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
Sat May 01 2021
Journal Name
Journal Of Physics: Conference Series
Characteristics of probing electrons behavior inside the chamber of scanning electron microscope
...Show More Authors
Abstract<p>The electron mirror phenomenon has been explored to describe the behavior of a probing electron trajectory inside the chamber of scanning electron microscope (SEM). This investigation has been carried out by means of the modulated mirror plot curve technique. This method is based on expanding sample potential to a multipolar form to detect the actual distribution of the trapped charges. Actually an experimental result is used to guiding results of this work toward the accurate side. Results have shown that the influence of each type of multipolar arrangement (monopole, dipole, quadruple, octopole … etc.) mainly depends on the driving potential.</p>
View Publication
Scopus (1)
Crossref (1)
Scopus Crossref
Publication Date
Wed Oct 10 2018
Journal Name
Al-kindy College Medical Journal
Role of Diffusion-Weighted MR Imaging in Characterization of Posterior Fossa Tumors
...Show More Authors

Background: Conventional  MR imaging is essential for diagnosis and evaluation of the posterior fossa tumors  Objectives: To assess the value of diffusion weighted imaging and apparent diffusion coefficient in making distinction between different histological types of posterior fossa tumors.

Type of the study: Cross-sectional study.

Methods: Brain MRI and DWI assessed 19 patients (12 female and 7 male) with MRI diagnosis of posterior fossa tumors. absolute ADC values of contrast -enhancing solid tumor region and ADC ratio of solid tumor to ADC of normal -appearing deep White matter were compared with histological diagnosis postoperatively .The m

... Show More
View Publication Preview PDF
Crossref
Publication Date
Mon Jan 01 2018
Journal Name
Aip Conference Proceedings
Study the effect of nano SiO2 on dielectric strength property of zirconia
...Show More Authors

View Publication
Scopus (3)
Crossref (2)
Scopus Clarivate Crossref
Publication Date
Mon Dec 02 2019
Journal Name
Technologies And Materials For Renewable Energy, Environment And Sustainability
Effect of thickness variation CdO/PSi thin films on detection of radiation
...Show More Authors

CdO films were deposited on substrates from glass, Silicon and Porous silicon by thermal chemical spray pyrolysis technique with different thicknesses (130 and 438.46) nm. Measurements of X-ray diffraction of CdO thin film proved that the structure of the Polycrystalline is cubic lattice, and its crystallite size is located within nano scale range where the perfect orientation is (200). The results show that the surface’s roughness and the root mean square increased with increasing the thickness of prepared films. The UV-Visible measurements show that the CdO films with different thicknesses possess an allowed direct transition with band gap (4) eV. AFM measurement revealed that the silicon porosity located in nano range. Cadmium oxide f

... Show More
Scopus (2)
Scopus
Publication Date
Sun Mar 01 2009
Journal Name
Baghdad Science Journal
Effect Of Chlorothalonil On Some Cytogenetic Parameters Of Human Peripheral Blood Lymphocytes
...Show More Authors

The study aimed to investigate the effect of fungicides chlorothalonil at different concentrations ( 0.1 , 0.5 , 5 , 25 , 50 ) × 10 - 5 M on some cytogenetic parameters of human peripheral blood lymphocytes . The genotoxicity parameters were estimated by the number of chromosomal aberrations (CAs) and their types and by estimating the induced micronuclei (Mn) . Cytotoxic effect recorded by estimating the mitotic index (MI) . Results revealed that the fungicide increased the CAs in dose – response pattern with positive correlation coefficient ( r = + 0.964) , there was a significant differences among the concentrations (P<0.01) . The major CAs records chromosomal breakage at concentrations. 0.5 , 5 , 25 , and 50 , while the lowest concen

... Show More
View Publication Preview PDF
Crossref
Publication Date
Tue Feb 17 2026
Journal Name
Al-adab Journal
The Sense of Freedom in Kate's Chopin's The Story of an Hour
...Show More Authors

View Publication
Publication Date
Tue Jan 01 2019
Journal Name
Technologies And Materials For Renewable Energy, Environment And Sustainability: Tmrees19gr
Theoretical study for the calculation of some attenuation parameters of polymeric composites
...Show More Authors

View Publication
Scopus (3)
Scopus Clarivate Crossref
Publication Date
Wed Dec 14 2016
Journal Name
Journal Of Baghdad College Of Dentistry
Comparison of Immunohistochemical Expression of DNMT3B among Oral, Laryngeal and Skin SCC
...Show More Authors

Background: Recently epigenetic alterations have received increased attention because of theirimportant role in the process of tumerigenesis. It has been found that more than half of genetic changes were epigenetic. Epigenetic alterations are catalyzed by DNMTs enzymes. Increased knowledge about this molecular event may achieve progress in the war against cancer. The aim of this study was to evaluate and compare the expression of DNMT3B among oral, laryngeal and skin SCC. Materials and Methods: This study was performed on (120) formalin-fixed, paraffin-embedded blocks, histopathologically diagnosed as oral, laryngeal and skin SCC). Immunohistochemical staining of DNMT3B antibody was performed on each case of this study. Results: The immunoh

... Show More
View Publication Preview PDF
Crossref
Publication Date
Sun Jan 01 2023
Journal Name
International Journal Of Research In Social Sciences &amp; Humanities
The Role of Labor Relations in Reducing the Cases of Job Withdrawal
...Show More Authors

he current research aims to analyze the relationship and the level of influence of labor relations in reducing the cases of job withdrawal in private colleges in Baghdad. (265) individuals from department heads, university professors, and teaching staff in (7) private colleges located in the capital, Baghdad, and based on the Stephen Thompson equation for small samples, the sample size was determined by (157) teachers, and the questionnaire was adopted as a main tool for collecting data and information After ensuring the validity and reliability of its contents, and to test the relationship of influence, correlation and interaction between the research variables, two main hypotheses were formulated from which (5) sub-hypotheses eman

... Show More
View Publication
Crossref
Publication Date
Sun Mar 06 2011
Journal Name
Baghdad Science Journal
The effect of additives metal on the D.C conductivity of epoxy resin
...Show More Authors

The present studies are focused on the modification of the properties of epoxy resin with different additives namely aluminum, copper by preparing of composites systems with percentage (20%, 40% and 50%) of the above additives. The experimental results show that the D.C of conductivity on wt% filler content at ( 293-413 ) K electrical conductivity of all above composites increased with temperature for composites with filler contact and find the excellent electrical conductivity of copper and lie between (2.6*10-10 - 2.1*10-10)?.cm . The activation energy of the electrical conductivity is determined and found to decrease with increasing the filler concentration.

View Publication Preview PDF
Crossref