Pharmaceutical Co-Crystals - Design, Development and Applications

2020 ◽  
Vol 10 (3) ◽  
pp. 169-184
Author(s):  
Rachna Anand ◽  
Arun Kumar ◽  
Arun Nanda
Keyword(s):  
Physicochemical Properties ◽  
Crystal Engineering ◽  
Pharmacological Action ◽  
Physicochemical Characteristics ◽  
Research Area ◽  
Dissolution Profile ◽  
Design Development ◽  
Drug Molecule ◽  
Wide Range ◽  
Major Factors

Background: Solubility and dissolution profile are the major factors which directly affect the biological activity of a drug and these factors are governed by the physicochemical properties of the drug. Crystal engineering is a newer and promising approach to improve physicochemical characteristics of a drug without any change in its pharmacological action through a selection of a wide range of easily available crystal formers. Objective: The goal of this review is to summarize the importance of crystal engineering in improving the physicochemical properties of a drug, methods of design, development, and applications of cocrystals along with future trends in research of pharmaceutical co-crystals. Co-crystallization can also be carried out for the molecules which lack ionizable functional groups, unlike salts which require ionizable groups. Conclusion: Co-crystals is an interesting and promising research area amongst pharmaceutical scientists to fine-tune the physicochemical properties of drug materials. Co-crystallization can be a tool to increase the lifecycle of an older drug molecule. Crystal engineering carries the potential of being an advantageous technique than any other approach used in the pharmaceutical industry. Crystal engineering offers a plethora of biopharmaceutical and physicochemical enhancements to a drug molecule without the need of any pharmacological change in the drug.

Structure and Activity of Pentacyclic Triterpenes Codrugs. A Review

2021 ◽  
Vol 21 ◽  
Author(s):  
Justyna Żwawiak ◽  
Anna Pawełczyk ◽  
Dorota Olender ◽  
Lucjusz Zaprutko
Keyword(s):  
Biological Activities ◽  
Anticancer Activities ◽  
Drug Molecule ◽  
Pentacyclic Triterpene ◽  
Formation Pathway ◽  
Chemical Systems ◽  
Drug Molecules ◽  
Wide Range ◽  
Anti Hiv ◽  
Structure And Activity

: Triterpenes are a wide and important group of compounds that have several promising pharmacological properties, such as hepatoprotective, anti-inflammatory, anti-HIV, antioxidant, or anticancer activities. Such potent substances can be successfully incorporated in more complex chemical systems e.g. codrugs or pro-drugs that have better pharmacological profile. The codrug is connected with a drug formation pathway to chemically cohere at least two drug molecules to improve positive therapeutic efficiency or decrease side effects. The codrug can be cleaved in the organism to generate effective compounds previously used as substrates. This article presents an overview of codrugs that consist of pentacyclic triterpene moiety that is chosen as a basic codrug moiety due to their wide range of vital activities and another drug molecule fragment. It was found that triterpenoid codrugs are characterized by a wide range of biological activities. However, most of them have anticancer potency.

scholarly journals Anti-Biofilm Molecules Targeting Functional Amyloids

Antibiotics ◽  
2021 ◽  
Vol 10 (7) ◽  
pp. 795
Author(s):  
Leticia Matilla-Cuenca ◽  
Alejandro Toledo-Arana ◽  
Jaione Valle
Keyword(s):  
Biofilm Formation ◽  
Therapeutic Strategy ◽  
Research Area ◽  
Therapeutic Strategies ◽  
Structural Components ◽  
Significant Issue ◽  
Wide Range ◽  
Effective Therapeutic Strategy ◽  
Functional Amyloids ◽  
Biofilm Matrix

The choice of an effective therapeutic strategy in the treatment of biofilm-related infections is a significant issue. Amyloids, which have been historically related to human diseases, are now considered to be prevailing structural components of the biofilm matrix in a wide range of bacteria. This assumption creates the potential for an exciting research area, in which functional amyloids are considered to be attractive targets for drug development to dissemble biofilm structures. The present review describes the best-characterized bacterial functional amyloids and focuses on anti-biofilm agents that target intrinsic and facultative amyloids. This study provides a better understanding of the different modes of actions of the anti-amyloid molecules to inhibit biofilm formation. This information can be further exploited to improve the therapeutic strategies to combat biofilm-related infections.

scholarly journals An Overview on the Rheology, Mechanical Properties, Durability, 3D Printing, and Microstructural Performance of Nanomaterials in Cementitious Composites

