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 06 2012
Journal Name
Journal Of Engineering
Prediction of Smear Effect on the Bearing Capacity of Driven Piles
...Show More Authors

Publication Date
Wed Sep 30 2020
Journal Name
Association Of Arab Universities Journal Of Engineering Sciences
Impact of Rationing on The Properties of Cement-Treated Gypsum Canals
...Show More Authors

The scarcity of irrigation water requires procedures of specific. One of these procedures is the implementation of the rationing system (a period of the irrigation followed by a period of the dry). This system can have an impact on the properties of irrigation channels. Therefore, the study of rationing system for irrigation channels is important in both water resources and civil engineering, especially if they are constructed with gypseous soil. In order to assess the rationing system on gypseous canals stabilized with a specific ratio of cement, practical experiments were conducted to detect the effect of wetting and drying cycles on the physical and hydraulic behavior of this soil and calculation of some properties of soil such a

... Show More
View Publication
Crossref (3)
Crossref
Publication Date
Sun Dec 01 2013
Journal Name
Journal Of Economics And Administrative Sciences
The Influence of the Industrial Buyer Behavior on channels of distribution
...Show More Authors

Abstract:

This study deals with the influence of the industrial buyer behavior in Channels of distribution. It concentrates on one section of management levels in the company. Which is that of administrative managers The research problem is attempt to study and analysis the influence of industrial buyer behavior in channels of distribution.. The aiming at achieving a number of applicable goals depending on one major hypotheses I set a questionnaire in collecting the data and information relating to the study، which was distributed to sample of ( 30) department manager heads of section states company .  In order to process the data resorted to many statistical methods such as arithmetic means the sta

... Show More
View Publication Preview PDF
Crossref
Publication Date
Tue Feb 12 2019
Journal Name
Iraqi Journal Of Physics
Effect of Pb dopant On A.C mechanism of ZnS thin films
...Show More Authors

Vacuum evaporation technique was used to prepare pure and doped ZnS:Pb thin films at10% atomic weight of Pb element onto glass substrates at room temperature for 200 nm thickness. Effect of doping on a.c electrical properties such as, a.c conductivity, real, and imaginary parts of dielectric constant within frequency range (10 KHz - 10 MHz) are measured. The frequency dependence of a.c conductivity is matched with correlated barrier hoping especially at higher frequency. Effect of doping on behavior of a.c mechanism within temperature range 298-473 K was studied.

View Publication Preview PDF
Crossref
Publication Date
Wed Jan 01 2025
Journal Name
Scripta Medica
Effect of perinatal outcomes on the stage of primary dentition eruption
...Show More Authors

Background/Aim: Understanding how perinatal outcome variations affect dentition eruption can lead to healthcare providers monitoring and managing dental health in infants and children. This study aimed to evaluate the influence of gestational age, mode of delivery and birth weight on the stage of primary dentition eruption in children. Methods: A sample of 304 children aged 6-24 months from Baghdad City was studied. Information about gestational age, delivery method (vaginal vs Caesarean) and birth weight were evaluated through a parent-answered sheet. The stage of dental eruption was estimated based on the criteria established by Damodar P Swami. Statistical and descriptive analyses were utilised to compare the dental eruption stag

... Show More
View Publication Preview PDF
Scopus Crossref
Publication Date
Fri Jun 01 2018
Journal Name
Journal Of Engineering
Evaluation of Traffic Performance of Ahmed Urabi Square in Baghdad City
...Show More Authors

At present, smooth movement on the roads is a matter which is needed for each user. Many roads, especially in urban areas geometrically improved because of the number of vehicles increase from time to time.

In this research, Highway capacity software, HCS, 2000, will be adopted to determine the effectiveness of roundabout in terms of capacity of roundabout, delay and level of service of roundabout.

The results of the analysis indicated that the Ahmed Urabi roundabout operates under level of service F with an average control delay of 300 seconds per vehicle during the peak hours.

The through movements of Alkarrada- Aljadiriya direction (Major Direction) represent the heaviest traff

... Show More
View Publication Preview PDF
Crossref (7)
Crossref
Publication Date
Mon Nov 01 2021
Journal Name
Journal Of Engineering
Effect of Fly Ash on Some Properties of Reactive Powder Concrete
...Show More Authors

To achieve sustainability in the field of civil engineering, there has become a great interest in developing reactive powder concrete RPC through the use of environmentally friendly materials to reduce the release of CO2 gas produced from cement factories as well as contribute to the recycling of industrial wastes that have a great impact on environmental pollution.

In this study, reactive powder concrete was prepared using total binder content of 800 kg/m3, water to binder ratio (0.275), and micro steel fibers  1% by volume of concrete. The experimental program included replacing fly ash with (8, 12, 16) % by cement weight to find the optimal ratio, which achieved the best mechanical proper

... Show More
View Publication Preview PDF
Crossref (17)
Crossref
Publication Date
Sun Sep 01 2024
Journal Name
Gazi University Journal Of Science
Effect of Natural Bitumen on the Performance of Hot Asphalt Mixture‏
...Show More Authors

For over a century, the global consumption of asphalt binder in asphalt mixture production has been substantial. In the Heet region (west of Iraq), two distinct forms of natural asphalt (NA) deposits exist: rock asphalt and sulfur spring asphalt. This study focused on using NA sourced from sulfur springs. The aim was to investigate the potential of incorporating NA into local asphalt mixtures. To achieve this, NA was heated to 163°C for varying durations. After heat treatment, laboratory tests were conducted on NA. The findings suggest that by heating NA for 20 hours, it conforms to Iraqi specifications in terms of physical properties. Furthermore, compared to conventional petroleum asphalt, treated NA showed greater

... Show More
View Publication Preview PDF
Scopus (10)
Crossref (5)
Scopus Clarivate Crossref
Publication Date
Sun Mar 13 2011
Journal Name
Baghdad Science Journal
Effect of Manganese Chloride in Histological Testes of Male Albino Mice
...Show More Authors

The present study was conducted to determine the effect of Manganese on Histopathological changes in testes. Manganese Chloride was given to white mice with oral containing 150_200 and 250 mg/kg for periods of 15_30 and 45 days. The present study recorded the existence of histopathological symptoms in the testes, such as degeneration and necrosis in the tubules, congestion inside blood vessels and Edema in the interstitial tissue, as well as the appearance of giant cells inside the seminiferous tubules.

View Publication Preview PDF
Crossref
Publication Date
Sun Sep 01 2013
Journal Name
Journal Of Economics And Administrative Sciences
The reality of Taxation in Iraq and Aspect of it’s Development
...Show More Authors

This research is considered a simple attempt and effort which is it first and last target is to point at the procedures of the taxes account that aims to reduce the taxes from the persons and give free to the person who estimates the tax to practice what comes from the competent authorities to describe the person who estimates the tax and not an accountant who practice the accountant procedures which are imposed on him by the annual terms from higher administrations , So he can not evaluate   state of the person who pay the tax , and he might be dissatisfied with his job , because his role can’t  be activated from the general foundation taxes.

And so , this research includes four fields:-

... Show More
View Publication Preview PDF
Crossref