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bijps-706
Investigation of Solubility Enhancement Approaches of Ticagrelor
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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).  

 

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Publication Date
Thu Dec 13 2018
Journal Name
Iraqi National Journal Of Nursing Specialties
Evaluation of Women's Knowledge about Risk Factors and Early Detection of Breast Cancer at Ibn Rushd College of Education in Baghdad University
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Objective: Evaluation of women's knowledge about risk factors and early detection of breast cancer at
Ibn Rushd college of education in Baghdad University.
Methodology: The study sample included (184) women in the Ibn Rushd College / University of
Baghdad, whose age ranged between (17-58) years. Data were collected through a structured
questionnaire prepared by the National Cancer Research Center which were answered during a scientific
symposium about breast cancer. The score was calculated by correcting the results of the answer, giving
one score for each correct answer and then estimating the level of knowledge and inputting all data in a
statistical program.
Results: The results showed limited level of women's

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Publication Date
Thu Aug 01 2019
Journal Name
Journal Of Economics And Administrative Sciences
Analysis of the sustainability of the public debt in light of the volatile oil revenues in Iraq for the period (2005-2015)
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Abstract

This study deals with the fluctuations of oil revenues and its effect on the public debt. This can be studied through the indicators of debt sustainability, the financial, and economic indicators which express the risk of debt. The study focuses on clarification of the public debt path and its management both domestic and foreign. The sustainability of debt takes an important role according the macroeconomic variables. This study stresses the relationship between the rental economy in Iraq and the risk of the public debt, it is very important to work high oil prices, and on investigating during high work to establish a fund to support the budget deficit. This will reduce future risks arising from the use of publi

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Sat Jan 04 2020
Journal Name
زانكو - الإنسانيات
The Effect of Linguistic Propositions on the Collection of Arabic Language Norms and the Development of Critical Thinking among Middle-Grade Students.
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The reality of teaching the Arabic language rules is not satisfactory, as the pedagogical methods used do not help students develop their mental skills, especially critical thinking skills. They are often traditional in terms of teaching students, who are passive, passive, often passive, active, and often active, their listening task, and the teacher's task of narrating facts and judgments. It is a blind simulation student, a dependency on others, and a weak spirit of creativity, innovation, and opinion. The opinions of educators and teachers almost agree on the reasons for students' weakness in learning the rules of Arabic, and that the reason lies in the way of teaching. The difficulty or the ease of the rules of Arabic does not lie in th

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Publication Date
Tue Dec 15 2020
Journal Name
Journal Of Baghdad College Of Dentistry
Impact of two non-nutritive sucking patterns on the development of anterior open bite in children of two kindergartens in Baghdad city
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Background: Non-nutritive sucking habit (NNSH) is the main environmental causative factor that disturbs normal orofacial development. In spite of the harmful effect of pacifier as a NNSH, mothers aware from the other types of NNSH like thumb sucking far more than pacifier use. Open bite is one of the most challenging malocclusions in orthodontics due to the high prevalence of relapse after treatment, so preventing the causative factor of its occurrence is essential at early age of child life. This study aims to assess the impact of two non-nutritive patterns on the development of anterior open bite in primary dentition and to compare which of these habits mostly affect open bite development. Materials and Methods: The sample consisted of

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Publication Date
Sat Jul 13 2024
Journal Name
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The Effect of Systemic Proteolytic Enzymes on Postoperative Inflammatory Response and Quality of Life after Surgical Extraction of Impacted Mandibular Third Molar
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Background: The surgical extraction of impacted third molar usually results in postoperative inflammation manifested as pain, facial swelling and trismus which may cause deterioration in the patient’s quality of life. Methods: This randomized controlled study included 56 patients indicated for surgical extraction of IMTM under local anesthesia. These patients were randomly assigned into two groups: a study group that included patients who received Tibrolin® postoperatively and a control group that did not. The predictor variable was whether to use SET or not. Pain measured by the pain numerical rating scale (NRS), facial swelling, and the degree of trismus were the outcome variables. The Arabic version of the Oral Health Impact P

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Mon Mar 07 2022
Journal Name
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The Effectiveness of Teaching impact of the Reflex Learning Strategy on the Fifth Class Female Student Achievement of the Geography Content Material
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Publication Date
Wed Jul 01 2020
Journal Name
Indian Journal Of Forensic Medicine & Toxicology
Assessment of undergraduate critical care nursing students ‘ knowledge and attitudes toward caring of dying patients in colleges of nursing at Baghdad university
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Publication Date
Wed May 10 2017
Journal Name
Journal Of The College Of Languages (jcl)
ФОРМИРОВАНИЕ КОММУНИКАТИВНО-РЕЧЕВОЙ КОМПЕТЕНЦИИ СТУДЕНТОВ КАФЕДРЫ Р The formation of verbal communication for students of Russian Language Department at College of Languages at University of Baghdad by using multiple technological means
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В статье рассматривается вопрос об использовании мультимедийных средств для оптимизации процесса формирования коммуникативной компетенции  в иракской аудитории с привлечением компьютерных технологий. Статья посвящена  использованию мультимедийных технологий  и  различных  приемов формирования интереса к русскому языку. Включение в процесс обучения коммуникативно-значимого, аутентичн

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Publication Date
Sun Jan 01 2017
Journal Name
Iraq Journal Of Agricultural Research
THE COMPARATIVE STUDY OF THE TOTAL COSTS AND NET REVENUE OF DIFFERENT TILLAGE SYSTEMS USING TWO TYPES OF SEEDLINGS IN THE PRODUCTION OF BARLEY GREEN VARIETY SAMEER IN THE GYPSUM SOILS
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Publication Date
Mon Jan 02 2017
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The Mathematical construct and its relationship with effective mathematical operations in both sides of the brain among students of the Department of Mathematics at the Colleges of Education and Basic Education
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The current research aims to identify: 1. The level of mathematical construct among the Department of Mathematics students in the colleges of education and basic education. 2. The level of effective mathematical operations in both sides of the brain at the Department of Mathematics students in the colleges of education and basic education. 3. The strength and direction of the correlation between the mathematical construct and effective mathematical operations on both sides of the brain at the Department of Mathematics students in the colleges of Education and Basic Education. To investigate the research objectives, the researcher formulated zero-main hypothesis for each aim and from the same hypothesis, three sub-zero hypotheses are deri

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