Preferred Language
Articles
/
bijps-706
Investigation of Solubility Enhancement Approaches of Ticagrelor
...Show More Authors

ABSTRACT

                   Ticagrelor is an orally administered antiplatelet medicine, direct-acting P2Y12-receptor antagonist. Ticagrelor binds reversibly and noncompetitively to the P2Y12 receptor at a site distinct from that of the endogenous agonist adenosine diphosphate (ADP). Inhibition of platelet aggregation stimulated by ADP is a commonly used pharmacodynamic parameter for P2Y12-receptor antagonists.

                  Ticagrelor is a crystalline powder with an aqueous solubility of approximately 10?g/mL at room temperature. Ticagrelor exhibits no pKa value within the physiological range. Ticagrelor does not exhibit pH-dependent solubility and is defined as ‘low solubility low permeability’ under the Biopharmaceutics Classification System (Class IV). The mean absolute bioavailability of ticagrelor in healthy volunteers is 36 %

                   Nanoparticles preparation and complexation is one of the recently used approaches to enhance the solubility of drugs. The aim of the present work was to improve the solubility and dissolution of ticagrelor by preparing nanoparticles and cyclodextrin inclusion complex of ticagrelor and then incorporated in to tablet dosage form. Fifteen formulas of nanoparticles were prepared by antisolvent precipitation method (solvent displacement method) utilizing one of the three polymers (PVP, Poloxamer, and HPMC) at three different drugs: polymer and solvent: anti-solvent ratios and nine formulas of cyclodextrin inclusion complex with HP?CD  by three preparation methods, physical trituration, kneading and solvent evaporation, which increase the solubility and dissolution rate of ticagrelor via formation of inclusion complex with HP?CD.

              The prepared formulas were characterized regarding the saturated solubility, polydispersity index, particle size by nano laser particle size analyzer, % yield, entrapment efficiency, and flowability, FTIR, DSC, and SEM. The selected formulas were prepared as tablets.

             The prepared tablets were evaluated for drug content, weight variation, hardness, and friability. In vitro dissolution data of the prepared tablets were analyzed using similarity factor (f2) and dissolution efficiency (DE).  

           Among all the prepared nanoparticles formulas, formula (F12) which contain HPMC as a polymer at polymer: drug ratio of (1:1) and solvent: antisolvent ratio of (1:1) was considered as the optimum formula which shows good evaluation parameters in addition to the increment in the solubility to about 9 times than that of the pure drug. The nanoparticle of the selected formula (F12) incorporated tablets showed an acceptable tablet properties in addition to a considerable increase in the dissolution efficiency to (DE=92 % and 88 % in PH 1.2 and PH 6.8 respectively) in comparison to that of the marketed tablet (DE=89% and 85% in PH 1.2 and PH 6.8 respectively).  Moreover, the analysis by DSC and SEM of the nanoparticles of the selected formula (F12) indicate a reduction in the crystallinity and amorphization of the drug. It can be concluded that the selected formula is a promising formula for the preparation of ticagrelor nanoparticles the incorporation in a tablet dosage form.

          Regarding ticagrelor inclusion complex with HP?CD Solvent evaporation method was the most effective method regarding ticagrelor solubilization and optimum formula of inclusion complex (F23) show increment in saturated solubility about ten times that of pure drug.

          The ticagrelor inclusion complex of the selected formula (F23) incorporated tablets showed an acceptable tablet properties in addition to a considerable increase in the dissolution efficiency to (DE=92 % and 90 % in PH 1.2 and PH 6.8 respectively) in comparison to that of the marketed tablet (DE=89% and 85% in PH 1.2 and PH 6.8 respectively).  

 

Scopus Crossref
View Publication Preview PDF
Quick Preview PDF
Publication Date
Mon Feb 01 2021
Journal Name
Neuroquantology
Study and Investigation of Hard Photons Emission in Heavy Ion Collisions
...Show More Authors

This work involves hard photon rate production from quark -gluon plasma QGP interaction in heavy ion collision. Using a quantum chromodynamic model to investigate and calculation of photons rate in 𝑐𝑔 → 𝑠𝑔𝛾 system due to strength coupling, photons rate, temperature of system, flavor number and critical. The photons rate production computed using the perturbative strength models for QGP interactions. The strength coupling was function of temperature of system, flavor number and critical temperature. Its influenced by force with temperature of system, its increased with decreased the temperature and vice versa. The strength coupling has used to examine the confinement and deconfinement of quarks in QGP properties and inf

... Show More
Scopus (2)
Scopus
Publication Date
Fri Jun 01 2007
Journal Name
Al-khwarizmi Engineering Journal
Investigation of heat transfer phenomena and flow behavior around electronic chip
...Show More Authors

Computational study of three-dimensional laminar and turbulent flows around electronic chip (heat source) located on a printed circuit board are presented. Computational field involves the solution of elliptic partial differential equations for conservation of mass, momentum, energy, turbulent energy, and its dissipation rate in finite volume form. The k-ε turbulent model was used with the wall function concept near the walls to treat of turbulence effects. The SIMPLE algorithm was selected in this work. The chip is cooled by an external flow of air. The goals of this investigation are to investigate the heat transfer phenomena of electronic chip located in enclosure and how we arrive to optimum level for cooling of this chip. These par

... Show More
View Publication Preview PDF
Publication Date
Thu May 18 2023
Journal Name
Journal Of Engineering
Experimental and Theoretical Investigation of Noise Effect in Centrifugal Fan Impeller
...Show More Authors

