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
Mon Jan 01 2024
Journal Name
Journal Of Natural Science, Biology And Medicine
Effectiveness of Frenulum Subcutaneous Injection of Botox in the Treatment of Premature Ejaculation
...Show More Authors

Scopus (1)
Scopus
Publication Date
Thu Mar 30 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Effects of Different Concentrations of Melatonin on the Time-course of Nitrite–induced Oxidation of Hemoglobin: In vitro Study
...Show More Authors

         Melatonin is a potent scavenger of reactive oxygen species or free radicals like superoxide and hydroxyl radicals. The oxidation of hemoglobin to methemoglobin (meth-Hb) by oxidizing compounds has been widely studied. The present work was designed to evaluate the ability of different concentrations of melatonin to inhibit nitrite–induced oxidation of hemoglobin. Blood samples were obtained from apparently healthy individuals from which erythrocyte hemolysate was prepared. Different concentrations of melatonin (10-9-1.0 mg/ml) were incubated for 10 min with the hemolysate, then to the resultant mixture 1 ml of sodium nitrite (final concentration 0.6 mM) was added, and the

... Show More
View Publication Preview PDF
Crossref
Publication Date
Sun Sep 01 2013
Journal Name
Baghdad Science Journal
Derivative Zero - Crossing Spectrophotometry Of Binary Mixtures Of Acetyl Acetonates Of Micro – Amounts Of Mn (Ii) And Al (Iii).
...Show More Authors

New derivative molecular absorption spectrophotometric methods have been developed for the determination of Al (III) , Mn (II) , individually and binary mixtures . The aim of this model of study is to obtain analytical results characterized by adequate standard of analytical figures of merits through application of derivative Spectrophotometry (dnA/d?n). The two metals acetyl acetonates are chemically stable and are widely used as catalysts . Where Interferences are probable due to very close or nearby peaks or Summits, the Zero – Crossing derivative measurement technique is used to avoid interfering effects between two metals pairs.

View Publication Preview PDF
Crossref
Publication Date
Sun Mar 04 2018
Journal Name
Iraqi Journal Of Science
Effect of maternal exposure of silver nanoparticles on the histogenesis of cerebellum in post-implantation of albino rats embryos
...Show More Authors

View Publication
Scopus (3)
Crossref (1)
Scopus Crossref
Publication Date
Mon Jun 01 2015
Journal Name
Journal Of Economics And Administrative Sciences
Experience of Kurdistan province of Iraq in light of the development of economic and social indicators for sustainable development
...Show More Authors

Reflect the sustainable development of the interaction of three key elements are the economic component and the social component and the environmental component while focusing economic component to achieve economic growth and focuses social element to achieve social justice in the distribution of income and achieve prosperity, the environmental component related fields and including emphasizes the protection of the environment and to ensure the continuation and sustainability of resources physical, biological and form in which it believes the interaction required for development process real and effective and sustainable, and is considered the province of Kurdistan Iraq of important areas where the movement of developmental mount

... Show More
View Publication Preview PDF
Crossref
Publication Date
Thu Feb 13 2020
Journal Name
Energies
Impact of the Type of Fertilization and the Addition of Glycerol on the Quality of Spring Rape Straw Pellets
...Show More Authors

This paper presents an analysis of selected qualitative characteristics of pellets produced from rape straw obtained from cultivations subjected to different fertilization treatments and from mixtures of straw selected for testing with crude glycerol obtained as a by-product from biodiesel production. The assessment focused on the following qualities of the obtained pellets: Moisture content, mechanical durability, heating value and main elements, that is, carbon, hydrogen, nitrogen, sulphur, chlorine and oxygen. The obtained results indicated that the different treatment regimens applied in spring rape cultivations had a significant impact on the physicochemical qualities of the straw. In terms of the heating value, traditional fer

... Show More
View Publication
Scopus (14)
Crossref (12)
Scopus Clarivate Crossref
Publication Date
Sun Apr 02 2017
Journal Name
Journal Of Educational And Psychological Researches
Improving performance of the heads of academic departments at the University of Wasit in light of the administrative functions
...Show More Authors

            A field study aimed to improve  administrative performance of the Heads of Departments in Wasit University in light of the administrative functions, a questionnaire constructed was c of 38 items, as have been applied during the academic year 2014/2015 to a group of experts from the deans and assistants, professors and heads of departments using the Delphi method by two rounds the adoption rate of 90% and an agreement was numbered 30 experts and study reached important results have been analyzed and discussed according to fields of study, a planning, organization and direction.

View Publication Preview PDF
Publication Date
Fri Dec 01 2017
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
The impact of multiple sources of funding on the disclosure of cash flow and the activation of control procedures
...Show More Authors

The principle of an interview requires revenues to expenditures by linking the efforts and achievements and disclosure sufficient to result activity, in the case generate future benefits of a particular asset, this asset appears in the balance sheet to reflect with the rest of the accounting unit's assets on the strength of financial position In the absence of future benefits from the effort are so loaded effort on the result accounts that reflect the outcome of activity during a specific period if the month or be separated or fiscal year. 

The researcher reached the following conclusions:

 1- difficult to control the cash inflows and outflows as a result of the multiplicity of sources of funding.

2- wea

... Show More
View Publication
Crossref
Publication Date
Sun Mar 04 2018
Journal Name
Iraqi Journal Of Science
Effect of maternal exposure of silver nanoparticles on the histogenesis of cerebellum in post-implantation of albino rats embryos
...Show More Authors

The central nervous system is the most important system and is very sensitive to any accidental infection during ontogenesis; it includes brain and spinal cord. The cerebellum is the second largest part of the brain after cerebrum and it’s very sensitive to the abnormal changes during the embryological development. This study was designed to investigate the effect of the maternal exposure of selected concentrations of suspension of nanoparticles on the ontogenesis of the rat cerebellum after embryos implanted in uterus. A total of 60 female pregnant rats were divided in to three groups, each contains 20 females. Group1 (G1) was treated orally with 2mg/kg /body weight (b. wt) of suspension of silver nanoparticles (Ag NPs). While group 2 (G

... Show More
Preview PDF
Scopus (3)
Crossref (1)
Scopus Crossref
Publication Date
Sun Dec 01 2019
Journal Name
Journal Of Economics And Administrative Sciences
Organizational monitoring and reflex of suffacation of work . An opinions study of sample workers in manufacturing of Isphelt dohuk
...Show More Authors

The study aims to determine the organizational monitoring mechanism in target organization as well as knowing the suffocation of work. The study depends on a questionnaire as a tool of collecting data on distributed random sample involved (45) person from different   levels in manufacturing isphelt Dohuk. The study depends on some hypothesis, the most significant one is that there is not impact of organizational monitoring of suffocation especially on the target organization.

View Publication Preview PDF
Crossref