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 Jun 09 2022
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Improvement of the Solubility and Dissolution Characteristics of Risperidone via Nanosuspension Formulations
...Show More Authors

Risperidone is an atypical antipsychotic drug that is used for treating schizophrenia, bipolar mania, and autism. Risperidone rebalances dopamine and serotonin to improve thinking, mood, and behavior by working on dopamine and serotonin α2receptor antagonism. Risperidone has poor solubility and high permeability through the intestine, so it belongs to Biopharmaceutical Classification System (BCS) class II exhibits poor oral biopharmaceutical properties.

 The aim of the present work was to improve solubility and dissolution of Risperidone by preparing nanosuspension using different stabilizers and different solvents‎ in a method known as solvent-antisolvent precipitation method.  Twenty-eight formulas were prepared

... Show More
View Publication Preview PDF
Scopus (4)
Crossref (2)
Scopus Crossref
Publication Date
Thu May 30 2019
Journal Name
لارك
Approaches to Lexicography in English and Arabic
...Show More Authors

Lexicography, the art and craft of dictionary-making, is as old as writing. Since its very early stages several thousands of years ago, it has helped to serve basically the every-day needs of written communication among individuals in communities speaking different languages or different varieties of the same language. Two general approaches are distinguished in the craft of dictionary-making: the semasiological and the onomasiological. The former is represented by usually-alphabetical dictionaries as such, i.e. their being inventories of the lexicon, while the latter is manifested in thesauruses. English and Arabic have made use of both approaches in the preparation of their dictionaries, each having a distinct aim ahead. Wit

... Show More
View Publication Preview PDF
Crossref
Publication Date
Sat Apr 01 2023
Journal Name
Fluid Phase Equilibria
Prediction of solubility of vitamins in the mixed solvents using equation of state
...Show More Authors

View Publication
Scopus (1)
Crossref (1)
Scopus Clarivate Crossref
Publication Date
Wed Oct 25 2023
Journal Name
2023 Ieee 8th International Conference On Engineering Technologies And Applied Sciences (icetas)
Vibration Characteristics of Perforated Plate using Experimental and Numerical Approaches
...Show More Authors

Vibration analysis plays a vital role in understanding and analyzing the behavior of the structure. Where, it can be utilized from this analysis in the design process of the structures in different engineering applications, check the quality and safety of the structure under different working conditions. This work presents experimental measurements and numerical solutions to an out of plane vibration of a rectangular plate with a circular hole. Free edges rectangular plates with different circular holes diameters were studied. The effects of hole location on the plate natural frequencies were also investigated. A finite element modeling (using ANSYS Software) has been used to analyze the vibration characteristics of the plates. A good agree

... Show More
View Publication
Scopus Crossref
Publication Date
Sat Oct 01 2022
Journal Name
Baghdad Science Journal
A Crime Data Analysis of Prediction Based on Classification Approaches
...Show More Authors

Crime is considered as an unlawful activity of all kinds and it is punished by law. Crimes have an impact on a society's quality of life and economic development. With a large rise in crime globally, there is a necessity to analyze crime data to bring down the rate of crime. This encourages the police and people to occupy the required measures and more effectively restricting the crimes. The purpose of this research is to develop predictive models that can aid in crime pattern analysis and thus support the Boston department's crime prevention efforts. The geographical location factor has been adopted in our model, and this is due to its being an influential factor in several situations, whether it is traveling to a specific area or livin

... Show More
View Publication Preview PDF
Scopus (9)
Crossref (5)
Scopus Clarivate Crossref
Publication Date
Sat Apr 01 2017
Journal Name
Al–bahith Al–a'alami
Analytical Approaches between New Media and Traditional Media
...Show More Authors

The research deals with an analytical approach between new media and traditional one in the light of the changes imposed by technology, which has been able to change a number of common concepts in the field of communication and media. The researcher tries to find an analytical explanation of the relationship between technology by being an influential factor in building the information society, which is the basis of new media, and the technical output that influenced the forms of social relations and linguistic construction as a human communication tool. The research deals with an analytical approach between new media and traditional one in the light of the changes imposed by technology, which has been able to change a number of comm

... Show More
View Publication Preview PDF
Crossref
Publication Date
Tue Dec 11 2018
Journal Name
Iraqi National Journal Of Nursing Specialties
Episiotomy preventing approaches among midwives in Kurdistan region
...Show More Authors

Objectives: This study aimed to findout approaches which used by midwives for avoiding episiotomy and assess their knowledge regarding complications of episiotomy in three main cities of Kurdistan region. Methodology: A cross-sectional study was conducted between 1st January and 15th April 2014 in the three biggest maternity teaching hospitals. The study population included all the midwives (n=53) working in delivery rooms. Data were collected through interview with midwives. Results: The Midwives stated the followings as complications of episiotomy: tear into the rectum muscle or rectum itself (52.8%), bleedi

... Show More
View Publication Preview PDF
Publication Date
Wed Nov 01 2017
Journal Name
Journal Of Economics And Administrative Sciences
" employees voices behaviors: Theoretical concepts and thinking approaches
...Show More Authors

The concept of employees voice has received a great deal of attention by researchers in the field of organizational behavior and human resources management especially in the last three decades of the twentieth century , this importance has deep ranges limits in terms of its discussion history, so it became a behavioral variable received a great attention and care in managerial and organizational studied and basic pillar in the success and excellence of organizations in maintaining its human resources, the research explain the concept and benefits of paying attention to the voice of employees in business organizations , and the theories interpreted to employees voicing and clearing the motivations behind employees voicing, and dis

... Show More
View Publication Preview PDF
Crossref
Publication Date
Mon Feb 27 2023
Journal Name
Applied Sciences
Comparison of ML/DL Approaches for Detecting DDoS Attacks in SDN
...Show More Authors

Software-defined networking (SDN) presents novel security and privacy risks, including distributed denial-of-service (DDoS) attacks. In response to these threats, machine learning (ML) and deep learning (DL) have emerged as effective approaches for quickly identifying and mitigating anomalies. To this end, this research employs various classification methods, including support vector machines (SVMs), K-nearest neighbors (KNNs), decision trees (DTs), multiple layer perceptron (MLP), and convolutional neural networks (CNNs), and compares their performance. CNN exhibits the highest train accuracy at 97.808%, yet the lowest prediction accuracy at 90.08%. In contrast, SVM demonstrates the highest prediction accuracy of 95.5%. As such, an

... Show More
View Publication
Scopus (35)
Crossref (33)
Scopus Clarivate Crossref
Publication Date
Tue Dec 01 2020
Journal Name
Baghdad Science Journal
Detection of Suicidal Ideation on Twitter using Machine Learning & Ensemble Approaches
...Show More Authors

Suicidal ideation is one of the most severe mental health issues faced by people all over the world. There are various risk factors involved that can lead to suicide. The most common & critical risk factors among them are depression, anxiety, social isolation and hopelessness. Early detection of these risk factors can help in preventing or reducing the number of suicides. Online social networking platforms like Twitter, Redditt and Facebook are becoming a new way for the people to express themselves freely without worrying about social stigma. This paper presents a methodology and experimentation using social media as a tool to analyse the suicidal ideation in a better way, thus helping in preventing the chances of being the victim o

... Show More
View Publication Preview PDF
Scopus (36)
Crossref (25)
Scopus Clarivate Crossref