Materials ◽  
2021 ◽  
Vol 14 (11) ◽  
pp. 2950
Author(s):  
Hongwei Song ◽  
Xinle Li
Keyword(s):  
Mechanical Properties ◽  
3D Printing ◽  
Three Dimensional ◽  
Cementitious Materials ◽  
Research Area ◽  
Cementitious Composites ◽  
Split Tensile Strength ◽  
Contour Crafting ◽  
Wide Range ◽  
Active Research

The most active research area is nanotechnology in cementitious composites, which has a wide range of applications and has achieved popularity over the last three decades. Nanoparticles (NPs) have emerged as possible materials to be used in the field of civil engineering. Previous research has concentrated on evaluating the effect of different NPs in cementitious materials to alter material characteristics. In order to provide a broad understanding of how nanomaterials (NMs) can be used, this paper critically evaluates previous research on the influence of rheology, mechanical properties, durability, 3D printing, and microstructural performance on cementitious materials. The flow properties of fresh cementitious composites can be measured using rheology and slump. Mechanical properties such as compressive, flexural, and split tensile strength reveal hardened properties. The necessary tests for determining a NM’s durability in concrete are shrinkage, pore structure and porosity, and permeability. The advent of modern 3D printing technologies is suitable for structural printing, such as contour crafting and binder jetting. Three-dimensional (3D) printing has opened up new avenues for the building and construction industry to become more digital. Regardless of the material science, a range of problems must be tackled, including developing smart cementitious composites suitable for 3D structural printing. According to the scanning electron microscopy results, the addition of NMs to cementitious materials results in a denser and improved microstructure with more hydration products. This paper provides valuable information and details about the rheology, mechanical properties, durability, 3D printing, and microstructural performance of cementitious materials with NMs and encourages further research.

Design, Development and Application of Vehicle Gas Turbine Engines

1966 ◽  
Vol 181 (1) ◽  
pp. 149-172
Author(s):  
P. A. Phillips ◽  
Peter Spear
Keyword(s):  
Gas Turbine ◽  
Gas Turbines ◽  
Low Cost ◽  
Engine Performance ◽  
Turbine Engines ◽  
Gas Turbine Engines ◽  
Design Development ◽  
Turbine Engine ◽  
Wide Range ◽  
Cycle Temperature

After briefly summarizing worldwide automotive gas turbine activity, the paper analyses the power plant requirements of a wide range of vehicle applications in order to formulate the design criteria for acceptable vehicle gas turbines. Ample data are available on the thermodynamic merits of various gas turbine cycles; however, the low cost of its piston engine competitor tends to eliminate all but the simplest cycles from vehicle gas turbine considerations. In order to improve the part load fuel economy, some complexity is inevitable, but this is limited to the addition of a glass ceramic regenerator in the 150 b.h.p. engine which is described in some detail. The alternative further complications necessary to achieve satisfactory vehicle response at various power/weight ratios are examined. Further improvement in engine performance will come by increasing the maximum cycle temperature. This can be achieved at lower cost by the extension of the use of ceramics. The paper is intended to stimulate the design application of the gas turbine engine.

scholarly journals Non-invasive sensing for food reassurance

The Analyst ◽  
2016 ◽  
Vol 141 (5) ◽  
pp. 1587-1610 ◽  
Author(s):  
Zou Xiaobo ◽  
Huang Xiaowei ◽  
Malcolm Povey
Keyword(s):  
Chemical Composition ◽  
Physicochemical Properties ◽  
Food Quality ◽  
Physical Principle ◽  
Quality Traits ◽  
X Ray ◽  
Main Food ◽  
Non Invasive ◽  
Wide Range ◽  
Nutritional Characteristics

The main food quality traits of interest using non-invasive sensing techniques are sensory characteristics, chemical composition, physicochemical properties, health-protecting properties, nutritional characteristics and safety. A wide range of non-invasive sensing techniques, from optical, acoustical, electrical, to nuclear magnetic, X-ray, biosensor, microwave and terahertz, are organized according to physical principle.

scholarly journals Blocking of Bacterial Biofilm Formation by a Fish Protein Coating

