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
Sun Mar 02 2008
Journal Name
Baghdad Science Journal
Effect of Volatile Oil of Myrtus communis on growth and activities of some types of Pathogenic Bacteria and Candida albicans
...Show More Authors

This Study aimed to studying the effect of Volatile oil extracted from the leaves of Myrtus communis on the growth and activities of the following types of bacteria: Staphylococcus aureus, Streptococcus pyogenes, Klebsilla pneumoniae, Pseudomonas aeruginosa, and the yeast Candida albicans. The results showed an inhibitory effect of the oil on both the growth and activity of the tested microbes. This was reflected by the minimum inhibitory concentration (MIC) of Staphylococcus aureus, Streptococcus pyogenes, Klebsilla pneumoniae, Pseudomonas aeruginosa which was: (2.5, 1.25, and 2.5,5 % respectively), and the yeast (5) %. Also, the Minimum bactericidal concentration (MBC) to the bacteria mentioned above was (5, 2.5,5,10 % respectivel

... Show More
View Publication Preview PDF
Crossref
Publication Date
Tue Dec 31 2019
Journal Name
Iraqi Journal Of Market Research And Consumer Protection
USE OF IMMOBILIZED L-ARABINOSE ISOMERASE FOR PRODDUCTION OF TAGATOSE: USE OF IMMOBILIZED L-ARABINOSE ISOMERASE FOR PRODDUCTION OF TAGATOSE
...Show More Authors

L-arabinose isomerase from Escherichia coli O157:H7 Was immobilized with activated Bentonite from local markets of Baghdad, Iraq by 10% 3-APTES and treated with 10% aqueous glutaraldehyde, the results refer that the yield of immobilization was 89%, and pH profile of free and immobilized L-arabinose isomerase was 7 and 7.5 and it is stable at 6-8 for 60 min respectively, while, the optimum temperature was 30 and 35°C and it was stable at 35 and 40°C for 60 min but it loses more than 60 and 30% from its original activity at 50°C for free and immobilized L-arabinose isomerase respectively. Immobilized enzyme retained its full activity for 32 day, but it retained 73.58% of its original activity after storage for 60 d

... Show More
View Publication Preview PDF
Publication Date
Mon Jun 19 2023
Journal Name
Journal Of Engineering
A STUDY OF THE EFFECT OF SEMI-ANGLE OF CONE ON THE VIBRATION CHARACTERISTICS OF CYLINDRICAL-CONICAL COUPLED SHELL STRUCTURE
...Show More Authors

In this work, the effect of variation of semi-angle of the conical part on the vibration characteristics of cylindrical-conical coupled structure is investigated. The shell is made of polyester resin reinforced by continuous E-glass fibers. The case is analyzed experimentally and numerically for orthotropic shell structures. The experimental program is conducted by exciting the fabricated structure by an impact hammer and monitoring the response using an attached accelerometer for different semi-angles of the conical part.
Software named SIGVIEW is used to perform the signal processing on the acquired signal in order to measure the natural frequencies and the corresponding mode shapes. The numerical investigation is achieved using ANS

... Show More
View Publication Preview PDF
Crossref (1)
Crossref
Publication Date
Wed Aug 16 2023
Journal Name
Journal Of Humanities And Social Sciences Research
The impact of the use of hydromassage rehabilitation exercises on the recovery of certain motor potentials of knee roughness sufferers
...Show More Authors

The research included the introduction to the research and its importance as knee joint is an important joint in the human body that is prone to injury. One such injury is knee roughness injury that occurs as a result of the stress of the knee joint and age. The importance of examining the need for the use of rehabilitation exercises, especially in the watercourse system, is highlighted by the fact that the aquatic environment is one of the most important factors helping to alleviate pain and rehabilitate the knee joint and thereby improve the mobility of those with knee roughness. The problem of research is that rehabilitation exercises have been developed in the watercourse system on the basis of scientific bases with a repetitive and sys

... Show More
View Publication Preview PDF
Publication Date
Sun Dec 07 2008
Journal Name
Baghdad Science Journal
Measurements of Radon-222 and its Daughters Concentrations in Buildings of Department Physics in College of Sciences of Baghdad University
...Show More Authors

