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
Sun Mar 01 2009
Journal Name
Al-khwarizmi Engineering Journal
Investigation of Thermal Stress Distribution in Laser Spot Welding Process
...Show More Authors

The objective of this paper was to study the laser spot welding process of low carbon steel sheet. The investigations were based on analytical and finite element analyses. The analytical analysis was focused on a consistent set of equations representing interaction of the laser beam with materials. The numerical analysis based on 3-D finite element analysis of heat flow during laser spot welding taken into account the temperature dependence of the physical properties and latent heat of transformations using ANSYS code V.10.0 to simulate the laser welding process. The effect of laser operating parameters on the results of the temperature profile were studied in addition to the effect on thermal stresses  and dimensions of the laser w

... Show More
View Publication Preview PDF
Publication Date
Fri Mar 31 2017
Journal Name
Al-khwarizmi Engineering Journal
Mechanical Properties Investigation of Composite Material Under Different Parameters Variations
...Show More Authors

         The main objective of this research is to design and select a composite plate to be used in fabricating wing skins of light unman air vehicle (UAV). The mechanical properties, weight and cost are the basis criteria of this selection. The fiber volume fraction, fillers and type of fiber with three levels for each were considered to optimize the composite plate selection. Finite element method was used to investigate the stress distribution on the wing at cruise flight condition in addition to estimate the maximum stress. An experiments plan has been designed to get the data on the basis of Taguchi technique. The most effective parameters at the process to be find out by employing L9

... Show More
View Publication Preview PDF
Crossref
Publication Date
Wed Mar 29 2023
Journal Name
Journal Of Optics
Enhancement of photodetector biased of ZnO nanoparticles/poly-TPD organic material by PEDOT PSS layer
...Show More Authors

View Publication
Scopus (4)
Crossref (3)
Scopus Clarivate Crossref
Publication Date
Tue Dec 13 2011
Journal Name
Iraqi Journal Of Laser
Evaluation of Low Level Laser Therapy Using Diode Laser in Enhancement of Episiotomy Wound Healing
...Show More Authors

we studied the effect of low level laser therapy (LLLT) using diode laser with wavelength of (790-805) nm in promotion and enhancement of wound healing of episiotomy and to evaluate the analgesic effect of LLLT in reducing the pain sensation caused by the episiotomy wounds. Nineteen women with episiotomy wound were selected and divided into three groups; 1st group (group No.1: control group) given antibiotics without laser therapy, in the 2nd group (group No.2) the wounds were exposed to laser therapy (4 sessions, each session with energy density of 19.90 J /cm2 every other day ) and systemic antibiotics were prescribed for 1 week. In the 3rd group (group No.3) the wounds were exposed to laser therapy (4 sessions, the same as in the 2nd

... Show More
View Publication Preview PDF
Publication Date
Mon Feb 01 2021
Journal Name
Indonesian Journal Of Electrical Engineering And Computer Science
Evaluation of the stability enhancement of the conventional sliding mode controller using whale optimization algorithm
...Show More Authors

The proposed work is an attempt to investigate the stability of the nonlinear system by using a whale optimization algorithm as of one of the meta-heuristic optimization methods, and this investigation was conducted on a single inverted pendulum as a study model. The evaluation measures which were used in this article values of gain and sliding surface of the conventional sliding mode controller to illustrate the extent of the system`s stability. Furthermore, control action, the relationship between error and its derivative, desired, and actual position in addition to sliding response graphically showed the feasibility of the proposed solution. The attained results illustrated considerable improvement in the settling time and minimizing the

... Show More
View Publication Preview PDF
Scopus (5)
Scopus Crossref
Publication Date
Wed Dec 22 2021
Journal Name
Antibiotics
Classic vs. Novel Antibacterial Approaches for Eradicating Dental Biofilm as Adjunct to Periodontal Debridement: An Evidence-Based Overview
...Show More Authors