2008 ◽  
Vol 74 (11) ◽  
pp. 3551-3558 ◽  
Author(s):  
Rebecca Munk Vejborg ◽  
Per Klemm
Keyword(s):  
Biofilm Formation ◽  
Fish Muscle ◽  
Physicochemical Characteristics ◽  
Economic Problem ◽  
Bacterial Attachment ◽  
Bacterial Biofilm ◽  
Adhesive Properties ◽  
Muscle Extract ◽  
Wide Range ◽  
Inert Surfaces

ABSTRACT Bacterial biofilm formation on inert surfaces is a significant health and economic problem in a wide range of environmental, industrial, and medical areas. Bacterial adhesion is generally a prerequisite for this colonization process and, thus, represents an attractive target for the development of biofilm-preventive measures. We have previously found that the preconditioning of several different inert materials with an aqueous fish muscle extract, composed primarily of fish muscle α-tropomyosin, significantly discourages bacterial attachment and adhesion to these surfaces. Here, this proteinaceous coating is characterized with regards to its biofilm-reducing properties by using a range of urinary tract infectious isolates with various pathogenic and adhesive properties. The antiadhesive coating significantly reduced or delayed biofilm formation by all these isolates under every condition examined. The biofilm-reducing activity did, however, vary depending on the substratum physicochemical characteristics and the environmental conditions studied. These data illustrate the importance of protein conditioning layers with respect to bacterial biofilm formation and suggest that antiadhesive proteins may offer an attractive measure for reducing or delaying biofilm-associated infections.

China’s shadow banking sector: beneficial or harmful to economic growth?

2015 ◽  
Vol 7 (4) ◽  
pp. 421-445 ◽  
Author(s):  
James R. Barth ◽  
Tong Li ◽  
Wen Shi ◽  
Pei Xu
Keyword(s):  
Economic Growth ◽  
Banking Sector ◽  
Commercial Banking ◽  
Global Perspective ◽  
Shadow Banking ◽  
Content Type ◽  
Wide Range ◽  
Recent Developments ◽  
Major Factors ◽  
Made In

Purpose – The purpose of this paper is to examine recent developments pertaining to China’s shadow banking sector. Shadow banking has the potential not only to be a beneficial contributor to continued economic growth, but also to contribute to systematic instability if not properly monitored and regulated. An assessment is made in this paper as to whether shadow banking is beneficial or harmful to China’s economic growth. Design/methodology/approach – The authors start with providing an overview of shadow banking from a global perspective, with information on its recent growth and importance in selected countries. The authors then focus directly on China’s shadow banking sector, with information on the various entities and activities that comprise the sector. Specifically, the authors examine the interconnections between shadow banking and regular banking in China and the growth in shadow banking to overall economic growth, the growth in the money supply and the growth in commercial bank assets. Findings – Despite the wide range in the estimates, the trend in the size of shadow banking in China has been upward over the examined period. There are significant interconnections between the shadow banking sector and the commercial banking sector. Low deposit rate and high reserve requirement ratios have been the major factors driving its growth. Shadow banking has been a contributor, along with money growth, to economic growth. Practical implications – The authors argue that shadow banking may prove useful by diversifying China’s financial sector and providing greater investments and savings opportunities to consumers and businesses throughout the country, if the risks of shadow banking are adequately monitored and controlled. Originality/value – To the authors’ knowledge, this paper is among the few to systematically evaluate the influence of shadow banking on China’s economic growth.

ANTIMICROBIAL AND POWDER CHARACTERIZATION OF HERBAL DENTIFRICES

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (11) ◽  
pp. 39-47
Author(s):  
V. K Sharma ◽  
◽  
B. Mazumder ◽  
P. P. Sharma
Keyword(s):  
Oral Cavity ◽  
Physicochemical Properties ◽  
Antimicrobial Effect ◽  
Physicochemical Characteristics ◽  
Water Soluble ◽  
Particle Rearrangement ◽  
Bulk Volume ◽  
The Impact ◽  
Tapped Density

