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
Thu Sep 01 2016
Journal Name
2016 8th Computer Science And Electronic Engineering (ceec)
Utilisation of multipath phenomenon to improve the performance of BCH and RS codes
...Show More Authors

View Publication
Scopus (7)
Crossref (4)
Scopus Crossref
Publication Date
Sun Sep 30 2001
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Effect of Velocity and Temperature on Mass Transfer of Oxygen in Corrosion Processes
...Show More Authors

View Publication Preview PDF
Publication Date
Mon Mar 27 2023
Journal Name
8th Engineering And 2nd International Conference For College Of Engineering – University Of Baghdad: Coec8-2021 Proceedings
Evaluation of the capability of Shatt Al-Arab River to control flood discharge
...Show More Authors

Abstract. Shatt Al-Arab River was the most important tide river in Iraq, it suffered from neglect and lack of maintenance in the past decades. The river embankment is constantly exposed to erosion processes due to several factors, one of the most important of these factors is the movement of water currents due to the tidal energy coming from the Arabian Gulf. In this study, one dimension unsteady-state model was implemented to study river flood capacity simulation by using HEC-RAS (5.0.7) software in Shatt Al Arab River and its tributaries. The data included flow rate, water level records were collected daily from 2018 to 2020 at different stations along the mentioned river and its feeders, additionally, the considered flood discharge data

... Show More
View Publication Preview PDF
Crossref (1)
Crossref
Publication Date
Sun Dec 10 2017
Journal Name
Al-academy
cognitive references of the directorial imagination and modeling of the theatrical actor performance
...Show More Authors

This research is determined by the study of  the " cognitive references of the directorial imagination and modeling of  the theatrical actor performance ." it has described an Iraqi theatrical model, The research began with the great importance of the director's imagination as the basic premise for crystallizing the  director's vision according to its cognitive references in creating a solid performance model based on the aesthetic, intellectual and technical bases, It is also contributes to the formation of the theatrical show as a technical framework that presents the show in one unified fabric.

The research sought to reach through the problem of research, which is in the question of: What is the modeling of the

... Show More
View Publication Preview PDF
Crossref
Publication Date
Fri Mar 01 2019
Journal Name
Journal Of Pharmaceutical Sciences And Research
Anatomical study of the vegetative parts and seeds of Vitex agnus-castus plant
...Show More Authors

The species Vitex agnus-castus is an important medicinal plants and it is one of the cultivated and dicotyledon plants in Iraq. The anatomical of stem, petiole, midrib area, epidermis, veins, type of leaf stomata and seeds were studied by light microscope. In this research, shows the knowledge of anatomical characteristics of the studied plant, showing its importance as taxonomic characteristics through the sections of the stem, petiole, the midrib and the petals.

Publication Date
Wed Apr 05 2023
Journal Name
Journal Of Agriculture And Crops
Distribution and Classification of Medicinal Plants in Zakhikhah Area of Al-Anbar Desert
...Show More Authors

This study included the Zakhikhah area in the Al- Anbar desert, which it bounded on the north, east, and west by the Euphrates River and on the south by the Ramadi-Qaim road. Several exploratory field trips were taken to the study area. During this time, a semi-detailed area survey was carried out based on satellite imagery captured by American Land sat-7, topographic maps, and natural vegetation variance. All necessary field tools, including a digital camera and GPS device, were brought to determine the soil type and collect plant samples. All of these visits are planned to cover the entire state of Zakhikhah. All vegetation cover observations, identifying sampling sites and attempting to inventory and collect medicinal plants in t

... Show More
View Publication
Crossref
Publication Date
Sat Feb 01 2020
Journal Name
Journal Of Economics And Administrative Sciences
The role of the strategic mind of human resources managers in strategic drift
...Show More Authors

Abstract

The research aims to identify the role played by the strategic mind of human resources managers in reducing the levels of strategic drift that can face the organization, as the problem of research to overlook the importance of this role in monitoring and follow-up all the changes that may face the organization during the implementation of its strategy, therefore highlights the importance Research in providing a set of solutions to the problems faced by the researched organization and as far as the research variables, the researchers have adopted the descriptive analytical approach in the applied side, as adopted the questionnaire as a main tool for data collection, which was prepared based on a number of ready me

... Show More
View Publication Preview PDF
Crossref (1)
Crossref
Publication Date
Tue Oct 22 2024
Journal Name
Hemoglobin
Prevalence and Molecular Characterization of β-Thalassemia in Kirkuk Province of Northern Iraq
...Show More Authors

View Publication
Scopus (2)
Crossref (2)
Scopus Clarivate Crossref
Publication Date
Fri Jun 01 2012
Journal Name
Journal Of Economics And Administrative Sciences
Analysis of composite variance of experiments carried out according to design Latin box
...Show More Authors

We know that the experiments which conducted by latin square in one location or in one period (season), but there are many cases that need to conduct the same experiments in many locations or in many periods (seasons) to study the interaction  between the treatments and locations or between the treatments and periods (seasons) .In this research we present  an idea for  conduct  the experiment in several locations and in many period (seasons) by using LSD , it represent  acontribution in the area of design and analysis of experiments ,we had written. we had written (theoretically)  the general plans, the mathematical models for these experiments, and finding the derivations of EMS for each component (

... Show More
View Publication Preview PDF
Crossref
Publication Date
Mon Jun 23 2025
Journal Name
Sabir
The importance of teaching the diatopic variety of Spanish in the ELE classroom
...Show More Authors

Trends in the teaching of Spanish in terms of diatopic variables have had a significant change around the world, thanks to the evolution of technology, teaching approaches, processes and methods, pan-Hispanic policies and the reason why a person studies this language, which has caught the attention of linguistic researchers who teach Spanish around the world. Hence, the objective of this research is to show the scientific production regarding opinion trends in the teaching-learning processes of diatopic variables in the Ele classroom indexed in Scielo, Dialnet plus, Redalyc.org, Dialnet. unirioja .es, Researchgate.net, and Google Scholar, Thematic analysis was used to analyze the opinions of linguistic researchers. Of the 6 articles analyze

... Show More