scholarly journals Impact of Crystal Habit on Solubility of Ticagrelor

Crystals ◽  
2019 ◽  
Vol 9 (11) ◽  
pp. 556 ◽  
Author(s):  
Ren ◽  
Shen ◽  
Yu ◽  
Phan ◽  
Chen ◽  
...  

Drugs with poor biopharmaceutical performance are the main obstacle to the development and design of medicinal preparations. The anisotropic surface chemistry of different surfaces on the crystal influences its physical and chemical properties, such as solubility, tableting, etc. In this study, the antisolvent crystallization and rapid-cooling crystallization were carried out to tune the crystal habits of ticagrelor (TICA) form II. Different crystal habits of ticagrelor (TICA) form II (TICA-A, TICA-B, TICA-C, TICA-D, and TICA-E) were prepared and evaluated for solubility. The single-crystal diffraction (SXRD) indicated that TICA form II belongs to the triclinic P1 space group with four TICA molecules in the asymmetric unit. The TICA molecules are generated through intermolecular hydrogen bonds along the (010) direction, forming an infinite molecular chain, which are further stacked by hydrogen bonds between hydroxyethoxy side chains, forming molecular circles composed of six TICA molecules along bc directions. Thus, in the case of TICA form II, hydrogen bonds drive growth along one axis (b-axis), which results in the formation of mostly needle-shape crystals. Morphology and face indexation reveals that (001), (010) and (01-1) are the main crystal planes. Powder diffractions showed that five habits have the same crystal structure and different relative intensity of diffraction peak. The solubility of the obtained crystals showed the crystal habits affect their solubility. This work is helpful for studying the mechanism of crystal habit modification and its effect on solubility.

1983 ◽  
Vol 38 (6) ◽  
pp. 738-746 ◽  
Author(s):  
Reinhold Tacke ◽  
Hartwig Lange ◽  
William S. Sheldrick ◽  
Günter Lambrecht ◽  
Ulrich Moser ◽  
...  

Abstract In the course of systematic investigations on sila-substituted parasympatholytics the diphenyl(2-aminoethoxymethyl)silanols 3b and 4b (and its carbon analogue 4a) were synthesized and characterized by their physical and chemical properties. In the solid state 4a and 4b form strong O-H---N hydrogen bonds, which are intramolecular (4a) and intermolecular (4b), respectively. 4a and 4b were found to be weak antimuscarinic agents (4b >4a) and strong papaverine-like spasmolytics (4a ≈4b).


Author(s):  
M. I. McMahon

Extreme conditions (EC) research investigates how the structures and physical and chemical properties of materials change when subjected to extremes of pressure and temperature. Pressures in excess of one million times atmospheric pressure can be achieved using a diamond anvil cell, and, in combination with high-energy, micro-focused radiation from a third-generation synchrotron such as Diamond, detailed structural information can be obtained using either powder or single-crystal diffraction techniques. Here, I summarize some of the research drivers behind international EC research, and then briefly describe the techniques by which high-quality diffraction data are obtained. I then highlight the breadth of EC research possible on Diamond by summarizing four examples from work conducted on the I15 and I19 beamlines, including a study which resulted in the first research paper from Diamond. Finally, I look to the future, and speculate as to the type of EC research might be conducted at Diamond over the next 10 years.


1966 ◽  
Vol 24 ◽  
pp. 101-110
Author(s):  
W. Iwanowska

In connection with the spectrophotometric study of population-type characteristics of various kinds of stars, a statistical analysis of kinematical and distribution parameters of the same stars is performed at the Toruń Observatory. This has a twofold purpose: first, to provide a practical guide in selecting stars for observing programmes, second, to contribute to the understanding of relations existing between the physical and chemical properties of stars and their kinematics and distribution in the Galaxy.


Author(s):  
Mehmet Sarikaya ◽  
Ilhan A. Aksay

Biomimetics involves investigation of structure, function, and methods of synthesis of biological composite materials. The goal is to apply this information to the design and synthesis of materials for engineering applications.Properties of engineering materials are structure sensitive through the whole spectrum of dimensions from nanometer to macro scale. The goal in designing and processing of technological materials, therefore, is to control microstructural evolution at each of these dimensions so as to achieve predictable physical and chemical properties. Control at each successive level of dimension, however, is a major challenge as is the retention of integrity between successive levels. Engineering materials are rarely fabricated to achieve more than a few of the desired properties and the synthesis techniques usually involve high temperature or low pressure conditions that are energy inefficient and environmentally damaging.In contrast to human-made materials, organisms synthesize composites whose intricate structures are more controlled at each scale and hierarchical order.


2017 ◽  
pp. 31-43
Author(s):  
Berta Ratilla ◽  
Loreme Cagande ◽  
Othello Capuno

Organic farming is one of the management strategies that improve productivity of marginal uplands. The study aimed to: (1) evaluate effects of various organic-based fertilizers on the growth and yield of corn; (2) determine the appropriate combination for optimum yield; and (3) assess changes on the soil physical and chemical properties. Experiment was laid out in Randomized Complete Block Design, with 3 replications and 7 treatments, namely; T0=(0-0-0); T1=1t ha-1 Evans + 45-30-30kg N, P2O5, K2O ha-1; T2=t ha-1 Wellgrow + 45-30-30kg N, P2O5, K2O ha-1; T3=15t ha-1 chicken dung; T4=10t ha-1 chicken dung + 45-30-30kg N, P2O5, K2O ha-1; T5=15t ha-1 Vermicast; and T6=10t ha-1 Vermicast + 45-30-30kg N, P2O5, K2O ha-1. Application of organic-based fertilizers with or without inorganic fertilizers promoted growth of corn than the control. But due to high infestation of corn silk beetle(Monolepta bifasciata Horns), its grain yield was greatly affected. In the second cropping, except for Evans, any of these fertilizers applied alone or combined with 45-30-30kg N, P2O5, K2O ha-1 appeared appropriate in increasing corn earyield. Soil physical and chemical properties changed with addition of organic fertilizers. While bulk density decreased irrespective of treatments, pH, total N, available P and exchangeable K generally increased more with chicken dung application.


Author(s):  
O.S. Bezuglova ◽  

Rostov Region belongs to the highly protected natural territories characterized by the continuous plowing. There territories are the only reserves with the soils preserved in their natural state. However, these areas often lack detailed information about the soils quality and composition. Surveying soils on these territories is crucial for determination of their basic physical and chemical properties. The resulted compilation of soil maps could lay a foundation for creating the Red Book of Soils and the formation of a section in the soil-geographical database of the Russian Federation. Subsequently, such information can be used as a background data for the main types of soils in the region. It will be also valuable during monitoring and justification of conservation measures.


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