Periodontitis is a multifactorial chronic inflammatory disease that affects tooth-supporting soft/hard tissues of the dentition. The dental plaque biofilm is considered as a primary etiological factor in susceptible patients; however, other factors contribute to progression, such as diabetes and smoking. Current management utilizes mechanical biofilm removal as the gold standard of treatment. Antibacterial agents might be indicated in certain conditions as an adjunct to this mechanical approach. However, in view of the growing concern about bacterial resistance, alternative approaches have been investigated. Currently, a range of antimicrobial agents and protocols have been used in clinical management, but these remain largely non-v

... Show More
View Publication Preview PDF
Crossref (24)
Crossref
Publication Date
Sun Mar 01 2009
Journal Name
Baghdad Science Journal
Investigation of the Porosity of Certain Iraqi Clay Deposits by Mercury Porosimeter
...Show More Authors

Pore volume, pore diameter, and pore volume distribution of three of Iraqi natural clay deposites were measured using mercury intrusion porosimetry .The clays are white kaolin, colored kaolin, and bentonite .The results showed that the variation of the pore area of the clay deposites followed the following order :- Coloured Kaolin > White Kaolin > Bentonite While the pore volume may be arranged as in the following sequence:- White Kaolin > Coloured Kaolin >Bentonite Also , Bentonite exhibits the narrow range pore size distribution than the white and coloured kaolin.

View Publication Preview PDF
Crossref
Publication Date
Tue Jul 02 2019
Journal Name
Fibers
Experimental Investigation of the Behavior of Self-Form Segmental Concrete Masonry Arches
...Show More Authors

This research aims to introduce a new technique-off-site and self-form segmental concrete masonry arches fabrication, without the need of construction formwork or centering. The innovative construction method in the current study encompasses two construction materials forms the self-form masonry arches, wedge-shape plain concrete voussoirs, and carbon fiber-reinforced polymer (CFRP) composites. The employment of CFRP fabrics was for two main reasons: bonding the voussoirs and forming the masonry arches. In addition, CFRP proved to be efficient for strengthening the extrados of the arch rings under service loadings. An experimental test was conducted on four sophisticated masonry arch specimens. The research parameters were the Keystone thic

... Show More
View Publication Preview PDF
Scopus (15)
Crossref (10)
Scopus Clarivate Crossref
Publication Date
Mon Mar 01 2021
Journal Name
Iraqi Journal Of Physics
Investigation of Structural, Mechanical, Thermal and Optical Properties of Cu Doped TiO2
...Show More Authors

In this work, Pure and Cu: doped titanium dioxide nano-powder was prepared through a solid-state method. the dopant concentration [Cu/TiO2 in atomic percentage (wt%)] is derived from 0 to 7 wt.%. structural properties of the samples performed with XRD revealed all nanopowders are of titanium dioxide having polycrystalline nature. Physical and Morphological studies were conducted using a scanning electronic microscope SEM test instrument to confirm the grain size and texture. The other properties of samples were examined using an optical microscope, Lee's Disc, Shore D hardness instrument, Fourier-transform infrared spectroscopy (FTIR), and Energy-dispersive X-ray spectroscopy (EDX). Results showed that the thermal conductivity

... Show More
View Publication Preview PDF
Crossref (4)
Crossref
Publication Date
Thu May 18 2023
Journal Name
Journal Of Engineering
Theoritical and Experimental Investigation of the Dynamical Behaviour of Complex Configuration Rotors
...Show More Authors

The present work considers an alternative solution for a complex configuration of rotor discs by applying Galerkin Method. The theoretical model consists of elastic shaft carrying number of discs and supported on number of journal bearings. The equation of motion was discretized to finite degree of freedom in terms of the system generalized coordinates. The various effects of the dynamical forces and moments arising from the bearing, discs and shaft were included. Rayleigh beam model is used for analyzing the shaft while the discs are considered rigid . The validity and convergence of the present analysis was carefully checked by comparing with the Finite Element solution. An example of rotor consists of three different size discs and su

... Show More
View Publication Preview PDF
Crossref