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
Fri Dec 29 2017
Journal Name
Al-khwarizmi Engineering Journal
Design And Implementation of Microcontroller Based Curing Light Control of Dental System.
...Show More Authors

In this paper, a microcontroller-based electronic circuit have been designed and implemented for dental curing system using 8-bit MCS-51 microcontroller. Also a new control card is designed while considering advantages of microcontroller systems the time of curing was controlled automatically by preset values which were input from a push-button switch. An ignition based on PWM technique was used to reduce the high starting current needed for the halogen lamp. This paper and through the test result will show a good performance of the proposed system.

 

 

View Publication Preview PDF
Publication Date
Fri Mar 03 2017
Journal Name
Chalcogenide Letters
INFLUENCE OF HEAT TREATMENT ON SOME PHYSICAL PROPERTIES OF Zn0.9Sn0.1S THIN FILMS
...Show More Authors

Publication Date
Mon Jul 15 2019
Journal Name
Journal Of Pharmaceutical And Biological Sciences
Analysis of genome variation in Simple sequence repeat (SSR) of meningococcal isolates
...Show More Authors

Alteration of repeat tract length within the SSR of phase variable genes may enhance the persistence of isolates within their host for a long time (a period of months) (Alamro et al.,2014). Alamro et al. (2014) showed there was trend towards selection for OFF state or low expression for five phase variable genes (opc, hmbr, nadA, nalP, hpuAB) in three carriers (V54, V124 and V64) within strains belonging into CC174 and CC167 in first, second and third time points. He concluded that the selection for low or OFF state helped N. meningitidis to persist for a long time (Alamro et al., 2014). The current study aimed to detect the alteration in the repeat tracts of the same five variable genes within the previous three carriers (V54, V124, and V6

... Show More
View Publication
Crossref
Publication Date
Wed Jun 19 2019
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
Efficient of Government Organization to attain the Ten Recommendation of social Responsibility
...Show More Authors

   In this study, the researcher aimed to define and measure the relevance and effect of the governmental organizations in complying with Iraqi Ministry of Transportation's requirements towards achieving the social responsibility, embodied in the ten commandments of the United Nations Findings displayed the availability of realization regarding organization managers towards social responsibility with their various capabilities and tendencies in relation with the representing entries of those Ten Commandments.The study showed the relation between the effectiveness of those organizations and dimensions of the ten commandments of social responsibility, with the existence of a significant effect for the said effectiveness on achiev

... Show More
View Publication Preview PDF
Crossref
Publication Date
Wed Mar 01 2017
Journal Name
Photodiagnosis And Photodynamic Therapy
Photodynamic therapy in the management of actinic keratosis: Retrospective evaluation of outcome
...Show More Authors

View Publication Preview PDF
Scopus (20)
Crossref (18)
Scopus Clarivate Crossref
Publication Date
Mon Mar 08 2021
Journal Name
Baghdad Science Journal
Determination of the neutron refleetion coefficient as a function of reflector material
...Show More Authors

This work presents a simple method for determination of the neutron reflection coefficient (n) as a function of different neutron reflector materials.A laboratory neutron source (Am-Be) with activity of 16 ci is employed with a (BF3) neutron detector. Am-BeThree types of reflector materials are used as samples, the thickness of each sample is (5cm).It is found that( ?7) is: -For polyethlyene = 0.818

View Publication Preview PDF
Publication Date
Sun Feb 10 2019
Journal Name
Journal Of The College Of Education For Women
The hydrological regime of the Tigris River in the city of Baghdad
...Show More Authors

Water drainage pattern in the rivers and changed the nature of the renewed feeding areas
in the basin in terms of topographic and geological conditions and climate in addition to the
human role in organizing the process flow within these basins. This study addressed the
development of the Tigris River Hydrological in the city of Baghdad and found that the
annual rate of water drainage in the Tigris River was driven down very significantly,
especially in the past twenty years, and since 1996 up to 2014 record flow rates of less than
the overall rate of discharge of water, a (950 m3 / s ), in addition to the quarterly decrease the
discharge rates, especially since the beginning of the year 2000 and took converge all fo

... Show More
View Publication Preview PDF
Publication Date
Sun Mar 01 2020
Journal Name
Journal Of Engineering
Performance Evaluation of Trickling Filter and Extended Aeration of Wastewater Treatment Plants
...Show More Authors

In recent decades, there has been increasing interest in wastewater treatment because of its direct impact on the environment and public health. Over time, other forms of treatment have been developed and modified, including extended aeration. This process is included in the suspended growth system. In this paper, a comparative study was conducted between the efficiency of the extended aeration plant and that of the trickling filter plant in removal of BOD and COD.  The method of comparison was done by knowing the value of the pollutant before and after the treatment and then extract the removal ratio of each pollutant within each plant. The results showed that the percentage of removal of BOD in the trickling filte

... Show More
View Publication Preview PDF
Crossref (2)
Crossref
Publication Date
Mon Oct 01 2012
Journal Name
Iraqi Journal Of Physics
Influence of substrate temperature on structural and optical properties of SnO2 films
...Show More Authors

Tin Oxide (SnO2) films have been deposited by spray pyrolysis technique at different substrate temperatures. The effects of substrate temperature on the structural, optical and electrical properties of SnO2 films have been investigated. The XRD result shows a polycrystalline structure for SnO2 films at substrate temperature of 673K. The thickness of the deposited film was of the order of 200 nm measured by Toulansky method. The energy gap increases from 2.58eV to 3.59 eV when substrate temperature increases from 473K to 673K .Electrical conductivity is 4.8*10-7(.cm)-1 for sample deposited at 473K while it increases to 8.7*10-3 when the film is deposited at 673K

View Publication Preview PDF
Publication Date
Tue Sep 01 2020
Journal Name
Iraqi Journal Of Physics
Enhancment of the corrosion resistance of copper metal by laser surface treatment
...Show More Authors

In this work, the copper metal was treated using Nd:YAG laser with energy 1Joul to enhance corrosion resistance and improve surface properties. The copper metal has many applications in industry as well as water, oil and gas pipes. The same conditions, (laser power density, scan speed, distance between paths, medium gas-air) were applied in the laser surface treatment, After laser treatment, the samples microstructures were investigated using optical microscope (OM) to examine micro structural changes due to laser irradiation. Specimen surfaces were investigated using atomic force microscopy (AFM), X-ray diffraction (XRD), macro hardness, and corrosion test before and after laser treatment to

... Show More
View Publication Preview PDF
Crossref (5)
Crossref