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 Jan 01 2024
Journal Name
International Journal Of Literacy And Education
The availability of concepts and applications of artificial intelligence in the content of the chemistry textbook for the fourth scientific grade
...Show More Authors

View Publication
Crossref
Publication Date
Sun Feb 15 2026
Journal Name
University Of Anbar Sport And Physical Education Sciences
The Impact of the Concept Maps Strategy in the Guided Discovery Method at Learning the Skill of Layup Shooting of Basketball
...Show More Authors

View Publication
Publication Date
Fri Jan 22 2021
Journal Name
International Journal Of Agricultural & Statistical Sciences
EFFECT OF GROWING MEDIA, NUTRIENT SOLUTION AND CONTROL OF FLOWERING ON THE PRODUCTIVITY OF THE CUCUMBER CULTIVATED BY THE SOILLESS CULTURE.
...Show More Authors

Publication Date
Tue Nov 09 2021
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
Enhancing the effectiveness of the company in light of the practice of leadership empowerment: Applied research in the National Insurance Company
...Show More Authors

The aim of the research is to demonstrate the importance of leadership empowerment in its dimensions (knowledge, participation in decision-making, incentives, trust between the leader and subordinate, delegation of authority and communication) and its impact on enhancing the effectiveness of the company in its dimensions Represented by (achievement of objectives, quality of insurance service, adaptation to work environment and job satisfaction), by adopting the questionnaire as a main tool in collecting data from officials in the National Insurance Company, numbering (56) surveyed in job sites (section manager, division official and unit official) Their answers were analyzed using the SPSS statistical program in calculating the a

... Show More
View Publication Preview PDF
Publication Date
Fri Aug 06 2021
Journal Name
Webology
The Role Of Digital Informatics In The Quality Of Scientific Research In In University Libraries: An Analytical Study Of Iraqi Libraries
...Show More Authors

View Publication
Publication Date
Fri Jan 01 2021
Journal Name
International Journal Of Agriculture And Statistical Science
COMPARISON OF FORECASTING OF THE RISK OF CORONAVIRUS (COVID-19) IN HIGH-QUALITY AND LOW-QUALITY HEALTHCARE SYSTEMS, USING ANN MODELS
...Show More Authors

COVID-19 is a disease that has abnormal over 170 nations worldwide. The number of infected people (either sick or dead) has been growing at a worrying ratio in virtually all the affected countries. Forecasting procedures can be instructed so helping in scheming well plans and in captivating creative conclusions. These procedures measure the conditions of the previous thus allowing well forecasts around the state to arise in the future. These predictions strength helps to make contradiction of likely pressures and significances. Forecasting procedures production a very main character in elastic precise predictions. In this case study used two models in order to diagnose optimal approach by compared the outputs. This study was introduce

... Show More
Preview PDF
Scopus (3)
Scopus
Publication Date
Tue Sep 15 2015
Journal Name
Alustath Journal For Human And Social Sciences
The Degree of Satisfaction of Secondary School Principals with the Role of Universities and their Obstacles in Developing their Administrative Skills
...Show More Authors

    A field study aimed at identifying the degree of satisfaction of secondary school principals with regard to the role of universities and their obstacles in developing their administrative skills. It adopted the descriptive analytical approach. The research community consisted of (249) male and female principals in the schools of Baghdad (Al-Rusafa and Karkh), and the research sample was chosen by the simple random stratified method at a percentage of (40%) of the research community, and the number of the sample was (100) male and female principals. A questionnaire consisting of (40) items distributed between two domains was developed. Its validity and reliability were confirmed. The researcher used the (SPS

... Show More
View Publication Preview PDF
Publication Date
Thu Jun 01 2017
Journal Name
Journal Of The College Of Languages (jcl)
Plain Language Movement and Legal Translation : An Analytical Study of Two Translations of a Contract of Lease from Arabic into English
...Show More Authors

The present paper addresses one of the most challenging topics in translation; namely legal translation in the framework of two different approaches; the classical (formal) and the more recent (functional). The latter approach is the outcome of the process of simplifying legal language known technically as Plain Language Movement. The advent of this movement dates back to the 1950s, in response to the widely-held complain about the awkwardness of the legal register. Within this framework, the salient features of legal language, at the various linguistic and textual levels, underwent reconsideration in favor of more publicly digested expressions. The paper then subjects two translations of a lease contract to analysis in the ligh

... Show More
View Publication Preview PDF
Publication Date
Mon Sep 30 2019
Journal Name
College Of Islamic Sciences
Critical mindset in the philosophy of Sadruddin Shirazi         (D 1050 AH)              And the concepts of originality of existence and what time
...Show More Authors

The researcher deals with an important issue in her research - especially as she progresses to the doctoral stage thanks to God (Almighty) and his mentor - the relationship of philosophy to nodal origins. Therefore, she studied the philosophy of Shirazi, which is the key to the mental solutions that the speakers and philosophers stopped. And to conclude scientific results as well as the study of philosophy researcher as a station in the doctoral stage, to be familiar with the philosophical interpretation and the origins of the faith and its philosophical vocabularies such as existence, self, movement, astronomy, time and others. At the same time draw the attention of science students to the issue of philosophical interpretation and its r

... Show More
View Publication Preview PDF
Publication Date
Sat Dec 30 2023
Journal Name
Journal Of Economics And Administrative Sciences
The Role of Quality of Work Life in Reinforcing Core Competencies: A Descriptive and analytical research in the Ministry of Health
...Show More Authors

The research aims to diagnose the shortcomings and weaknesses in applying the dimensions of the quality of work life and the extent of their impact on employees’ attitudes and behaviors, and thus their relationship to enhancing their core competencies. The scientific value of the research stems from highlighting the importance of the dimensions of the quality of professional life in improving the productive efficiency of workers in the public sector and raising the level of organizational performance. Because the quality of working life plays an important role in enhancing the core competencies of employees in the public sector, it can also be an incentive or a disincentive for any employee by adapting to the economic and social condit

... Show More
View Publication Preview PDF
Crossref