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
Thu Dec 13 2018
Journal Name
Iraqi National Journal Of Nursing Specialties
Evaluation of Adolescents' Quality of life in Hilla City
...Show More Authors

Objective(s): The present study describes the quality of life (QOL) among adolescents with age of (12-22) year old and identifies factors that may be associated with it. Methodology: A cross-sectional design is carried throughout to evaluate adolescents' quality of life in Hilla City for the period of September 2nd 2016 to November 6th 2016. The present study is conducted in different settings that include schools and colleges in Hilla City. A non-probability "purposive" sample of (144) participant is selected and comprised of (50%) males and (50%) females. An instrument is constructed for the intent of the st

... Show More
View Publication Preview PDF
Publication Date
Sun Sep 07 2008
Journal Name
Baghdad Science Journal
Measurements of The Spectroscopic Properties of Hydrogen Iodide Molecules
...Show More Authors

A calculation have been carried out for determination some of the spectroscopic properties of Hydrogen Iodide HI molecules such as, the intensity of the absorption spectrum as a function of the variation of the temperature ranging from 10 to 1000 K. This study shows that the populations and hence intensity of the molecule increased as the temperature increased. Another determination of the maximum rotational quantum number Jmax of N2 , CO , BrF AgCl and HI molecules has been carried out.

View Publication Preview PDF
Crossref (1)
Crossref
Publication Date
Tue Jul 17 2012
Journal Name
مجلة مركز بحوث التقنيات الاحيائية
Effecienty of Immobilization technique of Bacillus Sublilis Asperginase producer
...Show More Authors

Abstract Twenty Bacillus isolated were obtained from different sample food and water. Bacillus B1 isolated was the highest asparaginase producer, it was identified as a strain of B. subtilis. The highest production of asparaginase was observed when mineral salt medium containing 0.3% asparagen, pH 8 and incubated at 40°c for 24 hrs. B. subtilis B1 cells were immobilized by entrapment methods (calcium alginate and agar), and by adsorption on solid surface such as sawdust and cotton. The result showed that the immobilized cells by adsorption on sawdust was the best, the immobilized cell retained 88% of asparginase activity after 48h while free cell retained 65%. Cells immobilized by adsorption on sawdust was incubated at different temperatu

... Show More
Publication Date
Mon Feb 01 2021
Journal Name
Materials Science And Engineering
Effect of magnetic water on strength properties of concrete
...Show More Authors
Abstract<p>The research’s main goal is to investigate the effects of using magnetic water in concrete mixes with regard to various mechanical properties such as compressive, flexural, and splitting tensile strength. The concrete mix investigated was designed to attain a specified cylinder compressive strength (30 MPa), with mix proportions of 1:1.8:2.68 cement to sand to crushed aggregate. The cement content was about 380 kg/m<sup>3</sup>, with a w/c ratio equal to 0.54, sand content of about 685 kg/m3, and gravel content of about 1,020 kg/m3. Magnetic water was prepared via passing ordinary water throughout a magnetic field with a magnetic intensity of 9,000 Gauss. The strength test</p> ... Show More
Crossref (6)
Crossref
Publication Date
Wed Oct 07 2020
Journal Name
Indian Journal Of Forensic Medicine &amp; Toxicology
Biological Activity of Complexes of Some Amino Acid: Review
...Show More Authors

View Publication
Scopus (3)
Crossref (2)
Scopus Crossref
Publication Date
Sun Dec 25 2022
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis and Atimicrobial Evaluation of Deuterated Analogues of Metronidazole
...Show More Authors

The discovery of novel therapeutic molecules is always difficult, and there are a variety of methodologies that use the most diverse and innovative medicinal chemistry approaches. One such approach is the deuteration technique: Deuteration is the process of substituting deuterium for hydrogen in a molecule. When compared to the drug molecule, its deuterated analogues may retain the features of the original molecule and, in some cases, improve its pharmacological activity, with fewer side effects and lower toxicity. Metronidazole is a commonly used antibiotic to treat anaerobic bacterial infections, protozoal and microaerophilic bacterial infections. Met

... Show More
View Publication Preview PDF
Scopus (2)
Crossref (2)
Scopus Crossref
Publication Date
Wed Dec 15 2021
Journal Name
Journal Of Baghdad College Of Dentistry
Evaluation of Cytotoxicity and Biocompatibility of Ti2AlC in Rabbits
...Show More Authors

Background: The Titanium and its alloys are suitable for dental implant and medical applications. Biocompatibility of the materials is a major factor in determining the success of the implant and has a great impact on their rate of osseointegration. The aim of this study was to evaluate the biocompatibility and cytotoxicity of Ti2AlC in comparison to CPTi & Ti6Al7Nb in rabbits. Materials and Methods: 10 male New Zealand White rabbits, weighing (2-2.5 kg), aged (10-12 months) were used in this study. Cylindrical implants were prepared from the study materials (CPTi, Ti6Al7Nb and Ti2AlC) with (8mm) height and (3mm) diameter for the evaluation of tissue response and disc specimens were prepared with (6 mm) diameter and (2 mm) thickness for ev

... Show More
View Publication Preview PDF
Scopus (3)
Crossref (3)
Scopus Crossref
Publication Date
Tue Dec 01 2015
Journal Name
Journal Of Engineering
Operation of the Iraqi Part of Al-Huweizah Marsh
...Show More Authors

Al-Huweizah Marsh is considered as the largest in Iraq. This research aims to maintain thesustainability of Al-Huweizah Marsh under all circumstances and within the limits of the
available natural resources from the Iraqi side and the absence of feeding from the Iranian sidedue to the recent Iranian separation dike along the international boundaries within the marsh.
Twelve scenarios have been suggested as a first step to restore the whole marsh. But the
uncontrolled Iranian feeders and exiguity of their discharges recently, it was necessary to studyonly the northern part of the marsh as an alternative case to ensure reasonable amounts of waterfor the purpose of maintaining and restore the marsh. Hydrological routing model was

... Show More
View Publication Preview PDF
Publication Date
Fri Feb 08 2019
Journal Name
Journal Of The College Of Education For Women
The concept of citizenship - The study of the theory
...Show More Authors

With the growth of democratic thought in our country, widened the trading term
citizenship to the magnitude of the meanings of participation in political life, economic, social
and cultural rights, as the recipe ( citizen ) does not mean only affiliation to the homeland and
link him as a child , but is as such an actor in various fields has his being independent , and
own convictions and the right to freely express his views and personal choices and play a
positive role in public life . Do not correct the democratic structure of any state without the
manifestation of the spirit of citizenship in the relations of each individual citizen to state
institutions.
The current research aims to Pfhom definition of citizen

... Show More
View Publication Preview PDF
Publication Date
Wed Mar 10 2021
Journal Name
Baghdad Science Journal
Effects of ethanol on the hippocampus of rat Brain
...Show More Authors

ten albino male rates were orally treated daily 20% and 30% ethanol for 30 days treatment with 30%ethanol caused of hippocampuse of darckness google hospital patients

View Publication Preview PDF