The consumption of edible products strongly recommends the regular hygiene of oral cavity. Various dental products of allopathic and herbal origin are used as dentifrices. The dentifrices are considered safe and effective in terms of cleansing effect of oral cavity and antimicrobial effect against microbes causing bad smell and diseases such as gingivitis, pyorrhea etc. These characteristics of preparations are basically related to physicochemical properties of ingredients present in their composition and some how on directions of their use. In the present study, the marketed allopathic dentifrices coded as Brand I and II and herbal tooth powders coded as Brand III and IV were selected to analyze the impact of physicochemical properties of incorporated ingredients on their cleansing efficiency. The physicochemical characteristics studied were pH, bulk volume, tapped volume, tapped density, bulk density, true density, porosity, flowability, compressibility, compactability, cohesiveness, dispersability, Carr’s index, Hausner’s ratio, water soluble content, alcohol soluble content, foaming index, particle rearrangement behaviour and particle rearrangement constant. The antimicrobial effect of these powders was studied against Staphylococcus sorbinus, Staphylococcus salivarius and Lactobacillus acidophilus. It was observed that some of the physicochemical properties of all powders were different from each other. Marked antimicrobial effect of tooth powders was observed against pathogens. In all preparations, remarkable foaming index was analyzed that was generally considered responsible for cleansing effect.

Chemical modification and Physicochemical properties of new derivatives 5-(thiophen-3-ilmethyl)-4-R1-1,2,4-triazole-3-thiol

2021 ◽  
pp. 4621-4629
Author(s):  
O.A. Bihdan ◽  
V.V. Parchenko
Keyword(s):  
Physicochemical Properties ◽  
High Reactivity ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Active Compounds ◽  
Triazole Derivatives ◽  
Pharmaceutical Ingredients ◽  
Current Trends ◽  
Wide Range ◽  
Derivatives Of

Current trends in the search for new biologically active compounds among synthetic molecules have arguably proved a priority in studies of the heterocyclic 1,2,4-triazole system. For many years, 1,2,4-triazole derivatives remain the object of close attention of scientists of various scientific fields. The unique properties of 1,2,4-triazole derivatives include high reactivity, which allows different modification of this system, practical absence of toxicity of these derivatives and the presence of a wide range of biological, pharmacological properties, which in the complex provides the prerequisites for the creation of new biologically active compounds, and in the future, active pharmaceutical ingredients (AFI). The aim of our work is to investigate some transformations in a number of derivatives of 5-(thiophen-3-ylmethyl) -4-R1-1,2,4-triazole-3-thiol, to study the physicochemical properties of the new synthesized compounds. A well-known fact remains the successful attempt of many scientists involved in the study of the heterocyclic 1,2,4-triazole system to synthesize potential biologically active compounds. The process of creating new molecules is very painstaking and requires considerable effort. The chemical approaches for the synthesis of the starting compounds required for further transformations are well known and described. Therefore, we used the corresponding N-R1-2 as intermediates for the synthesis of new 5-(thiophen-3-ylmethyl) -4-R1-1,2,4-triazole-3-thiols appropriate ones were used N-R1-2-(2-(thiophen-3-yl) acetyl) hydrazinocarbothioamide.

The Design, Development and Validation of an Innovative High Strength, Self Monitoring, Composite Pipe Liner for the Restoration of Energy Transmission Pipelines

2006 ◽  
Author(s):  
Kyle Bethel ◽  
Steven C. Catha ◽  
Melvin F. Kanninen ◽  
Randall B. Stonesifer ◽  
Ken Charbonneau ◽  
...  
Keyword(s):  
High Pressures ◽  
Large Diameter ◽  
Cylindrical Tube ◽  
High Strength ◽  
Design Development ◽  
Energy Transmission ◽  
Engineering Research ◽  
Wide Range ◽  
Transmission Pipelines

The research described in this paper centers on a composite of thermoplastic materials that can be inserted in a degraded steel pipe to completely restore its strength. Through the use of fabrics consisting of ultra high strength fibers that are co-helically wrapped over a thin walled thermoplastic cylindrical tube that serves as a core, arbitrarily high pressures can be achieved. This paper first outlines the design, manufacturing and installation procedures developed for this unique material to provide a context for the engineering research. Based on this outline, the technological basis that has been developed for assuring the strength and long term durability of this concept during its insertion, and in its very long term service as a liner in energy transmission pipelines, is presented in detail. The research that is described includes burst testing of the material in stand alone pipe form, load/elongation testing of ultra high strength fabrics, and linear and nonlinear elastic and viscoelastic analysis models. This body of work indicates that the concept is fundamentally feasible for restoring a wide range of large diameter natural gas and liquid transmission pipelines to be able to carry arbitrarily high pressures over very long lifetimes. It also indicates that liners can be safely installed in long lengths even in lines with severe bends in a continuous manner. With further research the concept has the potential for eliminating hydro testing and smart pigging during service, and could possibly be installed in some lines that are currently unpiggable.

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