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
Wed Mar 05 2025
Journal Name
Water, Air, & Soil Pollution
Adsorptive Performance of High Surface Area Date Palm Bunch Activated Carbon Towards Methyl Violet and Fuchsin Basic Dyes Removal: Thermochemical Activation And Statistical Optimization
...Show More Authors

Scopus (2)
Crossref (2)
Scopus Crossref
Publication Date
Mon Oct 11 2021
Journal Name
Nano Hybrids And Composites
Far Infrared Laser Detector Based on Multi-Walled Carbon Nanotubes and Blend of (Polyaniline - Polymethyl Methacrylate) Polymers with Methyl Blue Dye for Photoconductive Applications
...Show More Authors

Infrared photoconductive detectors working in the far-infrared region and room temperature were fabricated. The detectors were fabricated using three types of carbon nanotubes (CNTs); MWCNTs, COOH-MWCNTs, and short-MWCNTs. The carbon nontubes suspension is deposited by dip coating and drop–casting techniques to prepare thin films of CNTs. These films were deposited on porous silicon (PSi) substrates of n-type Si. The I-V characteristics and the figures of merit of the fabricated detectors were measured at a forward bias voltage of 3 and 5 volts as well as at dark and under illumination by IR radiation from a CO2 laser of 10.6 μm wavelengths and power of 2.2 W. The responsivity and figures of merit of the photoconductive detector

... Show More
View Publication
Crossref (1)
Clarivate Crossref
Publication Date
Wed Jan 01 2025
Journal Name
Open Veterinary Journal
<b>Molecular study of <i>Streptococcus equi</i> isolated from horses with strangles in Iraq</b>
...Show More Authors

Background: Strangles is a highly contagious equine respiratory disease caused by Streptococcus equi subsp. equi. It is a globally significant pathogen and one of the most common infectious agents in horses. In Iraq, no sequencing data on this pathogen are available, and only two molecular studies have been published to date. This study provides preliminary insights into strain diversity and provides a foundation for future large-scale investigations. Aim: This study aimed to investigate the molecular characteristics, identify SeM gene alleles, and perform a phylogenetic analysis of S. equi isolates from horses in Baghdad, Iraq. Methods: We analyzed 59 Streptococcus spp. isolates previously obtained from equine clinical sample

... Show More
View Publication Preview PDF
Scopus Clarivate Crossref
Publication Date
Wed Nov 01 2017
Journal Name
Journal Of Economics And Administrative Sciences
Building marketing culture and reflection on the mental image Search for a pilot sample of managers in the General Company for Vegetable Oil Industry
...Show More Authors

          The subject of marketing culture and mental image is one of the important topics in the field of management. There is no study that combines these two variables. The research is important because of the increasing importance of the subject. The future direction of the company in question will support the company's economic and marketing responsibilities. And reflect the company's mental image, as a culture that contributes to changing the reality of the organization investigated by polling the views of a sample of managers in the General Company for Vegetable Oil Industry, which (30) out of the (65) individual, and There are two hypotheses of research: There is a significant

... Show More
View Publication Preview PDF
Crossref
Publication Date
Tue Jun 20 2023
Journal Name
Baghdad Science Journal
Study the Chemical Bonding of Heterometallic Trinuclear Cluster Containing Cobalt and Ruthenium: [(Cp*Co) (CpRu)2 (μ3-H) (μ-H)3] using QTAIM Approach
...Show More Authors

 

The topological parameters of the metal-metal and metal-ligand bonding interactions in a trinuclear tetrahydrido cluster [(Cp*Co) (CpRu)2 (μ3-H) (μ-H)3]1 (Cp* = η5 -C5Me4Et), (Cp = η5 -C5Me5), was explored by using the Quantum Theory of Atoms-in-Molecules (QTAIM). The properties of bond critical points such as the bond delocalization indices δ (A, B), the electron density ρ(r), the local kinetic energy density G(r), the Laplacian of the electron density ∇2ρ(r), the local energy density H(r), the local potential energy density V(r) and ellipticity ε(r) are compared with data from earlier organometallic system studies. A comparison of the topological processes of different atom-atom interactions has become possible than

