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 Dec 25 2023
Journal Name
Journal Of Legal Sciences
The Principle of Prohibiting the Diversion of the Natural Course of International River Waters
...Show More Authors

The research deals with the principle of the prohibition of international waterway diversion in the law of international watercourses. The research reviews individual and collective doctrinal efforts that have touched upon the principle as an internationally wrongful act because of its serious damage and consequences for downstream States. The research addresses the nature of the principle of the prohibition of diversion of international watercourses; its various effects; principles of international law establishing the principle of prohibition of diversion; and its application in State practice and international justice. This principle has been enshrined in most international treaties and judicial decisions. The principle of prohibition

... Show More
View Publication Preview PDF
Publication Date
Wed Jul 01 2020
Journal Name
Plant Archive
A comparative taxonomic study of seeds of some plants of rosaceae family in Iraq
...Show More Authors

Preview PDF
Scopus
Publication Date
Wed Jun 07 2023
Journal Name
Journal Of Educational And Psychological Researches
Selective Visual Attention among Students of Colleges of Education At The University Of Mosul
...Show More Authors

The research aims to identify the level of selective visual attention among students of the faculties of education at the University of Mosul. To achieve the goal of the research, the researchers chose a stratified random sample of students from the faculties of education at the University of Mosul for the academic year (2020-2021). The sample size was (652) students from the scientific and humanitarian specializations, the second and fourth stages. The researchers developed a test of multiple-choice to measure the selective visual attention, which consisted of (42) items. The results revealed that the students of the faculties of education for human sciences have an appropriate level of selective visual attention. There are statisticall

... Show More
View Publication Preview PDF
Publication Date
Fri Dec 30 2022
Journal Name
Journal Of Mathematics
Estimation of Parameters of Finite Mixture of Rayleigh Distribution by the Expectation-Maximization Algorithm
...Show More Authors

In the lifetime process in some systems, most data cannot belong to one single population. In fact, it can represent several subpopulations. In such a case, the known distribution cannot be used to model data. Instead, a mixture of distribution is used to modulate the data and classify them into several subgroups. The mixture of Rayleigh distribution is best to be used with the lifetime process. This paper aims to infer model parameters by the expectation-maximization (EM) algorithm through the maximum likelihood function. The technique is applied to simulated data by following several scenarios. The accuracy of estimation has been examined by the average mean square error (AMSE) and the average classification success rate (ACSR). T

... Show More
View Publication Preview PDF
Scopus (5)
Crossref (2)
Scopus Clarivate Crossref
Publication Date
Thu Feb 01 2024
Journal Name
Baghdad Science Journal
Significance and Conservation of Birds of the Genus of Bee-eater (MEROPS) in Uzbekistan
...Show More Authors

The purpose of this article is to identify and evaluate the importance of birds of the genus Merops (European Bee-eater -Merops apiaster and Blue-cheeked Bee-eater -Merops persicus) in Uzbekistan, as well as to develop recommendations aimed at solving some problems associated with its conservation. As a result of the study, in the aspect of biocenotic relations, the natural significance of these species was revealed. The economic value is determined and analyzed in beekeeping farms. From the study of the remains of food contained in the stomachs, throats and nests of M.apiaster, a preliminary list of the main species of the food spectrum has been compiled. Based on the bioacoustic repellent "Korshun-8"

... Show More
View Publication Preview PDF
Scopus (3)
Crossref (3)
Scopus Crossref
Publication Date
Tue Feb 14 2023
Journal Name
Journal Of Educational And Psychological Researches
The Organizational Relaxation of Employees of the Educational Directorates in the Sultanate of Oman
...Show More Authors

Abstract

The current research aims to identify the level of organizational relaxation among the employees of educational directorates in the Sultanate of Oman. The descriptive approach was used, as well as a questionnaire of two parts to collect data. The questionnaire consists of (15) items divided into three themes about the relaxing level. It was applied on a sample of (406) male & female employees of the educational directorates who were randomly selected. The results of the study showed that the level of organizational relaxation was low. The study results also found that there were no statistically significant differences at the level of significance (α ≤ 0.05) of the study sample in the level of org

... Show More
View Publication Preview PDF
Publication Date
Sun Dec 07 2008
Journal Name
Baghdad Science Journal
The effect of doping ratio of Cu on the structural properties of CdSe Films
...Show More Authors

Films of CdSe have been prepared by evaporation technique with thickness 1µm. Doping with Cu was achieved using annealing under argon atmosphere . The Structure properties of these films are investigated by X-ray diffraction analysis. The effect of Cu doping on the orientation , relative intensity, grain size and the lattice constant has been studied. The pure CdSe films have been found consist of amorphous structure with very small peak at (002) plane. The films were polycrystalline for doped CdSe with (1&2wt%) Cu contents and with lattice constant (a=3.741,c=7.096)A°, and it has better crystallinty as the Cu contents increased to (3&5wt%) Cu. The reflections from [(002), (102). (110), (112), and (201)]planes are more prominen

... Show More
View Publication Preview PDF
Crossref
Publication Date
Thu Jun 15 2017
Journal Name
Journal Of Baghdad College Of Dentistry
A Comparison of Vertical Marginal Fit of different Brands of Translucent Zirconia Crown Restorations
...Show More Authors

Background: As the development of zirconia crown using CAD/CAM technology, the usage of full zirconia crown is gradually increased. The aim of this in-vitro study was to evaluate and contrast the vertical marginal fit of single all-ceramic translucent zirconia crowns constructed from different brands translucent zirconia blanks. Materials and Methods: An acrylic resin model of a left maxillary premolar was prepared all around the tooth with (1 mm) depth and 3D scanning to get fifteen STL files, then distributed into three groups (Imes-icor, Whitepeaks and Dental direct), 3D scanning and milling machine by Imes-icor CAD/CAM devise. Marginal gaps along vertical planes were measured at four indentations at the (mid mesial, mid distal, mid bucc

... Show More
View Publication Preview PDF
Crossref
Publication Date
Sat Mar 30 2002
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Effects of Drying Conditions on the Properties of Dried Particles of Powdered steep Liquor
...Show More Authors

View Publication Preview PDF
Publication Date
Fri Nov 14 2025
Journal Name
Al-fatih Journal
Effect of resistance training on the development of marital some elements of physical fitness
...Show More Authors

يشهد العالم تقدما في كافة مجالات الحياة المختلفة وتزداد الحياة صعوبة يوما بعد يوم, ويزداد البحث في كافة المجالات التي تعمل على خدمة الإنسان ولقد طال هذا التقدم النشاط الرياضي ,فقد يكون لتطور التدريب الرياضي وتنوع أساليبه الدور الكبير في تحقيق اللياقة البدنية التي تعد إحدى أهم الأهداف التي يرمي إليها الدرس في كلية التربية الرياضية . واللياقة البدنية تستمد أهميتها من كونها إحدى مكونات اللياقة الشاملة التي بدو

... Show More
View Publication