The present work aims to investigate approaches, measures and detection of indoor radon level in buildings of the department of physics in college of science of Baghdad University. CR-39 solid state nuclear track detectors were used to measure the radon concentrations inside the rooms, including five laboratories and five workplace rooms in ground and first storey of the department. The average radon concentration at first storey was found to be 43.1±13.2 Bq/m3 and 40.1±13.4 Bq/m3 at the ground storey. The highest level of radon concentration at the first storey in the radioactive sources store was 87.5±29 Bq/m3 while at the ground storey in room(2) was 70.2±24 Bq/m3 which is due to the existence radioactive sources in some selected

... Show More
View Publication Preview PDF
Crossref
Publication Date
Sun Apr 06 2014
Journal Name
Journal Of Educational And Psychological Researches
Spiritual intelligence in a sample of students from the University of Baghdad in the Light of some of the variables
...Show More Authors

The research aims to identify intelligence spiritual among a sample of students Baghdad University as well as to identify the differences between students in intelligence spiritual according to variable type (male - female), and variable area of ​​study (Science - a human) and variable (First grade - fourth grade), The research sample consisted of (300) students, were applied scale search - a spiritual Intelligence Scale (prepared by the researcher), has resulted in the search results for: -

The students of the University of Baghdad (sample) enjoyed a high level of spiritual intelligence.
- There are no differences between males and females in the spiritual intelligence.
- There

... Show More
View Publication Preview PDF
Publication Date
Tue Nov 01 2016
Journal Name
Journal Of Economics And Administrative Sciences
The Impact of the Financial Reporting of Liabilities and Assets of Deferred Income Tax in the quality of Accounting Information
...Show More Authors

Abstract

The research problem Focused about extent adoption of the financial reporting obligations and assets of the deferred income tax attributable to the concepts of accounting theory and whether the tax laws or accounting principles as well as local accounting rules to recognize the obligations and assets of deferred income tax in the financial statements, and what is the impact of the financial reporting of liabilities and assets Deferred tax in the quality of accounting information, and research aims to the statement of the accounting concepts of the theory of financial reporting obligations and assets of deferred income tax, view and analyze the differences in reporting, resulting from a discrepanc

... Show More
View Publication Preview PDF
Crossref
Publication Date
Wed Nov 01 2017
Journal Name
Journal Of Economics And Administrative Sciences
Analysis of the effects of foreign direct investment in financial account of the balance of payments iraqi for 2003-2015
...Show More Authors

The study aims to make an in-depth  analysis and the financial account components in the Iraqi balance of payments because it reflects the economic center of the country towards outside world, it also helps in making decision about monetary and financial policies, finance and foreign Trade the importance of FDI for Iraq lies as an important sources as wells provides advanced technology  and job chances, It also avoids the country negative effects of borrowing processes from abroad . for analyzing direct and indirect foreign investment on the balance of payments and financial account in a period between (2003 to 2015), a community and research sample have been selected, presented in CBI/ Balance of payments. Department,

... Show More
View Publication Preview PDF
Crossref
Publication Date
Wed Mar 23 2022
Journal Name
Journal Of Educational And Psychological Researches
The level of evaluation of the educational counselors ’performance as a predictor of their level of satisfaction with their evaluation
...Show More Authors

The current research aims to reveal the level of satisfaction of the mentors with the evaluation of their performance according to gender (male - female) and to formulate the predictive equation for the level of performance (dependent variable) from knowing the level of satisfaction with the evaluation (independent variable). (16 paragraphs) contains alternatives to the answer that measures the level of satisfaction (weak, medium, and high) (1,2,3), that is, with a hypothetical average of (32). It consisted of 100 educational counselors consisting of 45 males and 55 females, the results of the research concluded that the level of satisfaction with performance is below the mean when compared with the hypothetical average of the scale of s

... Show More
View Publication Preview PDF
Publication Date
Thu Feb 28 2019
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
The Role of Job Enrichment in Building Differentiation Strategy Service: Analytical Exploratory Study of the Views of a Sample of the General Managers and Heads of Departments and Officials of the People in the General Establishment of Civil Aviation
...Show More Authors

According to the importance of the subject of research, and the importance of the surveyed organization as a dynamic sector of the country in general , The research attempts to suggest to service organizations in general reconsidering the currently adopted mechanisms in the redesign of its functions , and in the services provided industry . The data was collected from (98) Director Mangers , head of department and head of division . The research tool is the questionnaire , which included (50) items . The results show Significant Effect & Correlation relationship between the two variables due to their dimensions . These lead to he application of job enrichment technology will increase the organization's ability to possess efficient hu

... Show More
View Publication Preview PDF
Crossref