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 Jul 28 2018
Journal Name
Journal Of Engineering
Experimental Investigation for the Removal of Toxic Gases from Vehicle Exhaust using Non-Thermal Plasma
...Show More Authors

In this study, the use of non-thermal plasma theory to remove toxic gases emitted from a vehicle was experimentally investigated. A non-thermal plasma reactor was constructed in the form of a cylindrical tube made of Pyrex glass. Two stainless steel rods were placed inside the tube to generate electric discharge and plasma condition, by connecting with a high voltage power supply (up to 40 kV). The reactor was used to remove the contaminants of a 1.25-liter 4-cylinder engine at ambient conditions. Several tests have been carried out for a ranging speed from 750 to 4,500 rpm of the engine and varying voltages from 0 to 32 kV. The gases entering the reactor were examined by a gas analyzer and the gases concentration ratio

... Show More
View Publication Preview PDF
Crossref (4)
Crossref
Publication Date
Fri Jan 01 2021
Journal Name
Journal Of Engineering
A Computational Fluid Dynamics Investigation of using Large-Scale Geometric Roughness Elements in Open Channels
...Show More Authors

The hydraulic behavior of the flow can be changed by using large-scale geometric roughness elements in open channels. This change can help in controlling erosions and sedimentations along the mainstream of the channel. Roughness elements can be large stone or concrete blocks placed at the channel's bed to impose more resistance in the bed. The geometry of the roughness elements, numbers used, and configuration are parameters that can affect the flow's hydraulic characteristics. In this paper, velocity distribution along the flume was theoretically investigated using a series of tests of T-shape roughness elements, fixed height, arranged in three different configurations, differ in the number of lines of roughness element

... Show More
View Publication Preview PDF
Crossref (3)
Crossref
Publication Date
Thu Nov 01 2018
Journal Name
Journal Of Biological Sciences
Investigation of Plasmid-Associated Fluoroquinolone Resistance in Nosocomial Pseudomonas aeruginosa Isolated from Infected Burn Wounds
...Show More Authors

View Publication
Scopus (5)
Crossref (1)
Scopus Crossref
Publication Date
Sat Dec 01 2018
Journal Name
Al-khwarizmi Engineering Journal
Investigation of Load and Pressure Distribution on Wing with Wake Rollup for Low Speed Aircraft
...Show More Authors

The presented work shows a preliminary analytic method for estimation of load and pressure distributions on low speed wings with flow separation and wake rollup phenomena’s. A higher order vortex panel method is coupled with the numerical lifting line theory by means of iterative procedure including models of separation and wake rollup. The computer programs are written in FORTRAN which are stable and efficient.

      The capability of the present method is investigated through a number of test cases with different types of wing sections (NACA 0012 and GA(W)-1) for different aspect ratios and angles of attack, the results include the lift and drag curves, lift and pressure distributions along the wing s

... Show More
View Publication Preview PDF
Publication Date
Thu Sep 01 2022
Journal Name
Journal Of Engineering
Experimental Investigation of Crack Initiation and Growth in Concrete Slabs Placed Directly on Clayey Soil
...Show More Authors

The main objective of this study is to examine the impact of moisture concrete of clayey soil on the concrete slabs placed directly over it. This experimental study presents the mechanical properties of the concrete slab when placed on different clayey soil moisture content ranging from 0% to the optimum moisture content of 35%. The tests were performed on soil concrete specimens of 25*30*50 mm exposed to sprayed water curing conditions for 28 days. Tests of compressive strength, ultrasonic pulse velocity, crack depth and crack width were investigated through this paper. An ejection relationship between compressive strength of concrete and water content in the soil was observed, with a 26% increase with water increasing from 0% to 35%. T

... Show More
View Publication Preview PDF
Crossref
Publication Date
Sat Jan 01 2022
Journal Name
The 2nd Universitas Lampung International Conference On Science, Technology, And Environment (ulicoste) 2021
Investigation of the vibrational spectral and electronic properties for ZnxBe7-xO7 wurtzoid via DFT approximation
...Show More Authors

View Publication
Scopus (1)
Scopus Crossref
Publication Date
Fri Sep 30 2011
Journal Name
Al-khwarizmi Engineering Journal
Steady State Performance Investigation of a Three Phase Induction Motor Running Off Unbalanced Supply Voltages
...Show More Authors

The objective of this work is to investigate the performance of a conventional three phase induction motor supplied by unbalanced voltages. An effort to study the motor steady state performance under this disturbance is introduced. Using per phase equivalent circuit analysis with the concept of symmetrical components approach, the steady state performance is theoretically calculated. Also, a model for the induction motor with the MATLAB/Simulink SPS tools has been implemented and steady state results were obtained. Both results are compared and show good correlation as well. The simulation model is introduced to support and enhance electrical engineers with a complete understanding for the steady state performance of a fully loaded induc

... Show More
View Publication Preview PDF
Publication Date
Mon Jan 02 2017
Journal Name
Al-nahrain Journal For Engineering Sciences (njes)
Experimental Investigation of Forced Convection Heat Transfer and Pressure Drop in Open Cell Aluminum Fins
...Show More Authors

Publication Date
Thu Apr 01 2021
Journal Name
International Journal Of Drug Delivery Technology
Phytochemical investigation of some chemical compounds present in vicia villosa l. Widely grown in Iraq
...Show More Authors

Scopus
Publication Date
Fri Sep 01 2023
Journal Name
Advancements In Life Sciences
Investigation of pathogenic Streptococci species in local and imported mozzarella soft cheese in Baghdad city
...Show More Authors

Background: The present work investigated the profile and biodiversity of the pathogenic streptococci species isolated from local and imported mozzarella soft cheese in Baghdad City from October 2022 to January 2023. The study aimed to examine the molecular characterization of 16Sr RNA gene in some streptococcus species isolates from mozzarella soft cheese in Baghdad city Methods: From 50 samples, 8 isolates in all were found and identified based on the VITEK, molecular, and sequencing of the 16SrRNA gene. The eight isolates represented Lactococcus cremoris. Streptococcus alactolyticus, Streptococcus sanguinis, and Streptococcus thoraltensis. The isolates were subjected to conventional PCR and electrophoresis to detect the 16SrRNA gene usi

... Show More
View Publication Preview PDF
Scopus (2)
Scopus