In this work a study was made in centrifugal fan blower to investigate the effect of impeller blade design on sound pressure level (SPL). Shroud and unshroud impeller of nine blades are used. The sound generation from flow inside the test rig at different positions was displayed by using spectral analyzer. The experiments were carried out in anechoic chamber with small holes in its walls, under ambient condition about (25-27) C ° to avoid the effect of temperature on the sound pressure level. The results showed that (SPL) decreased with the increase of distance from the source about (3-4)dB when distance varied about (0.8-1.06)m, and the (SPL) decreased with the decrease of velocity about (8-12)dB when velocity varied between (13000-260

... Show More
View Publication Preview PDF
Crossref
Publication Date
Thu Feb 15 2018
Journal Name
Ijca
Experimental Investigation and Performance Simulation of Kit Horizontal Axis Wind Turbine
...Show More Authors

Crossref
Publication Date
Sat Oct 28 2023
Journal Name
Baghdad Science Journal
Quantum Theory of Atom in Molecules Investigation Trinuclear Ruthenium: DFT Approach
...Show More Authors

The topological indices of the "[(µ3-2, 5-dioxyocyclohexylidene)-bis ((2-hydrido)-nonacarbonyltriruthenium]” were studied within the quantum theory of atoms in the molecule (QTAIM), clusters are
analyzed using the density functional theory (DFT). The estimated topological variables accord with prior
descriptions of comparable transition metal complexes. The Quantum Theory of Atom, in molecules
investigation of the bridging core component, Ru3H2, revealed critical binding points (chemical bonding)
between Ru (1) and Ru (2) and Ru (3). Consequently, delocalization index for this non-bonding interaction
was calculated in the core of Ru3H2, the interaction is of the (5centre–5electron) class.

View Publication Preview PDF
Scopus Crossref
Publication Date
Tue Dec 29 2020
Journal Name
Journal Of Mechanics Of Continua And Mathematical Sciences
NUMERICAL INVESTIGATION OF DEVELOPING LAMINAR FLUID FLOW THROUGH RECTANGULAR ANNULUS DUCT
...Show More Authors

The laminar fluid flow of water through the annulus duct was investigated numerically by ANSYS fluent version 15.0 with height (2.5, 5, 7.5) cm and constant length (L=60cm). With constant heat flux applied to the outer duct. The heat flux at the range (500,1000,1500,2000) w/m2 and Reynolds number values were ≤ 2300. The problem was 2-D investigated. Results revealed that Nusselt number decrease and the wall temperature increase with the increase of heat flux. Also, the average Nusselt number increase as Re increases. And as the height of the annulus increase, the values of the temperature and the local and average Nusselt number increase.

View Publication
Crossref
Publication Date
Thu Mar 30 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
An Investigation Release and Rheological Properties of Miconazole Nitrate from Emulgel
...Show More Authors

         In this study miconazole nitrate was formulated as topically applied emulgel; different formulas were prepared using sodium carboxymethylcellulose (SCMC) and carboxypolymethylene (carbomer 941) as gelling agents. The influence of type of gelling agent and concentration of both oil phase and emulsifying agent on drug release was studied and compared with commercially available miconazole nitrate cream (Mecozalen®). The results of in vitro release showed that SCMC emulgel bases gave better release than carbomer 941 bases and the release of drug increase from both bases as a function of increasing the concentration of emulisifying agent. The oil phase had retardation effect when

... Show More
View Publication Preview PDF
Crossref (6)
Crossref
Publication Date
Wed Jun 15 2022
Journal Name
Malaysian Journal Of Science
INVESTIGATION OF FAST NEURON ATTENUATION COEFFICIENTS FOR SOME IRAQI BUILDING MATERIALS
...Show More Authors

This research aims to improve the radiation shielding properties of polymer-based materials by mixing PVC with locally available building materials. Specifically, two key parameters of fast neutron attenuation (removal cross-section and half-value layer) were studied for composite materials comprising PVC reinforced with common building materials (cement, sand, gypsum and marble) in different proportions (10%, 30% and 50% by weight). To assess their effectiveness as protection against fast neutrons, the macroscopic neutron cross-section was calculated for each composite. Results show that neutron cross-section values are significantly affected by the reinforcement ratios, and that the composite material PVC + 50% gypsum is an effect

... Show More
View Publication
Scopus (3)
Crossref (1)
Scopus Crossref
Publication Date
Sat Jul 22 2023
Journal Name
Journal Of Engineering
Investigation Parameters of Resistance Spot Welding For AA1050 Aluminum Alloy Sheets
...Show More Authors

The parameters of resistance spot welding (RSW) performed on low strength commercial aluminum sheets are investigated experimentally, the performance requirements and weldability issues were driven the choice of a specific aluminum alloy that was AA1050. RSW aluminum alloys has a major problem of inconsistent quality from weld to weld comparing with welding steel
alloys sheet, due to the higher thermal conductivity, higher thermal expansion, narrow plastic temperature range, and lower electrical resistivity. Much effort has been devoted to the study of describing the relation between the parameters of the process (welding current, welding time, and electrode force) and weld strength. Shear-tensile strength tests were performed to ind

... Show More
View Publication Preview PDF
Crossref (1)
Crossref
Publication Date
Fri Oct 16 2020
Journal Name
Solid State Technology
Study and Investigation of Transition Rate at Metal–Organic Semiconductor Interfaces
...Show More Authors

In this paper,we focus on the investigated and studied of transition rate in metal/organic semiconductor interface due to quantum postulate and continuum transition theory. A theoretical  model has been used to estimate  the transition rate cross the interface through estimation many parameters such that ;transition energy  ,driving electronic energy U(eV) ,Potential barrier ,electronic coupling  ,semiconductor volume ,density ,metal work function ,electronic affinity and temperature T. The transition energy  is critical facter of charge transfer through the interfaces of metal organic films device and itscontrol of charge injection and transport cross interface. However,the potential at interfa

... Show More
View Publication Preview PDF