In order to explore the mechanism of action of meloxicam and α-amylase. The interaction between the rheumatoid arthritis drug meloxicam and α-amylase was studied by fluorescence spectroscopy, synchronous fluorescence spectroscopy and molecular docking under the experimental conditions of pH=6.80. The results showed that meloxicam was able to effectively quench the endogenous fluorescence of α-amylase in a static quenching form a 1:1 complex and change the conformation of α-amylase. Thermodynamic results indicated that the main type of meloxicam and α-amylase system was hydrophobic interaction. Molecular docking indicated that the binding system had hydrogen bonds in addition to hydrophobic interaction and meloxicam was surrounded by the active amino acid residues Trp13 and Trp263 of α-amylase, which changed the microenvironment of amino acid residues at the active center of α-amylase. By establishing the binding model, it can be seen that the protein binding rate W(B) of meloxicam to α-amylase was 2.76%-41.79% under the experimental conditions. The results showed that the binding of meloxicam to α-amylase had an effect on the number of free α-amylase. The drug binding rate W(Q) of the system was 2.76%-1.67%, which indicated that the combination of α-amylase and meloxicam would not affect the efficacy of meloxicam.
The binding pursuits of trans-resveratrol (t-RSV), an amazing health supplement are investigated with an antioxidant enzyme, superoxide dismutase (SOD1). The aim of the study is to dock t-RSV on the adrenaline binding site on SOD1 in order to explore its potential to act as a safety net against amyotrophic lateral sclerosis (ALS), a fatal neurodegenerative disorder that affects motor neurons. In silico GLIDE docking methodology and in vitro microcalorimetry technique is utilized for the investigation of binding parameters of t-RSV with SOD1. The study provides useful and distinct information about the amino acids involved in the interactions at molecular level along with the nature of forces involved in binding of t-RSV with SOD1. The docking analysis using the scoring functions of Schrodinger's Glide package depicts that GLU100, PRO28, LYS23, TRP32 residues of the peptide backbone on SOD 1 interact with phenolic groups of t-RSV. The information on thermodynamic parameters, i.e. binding constant (Kb), free energy (ΔG) and enthalpy (ΔH) generated through calorimetric titrations suggests that the reaction between t-RSV and SOD 1 is spontaneous and exothermic. Both the studies are found to be in close agreement with each other based as far as the magnitude of binding constant (Kb =9.9 x10 4) is concerned.
In the present work an attempt has been made to design the antibiotic drug loaded carbopol-poly(NVP) based hydrogel wound dressings for better wound care. The polymer films were characterized by SEM-EDX, AFM, FTIR, 13CNMR, TGA/DTA/DTG, DSC, and swelling studies. Besides drug release, various biomedical properties (viz. blood compatibility, mucoadhesion, oxygen permeability, water vapour transmission rate, microbial penetration, tensile strength, bursting strength, resilience, stress relaxation, and folding endurance) have also been studied. The polymer films have been observed to be biocompatible, permeable to oxygen and water vapour and have absorbed simulated wound fluid 11.37±0.31 g/g of polymer film.The drug release profile followed the Case-II diffusion mechanism and release profile best fitted in Hixson-Crowell's kinetic models.Mechanical properties results showed that the polymer film had 0.65±0.12 Nmm-2 tensile strength, 119.38±14.26% elongationand 25.49±0.72% resilience.
Garcinia Glycosides is a candidate drug obtained by structural modification of Gambogic Acid (GA), which was acquired through High Throughput Screening(HTS). As Garcinia Glycosides is an effective but insoluble anti-tumor drug, the aim of this study was to obtain a solid dispersion form Garcinia Glycosides by using solvent-melt method so that improve the solubility and dissolution rate. The solid dispersion was characterized by High Performance Liquid Chromatography (HPLC), infrared spectroscopy and evaluated the intestinal absorption of the drug by rat in situ single pass intestinal perfusion. The results showed the increase of solubility, dissolution velocity and absorption compared to other forms. This indicated that solid dispersion could greatly improve the relative bioavailability of Garcinia Glycosides in vivo.
The SeDeM Expert System was first known as a galenic pre-formulation system, which was based on the experimental research and quantitative determination of powdered substances. And the mathematical formula provided by the SeDeM Expert System has plays an important role in the study of powder properties. The system can be used not only to evaluate the powder direct compression (DC) of excipients and active pharmaceutical ingredients (API's), but also to predict the possible formulations, so it can reduce unnecessary research and trials, and shorten the time of development. In this paper, the research development and application of SeDeM Expert System in DC was summarized, and the results showed that with a few exceptions, the system was skilled in predicting acceptable tablet formulations. Finally, the new application prospect of the system is presented, including the application of the Internet traffic and content management (iTCM) database and the new co-processed excipients.
Pharmacy is an interdisciplinary field of science, which covers the knowledge of fate of drugs (pharmacons), excipients and formulated pharmaceutical products outside and inside the body. Separation of pharmacy as a separate entity of medicine is dated back to the ninth century. The trend toward specialization was later reinforced by a law enacted by the German Emperor Frederic II at the beginning of the thirteenth century. Since these early times pharmacy underwent a continuous and intense development. Pharmaceutics, Pharmaceutical chemistry, Pharmacognosy, Pharmacology and Toxicology are the conventional fields of pharmacy, which serve as the source of practical and theoretical basis of development of new pharmaceutical products......