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 Sep 30 2023
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Optimization of Gas Lifting Design in Mishrif Formation of Halfaya Oil Field
...Show More Authors

The optimization of artificial gas lift techniques plays a crucial role in the advancement of oil field development. This study focuses on investigating the impact of gas lift design and optimization on production outcomes within the Mishrif formation of the Halfaya oil field. A comprehensive production network nodal analysis model was formulated using a PIPESIM Optimizer-based Genetic Algorithm and meticulously calibrated utilizing field-collected data from a network comprising seven wells. This well group encompasses three directional wells currently employing gas lift and four naturally producing vertical wells. To augment productivity and optimize network performance, a novel gas lift design strategy was proposed. The optimization of

... Show More
View Publication Preview PDF
Crossref (1)
Crossref
Publication Date
Mon Oct 03 2022
Journal Name
....
THE SEEDS OF ECOCRITICISM: A STUDY IN THE POETRY OF JOHN CLARE
...Show More Authors

Nowadays, the worldwide issue of the environment occupies the minds not only of ecological experts and politicians but also is addressed in cultural fields and literature in particular. The conceptualization of ecocriticism, whether in the ecological field or cultural studies, has come as a response to the increasing public awareness of numerous environmental crises. Most ecocritics regard John Clare (1793-1864) as a 'proto-ecological' British poet since his poetry incorporates ecological issues which were not then categorized as they are now. The study offers a precise illustration of ecocriticism coupled with a number of the most significant ecological concepts proven in selected poems by John Clare. The ecocritical reading of Clare's po

... Show More
Preview PDF
Publication Date
Sat Oct 15 2022
Journal Name
Diyala Journal Of Medicine
Chemical and microbiological properties of drinking water in the city of Baghdad
...Show More Authors

Background: The quality of drinking water is directly related to community health. Therefore, improving the quality of drinking reflects positively on the health situation in general. The studies that deal with the quality of drinking water in the city of Baghdad in terms of chemical or microbial content are very scanty. Objective: The current review highlights the most important studies and research articles that concern the quality of drinking water, both bottled water and tap water, in terms of chemical and biological contamination and chemophysical specifications for drinking water. Abstract: Studies have shown that drinking water in the city of Baghdad, especially tap water, contains certain levels of heavy metals,

... Show More
View Publication
Scopus (3)
Crossref (1)
Scopus Crossref
Publication Date
Wed Apr 29 2020
Journal Name
Indian Journal Of Forensic Medicine & Toxicology
Scolicidal Activity of Zirconium Oxide (ZrO2) nanoparticles Against Protoscolices of Hydatid Cysts
...Show More Authors

Hydatidosis is a sickness that affects human and farm animals. This disease is deemed as a public health problem in different regions of the world until nowadays. Surgical overlaps is the best way to treat the disease, while the risk of surgery lies in the possibility of cyst rupture and leakage of protoscolices and the recurrence of infection again, this prompted researchers to use scolicidal agents before surgery such as ethanol, plant extracts, to reduce parasite spread and recurrence of infection, recently researchers have been using nanoparticles as a scolicidal agent, like gold nanoparticles, silver nanoparticles, selenium nanoparticles, and others. This research aims to evaluate the fatal effect of zirconium oxide (ZrO2) nanoparticle

... Show More
View Publication Preview PDF
Crossref (3)
Crossref
Publication Date
Tue Oct 12 2021
Journal Name
Engineering, Technology & Applied Science Research
The Effect of Nanomaterials on the Properties of Limestone Dust Green Concrete
...Show More Authors

Portland cement is considered the most involved product in environmental pollution. It is responsible for about 10% of global CO2 emissions [1]. Limestone dust is a by-product of limestone plants and it is produced in thousands of tons annually as waste material. To fulfill sustainability requirements, concrete production is recommended to reduce Portland cement usage with the use of alternative or waste materials. The production of sustainable high strength concrete by using nanomaterials is one of the aims of this study. Limestone dust in 12, 16, and 20% by weight of cement replaced cement in this study. The study was divided into two parts: the first was devoted to the investigation of the best percentage of replacement of waste

... Show More
View Publication
Crossref (10)
Crossref
Publication Date
Thu Feb 05 2026
Journal Name
Philosophy Journal
Philosophy of Civilization Read and critique and analysis of the selected models
...Show More Authors

View Publication
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