... Show More
View Publication Preview PDF
Scopus (3)
Crossref (3)
Scopus Crossref
Publication Date
Tue Oct 01 2013
Journal Name
Journal Of Economics And Administrative Sciences
Analysis of the causal relationship between the gross fixed capital formation and gross domestic product for the agricultural sector for the period 1980 -2010
...Show More Authors

Despite Iraq's possession of the energies material, human and agricultural resources and great economic but that contribution of the agricultural sector in the total gross fixed capital formation and gross domestic product in the Iraqi economy remained low and declining continuously since the nineties of the last century, as well as the inability of agricultural production to meet the country's needs of food . The food gap increased strategic food crops until it reached 1049 thousand tons in 2010. On this basis, there is a need to study and analysis the behavior of the function of  gross fixed capital format

... Show More
View Publication Preview PDF
Crossref (3)
Crossref
Publication Date
Tue Dec 01 2020
Journal Name
Journal Of Economics And Administrative Sciences
Deposit insurance system and its role in financial security for the period (2010-2018) Study the experiences of Selected countries with reference to Iraq
...Show More Authors

Founding a System to secure deposits and protecting the depositors is considered one of the important and exchanged subjects out there in the banking system/field in Iraq at the current time, and the reason behind the exchange and spread of this subject is due to the financial crisis of which the banking sector is suffering from and the stumbling of many banks, those factors have had led to the insecurity of the depositors and their mistrust towards banks, thus, it is necessary to create a system to secure deposits in which depositors would be compensated for the losses caused by the banks' failures. in addition, it could be a countermeasure system which maintains the banking stability, protects the rights of depositors and gains

... Show More
View Publication Preview PDF
Crossref (1)
Crossref
Publication Date
Sun Dec 27 2020
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Isolation, Structural Characterization and Identification of Major Constituents in Ephedra foliata Naturally Growing in Iraq by TLC, GC-MS and UPLC-ESI-MS/MS
...Show More Authors

Abstract:

   The aerial part of Ephedra foliata Family Ephedraceae have long been used in traditional medicine and now Ephedra species have medicinal, ecological, and commercial value. The variety of pharmacological actions of this plant is due to its chemical constituents. Ephedrine and
related alkaloids; are the newly potential medicinal value of Ephedra supplements for weight loss or performance improvement. Other pharmacological actions like antibacterial and antifungal effects of the phenolic acid compounds, the immunosuppressive action of the polysaccharides, and the antitumor action of flavonoids. The genus of this plant wildly distributed t

... Show More
View Publication Preview PDF
Scopus (4)
Crossref (2)
Scopus Crossref
Publication Date
Thu Feb 01 2018
Journal Name
Journal Of Economics And Administrative Sciences
Equity financing within the framework the signal theory and its reflection on prices of stocks avarege: an empirical study in the Iraq stock exchange
...Show More Authors

 Since there is no market for bond issuance by companies in the Iraqi market and the difficulty of borrowing, companies must resort to proprietary financing to finance their investments. However, in the framework of the literature of financial management, the type of financing used by the company sends signals to investors and therefore reflected on the market value. Therefore, the problem of the study revolves around the variables of the study (Equity financing within the framework the signal theory, price of common stock in the Iraqi market).     

The study aims to verify the impact of the capital increase through the issuance of new stock on the price of

... Show More
View Publication Preview PDF
Crossref
Publication Date
Thu Oct 12 2017
Journal Name
Iraqi Journal Of Laser
A Comparative Evaluation of Post-Operative Pain and Function after Gingival Depigmentation Using 940 Nm Diode Laser And Conventional Bur Method: 6 Months Study
...Show More Authors

The aim of the study was to evaluate the efficacy of diode laser (λ=940 nm) in the management of gingival hyperpigmentation compared to the conventional bur method. Materials and methods: Eighteen patients with gingival hyperpigmentation were selected for the study with an age between 12-37 years old. The site of treatment was the upper gingiva using diode laser for the right half and the conventional method for the left half. All patients were re-evaluated after the following intervals: 3 days, 7 days, 1 month and 6 months post-operation. Pain and functions were re-evaluated in each visit for a period of 1 day, 3 days and 1 week post-operation. Laser parameters included 1.5 W in continuous mode with an initiated tip (400 μm) placed in

... Show More
View Publication Preview PDF