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
Wed Dec 30 2015
Journal Name
College Of Islamic Sciences
Methodology of the concept of sovereignty in contemporary Islamic thought
...Show More Authors

The methodology of the concept of sovereignty in contemporary Islamic thought

View Publication Preview PDF
Publication Date
Sun May 12 2019
Journal Name
Journal Of Planner And Development
Modern architecture in the planning of the city of Baghdad
...Show More Authors

The city of Baghdad underwent various changes and developments, which significantly influenced its urban character. And other urban fabric. The most prominent changes in the architecture of that period characterized by the emergence and spread of modern architecture, it represents the period between the 1940s and the late seventies of the twentieth century, which had its many reasons and various factors that paved and supported, and even encouraged the spread of modern architecture of the world, The advanced world in the adoption of a global architecture spread in the city of Baghdad by a number of international architects and Iraqis, who came from those countries and saturation ideas

... Show More
View Publication Preview PDF
Publication Date
Mon Apr 01 2013
Journal Name
Advances In Bioresearch
Survey of the genus Liriomyza Mik. (Diptera: Agromyzidae) of Iraq
...Show More Authors

Publication Date
Thu Dec 01 2016
Journal Name
Journal Of Economics And Administrative Sciences
The role of quality of working life in regulatory alienation
...Show More Authors

Abstract

The goal of this research is to know the quality of working life and its impact on the level of the organizational sense of alienation among a sample of teaching Anbar University in the center of Baghdad. Find and seek to achieve a number of cognitive and practical goals.

Where the quality of work life constitutes one of the main sources to enable organizations of excellence in light of the volatile environment, as is one of alienation regulatory organizations avoid the phenomena that occur because of their negative effects on performance and thus achieve their goals. The most research problem in question the existence of the main deficiencies in the application of the concepts of organiz

... Show More
View Publication Preview PDF
Crossref
Publication Date
Wed Mar 10 2021
Journal Name
Baghdad Science Journal
The Effect Of Thickness on The Optical Properties Of ZnS
...Show More Authors

Zinc sulfide(ZnS) thin films of different thickness were deposited on corning glass with the substrate kept at room temperature and high vacuum using thermal evaporation technique.the film properties investigated include their absorbance/transmittance/reflectance spectra,band gap,refractive index,extinction coefficient,complex dielectric constant and thickness.The films were found to exhibt high transmittance(59-98%) ,low absorbance and low reflectance in the visible/near infrared region up to 900 nm..However, the absorbance of the films were found to be high in the ultra violet region with peak around 360 nm.The thickness(using optical interference fringes method) of various films thichness(100,200,300,and 400) nm.The band gap meas

... Show More
View Publication Preview PDF
Crossref (1)
Crossref
Publication Date
Sun Mar 04 2018
Journal Name
Baghdad Science Journal
Biodegradation of Anthracene Compound by Two Species of Filamentous Fungi
...Show More Authors

Isolation and identification fungi of Emericella nidulans and Aspergillus flavus from a pinkish and yellowish artificial clay, by using potato dextrose agar (PDA). Results revealed that E. nidulans was the best for degrading anthracene (92.3%) with maximum biomass production (3.7gm/l), compared to A. flavus with the rate of degradation (89%) and biomass production of (1.2gm/l), when methylene blue was used as redox indicator after incubating in a shaker incubator 120rpm at 30Co for 8days. Results indicated that E. nidulans has a high ability of anthracene degradation with the rate of (84%), while A. flavus showed the lower level with (77%) by using HPLC.

View Publication Preview PDF
Scopus (3)
Scopus Clarivate Crossref
Publication Date
Mon Feb 04 2019
Journal Name
Journal Of The College Of Education For Women
Married population of Baghdad (The study of the POPULATION geography)
...Show More Authors

The study found a number of results. The most prominent were the low married during the years of the study in 1997-2012. The study also showed the level of administrative units that the percentage of widows and single rise in urban and rural decline. This is due to the different nature of urban and rural society of the behavior and social habits and traditions.As the proportion of divorced and unmarried are decreased in urban and increase proportion in the countryside, and this is due to the influence of the rural population in the urban centers. As well as the study showed that there was a significant effect of the economic and social factors and other factors on marital status on its parts in the study area.

View Publication Preview PDF
Publication Date
Sat Sep 01 2007
Journal Name
Al-khwarizmi Engineering Journal
Parametric study of thermal behavior of thrust chamber cooling channels
...Show More Authors

A numerical investigation is adopted for two dimensional thermal analysis of rocket thrust chamber wall (RL10), employing finite difference model with iterative scheme (implemented under relaxation factor of 0.9 for convergence) to compute temperature distribution within thrust chamber  wall (which is composed of Nickel and Copper layers). The analysis is conducted for different boundary conditions: only convection boundary conditions then combined radiation, convection boundary conditions also for  different aspect ratio (AR) of cooling channel. The results show that Utilizing cooling channels of high aspect ratio leads to decrease in temperature variation across thrust chamber wall, while no effects on heat transferred to the

... Show More
View Publication Preview PDF
Publication Date
Tue Dec 21 2021
Journal Name
Physical Chemistry Research
Photocatalytic and optical performances of CeO2 by substitution of titanium
...Show More Authors

In this contribution, density functional theory-based calculations have been carried out to assess the electronic, photocatalytic and optical properties of Ce1-xTixO2 system. Ti incorporation leads to a decrease of Ce 4f states and enhancement of Ti 3d states in the bottom of conduction band. Furthermore, it was found that doping ceria with Ti-like transition metals could evidently shift the absorption of pure CeO2 towards higher wavelength range. These findings can provide some new insights for designing CeO2-based photocatalysts with high photocatalytic performance. To the best of our knowledge, this investigation calculates Mullikan’s charge transfer of Ce1-xTixO2 system for the first time. Charge transfer reveals an ionic bond between

... Show More
Preview PDF
Publication Date
Thu May 18 2023
Journal Name
Journal Of Engineering
Improving Fatigue Life of Bolt Adapter of Prosthetic SACH Foot
...Show More Authors

In this research an analysis for improving the fatigue behavior (safety factor of fatigue) of non- articular prosthetic foot (SACH) in the region (Bolt Adapter).The laser peening was carried to the fatigue specimens to improving the fatigue properties of bolt’s material. The tests of mechanical properties and fatigue behavior were carried for material that the bolt manufacture from it, a region where the failure occur and inserted of these properties to the program of engineering analysis (Ansys) to calculate the safety factor of fatigue. The results showed that the safety factor after hardening by laser is increased by 42.8%.

View Publication Preview PDF
Crossref (4)
Crossref