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 Oct 08 2022
Journal Name
Journal Of Computational Design And Engineering
Twisted-fin parametric study to enhance the solidification performance of phase-change material in a shell-and-tube latent heat thermal energy storage system
...Show More Authors
Abstract<p>Phase change material (PCM) is considered as one of the most effective thermal energy storage (TES) systems to balance energy supply and demand. A key challenge in designing efficient PCM-based TES systems lies in the enhancement of heat transmission during phase transition. This study numerically examines the privilege of employing twisted-fin arrays inside a shell-and-tube latent heat storage unit to improve the solidification performance. The presence of twisted fins contributes to the dominating role of heat conduction by their curved shapes, which restricts the role of natural convection but largely aids the overall heat-transfer process during solidification. The heat-discharge </p> ... Show More
View Publication
Scopus (13)
Crossref (5)
Scopus Clarivate Crossref
Publication Date
Fri Feb 01 2019
Journal Name
Meta Gene
Cytokine gene variations and their impact on serum levels of IFN-γ, IL-2, IL-4, IL-10 and IL-12 among Iraqi Arabs
...Show More Authors

View Publication
Scopus (11)
Crossref (10)
Scopus Clarivate Crossref
Publication Date
Tue Jun 15 2021
Journal Name
Al-academy
The semiotic of the Islamic blazon - a related analytical study between the Islamic blazon and its publicity message: رغده بنت فيصل بن خضر الدعواني
...Show More Authors

This study discusses the semiotic of the Islamic blazon - a related analytical study between the Islamic blazon and its visual publicity message. The aim of the current study is to explore the related relationship between the Islamic blazon and its visual publicity message. The sample is contained Five of Islamic blazon in the Mamelukes period which is between 1250 to 1517. The methodology is descriptive-analytical, and the result is that there is a clear relation between the Islamic blazon with its visual publicity message. This study's recommendation is to go towards analyzing the meanings of the cultural legacies of the Islamic civilization, and researching the implicit meanings accompanying these features leads to a deeper understand

... Show More
View Publication Preview PDF
Crossref
Publication Date
Wed Jan 23 2019
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
Cancellation in the Life Insurance Policies and its Impact on the Financial Solvency of Insurance Companies: Applied Research in the Iraqi General Insurance Company
...Show More Authors

This research cancellations in life insurance policies and their impact on the solvency of the insurance companies (Applied Research in the Iraqi general insurance company), The study was descriptive approach in identifying and addressing variables which consists of {cancellations in life insurance} independent variable, the financial solvency of insurance companies as the dependent variable, and for the purpose of achieving the objectives of the research were formulated one hypothesis has been tested in the Iraqi insurance company, the researcher used the financial statements in the collection data needed for the study and information . The research found a number of conclusions highlighted that inflation, as well as economic variables

... Show More
View Publication Preview PDF
Crossref
Publication Date
Mon Jan 28 2019
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
The Managerial Skills and It`s Role in Strengthening the Competitive Edge of Companies: A Case Study in the General Company for Construction Industries
...Show More Authors

This research tries to reveal how to manage and control the competitive edge for business by building managerial skills in various organizational levels. Our research aims at finding out the nature of various technical, human and in tellectual skills of a new president whose superiority is his competitive ness in the application field at general company for construe tioual  industriesand testing the surveyed minor and major changes through a questionnaire to collect information from officials. The sample was composed of (45) director. The data was analyzed  using some methods and statistical programs. The most prominent of these is (SPSS) that was used to extract the arithmetic mean, standard deviation, correlation coefficient

... Show More
View Publication Preview PDF
Crossref
Publication Date
Sun May 22 2022
Journal Name
International Journal Of Early Childhood Special Education
The impact of an instructional-learning design based on the brain- compatible model in systemic thinking among first intermediate grade female students in Mathematics
...Show More Authors

The research aimed to identify “The impact of an instructional-learning design based on the brain- compatible model in systemic thinking among first intermediate grade female students in Mathematics”, in the day schools of the second Karkh Educational directorate.In order to achieve the research objective, the following null hypothesis was formulated:There is no statistically significant difference at the significance level (0.05) among the average scores of the experimental group students who will be taught by applying an (instructional- learning) design based to on the brain–compatible model and the average scores of the control group students who will be taught through the traditional method in the systemic thinking test.The resear

... Show More
Publication Date
Sat Sep 30 2023
Journal Name
Iraqi Geological Journal
Geology, Pb and S Isotope Geochemistry, and Genesis of the Na Bop-Pu Sap Lead-Zinc Deposit in the Cho Don area, Northeastern Vietnam
...Show More Authors

The Na Bop-Pu Sap Pb-Zn ore bodies represent a typical vein-type lead-zinc deposit situated in the Cho Don area and are currently being extracted for their lead and zinc resources. This deposit is characterized by its significant scale and quality and is considered one of the prominent lead-zinc deposits in the Cho Don area. Despite its significance, this deposit has not received adequate attention, resulting in limited knowledge of its geology, mineralization, and deposit genesis model. To address this knowledge gap, our study utilized several methodologies, including field surveying, ore mineral analysis under a microscope, and S and Pb isotopic geochemistry. By employing these approaches, we were able to obtain specific insights

... Show More
View Publication
Scopus (1)
Scopus Crossref
Publication Date
Wed Dec 14 2011
Journal Name
Journal Of Faculty Of Medicine Baghdad
The correlation between FEV1/ FVC with Arm span to height or chest to waist ratio as an index of pulmonary function in healthy subject.
...Show More Authors

Abstract

Publication Date
Fri May 10 2019
Journal Name
Research Journal Of Chemistry And Environment
Solid Phase Extraction of Theophylline in Aqueous Solutions by Modified Magnetic Iron Oxide Nanoparticles as an Extractor Material and Spectrophotometry Technique for the Determination
...Show More Authors

new, simple and fast solid-phase extraction method for separation and preconcentration of trace theophylline in aqueous solutions was developed using magnetite nanoparticles (MIONPs) coated with aluminium oxide (AMIONPs) and modified with palmitate (P) as an extractor (P@AMIONPs). It has shown that the developed method has a fast absorbent rate of the theophylline at room temperature. The parameters that affect the absorbent of theophylline in the aqueous solutions have been investigated such as the amount of magnetite nanoparticle, pH, standing time and the volume, concentration of desorption solution. The linear range, limit of quantification (LOQ) and limit of detection (LOD) for the determination of theophylline were 0.05-2.450 μg mL-

... Show More
View Publication
Publication Date
Tue Jun 12 2018
Journal Name
المجلة العراقية لبحوث السوق وحماية المستهلك
BIOLOGICAL ASPECTS AND PREDATORY EFFICIENY OF PREDATOR Chilocorus bipustulatus (L.) COLEOPTERA :COCCINELLIDAE ON DATE PALM SCALE Parlatoria blanchardi (T.) DIASPIDIDAE: HOMOPTERA UNDER LABORATORY CONDITIONS.
...Show More Authors

Laboratory studies were conducted at the biological control unit, college of Agriculture, University of Baghdad to evaluate some biological aspects of the predator Chilocorus bipustulatus (Coleoptera: Coccinellidae), which is considered one of the most important predators on many insect pests, especially the scale insect, Parlatoria blanchardi, (Homoptera: Diaspididae) on date palms. The results showed that biological parameters of the predator were varied according to different degree of temperature. Egg incubation period was significantly different and reached to 7.5 and 5.44 day at 25 and 30°C respectively, Fertility was the same 100% at both temperature degrees. Larval growth periods were 17.41 and 16.12 day as well as the mortality du

... Show More