period. Females were affected more than males. Maximum ADRs were reported in the age group of 19-60 years. ENT department had...
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