Search results for: drug administration
Commenced in January 2007
Frequency: Monthly
Edition: International
Paper Count: 3145

Search results for: drug administration

2335 Molecular Mechanism on Inflammation and Antioxidant Role of Pterocarpus Marsupiumin in Experimental Hyperglycaemia

Authors: Leelavinothan Pari , Ayyasamy Rathinam

Abstract:

Diabetes mellitus (DM) is a major and growing public health problem throughout the world. Pterocarpus marsupium (Roxb.) (Family: Fabaceae) is widely used as a traditional medicine to treat various diseases including diabetes. However, the molecular mechanism of Pterocarpus marsupium has not been investigated so far. Two fractions (2.5% and 5%) of extract from the medicinal plant, Pterocarpus marsupium (PME) were conducted in a dose dependent manner in streptozotocin (45 mg/kg b.w.) induced type 2 diabetic rats. Each fraction of PME was administered to diabetic rats intragastrically at a dose of 50, 100 and 200 mg/kg b.w for 45 days. The effective dose 200 mg/kg b.w of 5% fraction was more pronounced in reducing the levels of blood glucose (95.65 mg/dL) and glycosylated hemoglobin (HbA1c) (0.41 mg/g Hb), and increasing the plasma insulin (16.20 µU/mL) level. Moreover, PME (200 mg/kg b.w) significantly ameliorated lipid peroxidation products (thiobarbituric reactive substances, lipid hydroperoxides) enzymatic (superoxide dismutase, catalase and glutathione peroxidase) and non-enzymatic antioxidants (Vitamin C, Vitamin E and reduced glutathione) levels. The altered activities of the key enzymes of lipid metabolism along with the lipid profile in diabetic rats were significantly reverted to near normal levels by the administration of PME 5% 200 mg/kg b.w fraction. PME (200 mg/kg b.w) has the ability to reduce the inflammatory cytokines, such as TNF-α, IL-6 mRNA, as well as protein expression and apoptotic marker, such as caspase-3 enzyme in diabetic hepatic tissue. The above biochemical findings were also supported by histological studies such as improvement in pancreas and liver. Pterocarpus marsupium could effectively reduce the hyperglycemia, oxidative-stress, inflammation and hyperlipedimea in diabetic rats; hence it could be a useful drug in the management of diabetes without any side effects.

Keywords: diabetes mellitus, streptozotocin, Pterocarpus marsupium, lipid peroxidation, Antioxidants, inflammatory cytokines

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2334 Comparative in silico and in vitro Study of N-(1-Methyl-2-Oxo-2-N-Methyl Anilino-Ethyl) Benzene Sulfonamide and Its Analogues as an Anticancer Agent

Authors: Pamita Awasthi, Kirna, Shilpa Dogra, Manu Vatsal, Ritu Barthwal

Abstract:

Doxorubicin, also known as adriamycin, is an anthracycline class of drug used in cancer chemotherapy. It is used in the treatment of non-Hodgkin’s lymphoma, multiple myeloma, acute leukemias, breast cancer, lung cancer, endometrium cancer and ovary cancers. It functions via intercalating DNA and ultimately killing cancer cells. The major side effects of doxorubicin are hair loss, myelosuppression, nausea & vomiting, oesophagitis, diarrhoea, heart damage and liver dysfunction. The minor modifications in the structure of compound exhibit large variation in the biological activity, has prompted us to carry out the synthesis of sulfonamide derivatives. Sulfonamide is an important feature with broad spectrum of biological activity such as antiviral, antifungal, diuretics, anti-inflammatory, antibacterial and anticancer activities. Structure of the synthesized compound N-(1-methyl-2-oxo-2-N-methyl anilino-ethyl)benzene sulfonamide confirmed by proton nuclear magnetic resonance (1H NMR),13C NMR, Mass and FTIR spectroscopic tools to assure the position of all protons and hence stereochemistry of the molecule. Further we have reported the binding potential of synthesized sulfonamide analogues in comparison to doxorubicin drug using Auto Dock 4.2 software. Computational binding energy (B.E.) and inhibitory constant (Ki) has been evaluated for the synthesized compound in comparison of doxorubicin against Poly (dA-dT).Poly (dA-dT) and Poly (dG-dC).Poly (dG-dC) sequences. The in vitro cytotoxic study against human breast cancer cell lines confirms the better anticancer activity of the synthesized compound over currently in use anticancer drug doxorubicin. The IC50 value of the synthesized compound is 7.12 µM where as for doxorubicin is 7.2 µ.

Keywords: Doxorubicin, auto dock, in silco, in vitro

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2333 A Study Concerning Foreign Worker Migration in Thailand

Authors: Napatsorn Suput-Anyaporn

Abstract:

This paper aimed to investigate multilateral relationships across the factors which included labor shortage, trade union, turnover rate of employee, labor law and regulation, and effectiveness of foreign worker administration in the scope of foreign workers in the industrial manufacturing sector of Thailand. The research employed both quantitative and qualitative approaches, in which foreign workers from Myanmar, Laos and Cambodia in the industrial manufacturing sector in selected areas of Thailand were sampled for the quantitative data collection, and persons in the chief executive management and the supervisor levels, and persons in the academic area in relation with foreign workers were selected as the sample for the qualitative data collection method. Thus, a questionnaire, in-depth interview and focus group were utilized as tools in this research paper. The discussion placed an emphasis on the fact that Thailand should design more effective law and regulations for the foreign workers administration and management in response to preparing for the coming ASEAN Economic Community with the declaration of the free- flow labor movement policy.

Keywords: industrial manufacturing sector, labor law and regulation, labor shortage, migrant worker, trade union, turnover rate of employee

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2332 A Machine Learning-Based Model to Screen Antituberculosis Compound Targeted against LprG Lipoprotein of Mycobacterium tuberculosis

Authors: Syed Asif Hassan, Syed Atif Hassan

Abstract:

Multidrug-resistant Tuberculosis (MDR-TB) is an infection caused by the resistant strains of Mycobacterium tuberculosis that do not respond either to isoniazid or rifampicin, which are the most important anti-TB drugs. The increase in the occurrence of a drug-resistance strain of MTB calls for an intensive search of novel target-based therapeutics. In this context LprG (Rv1411c) a lipoprotein from MTB plays a pivotal role in the immune evasion of Mtb leading to survival and propagation of the bacterium within the host cell. Therefore, a machine learning method will be developed for generating a computational model that could predict for a potential anti LprG activity of the novel antituberculosis compound. The present study will utilize dataset from PubChem database maintained by National Center for Biotechnology Information (NCBI). The dataset involves compounds screened against MTB were categorized as active and inactive based upon PubChem activity score. PowerMV, a molecular descriptor generator, and visualization tool will be used to generate the 2D molecular descriptors for the actives and inactive compounds present in the dataset. The 2D molecular descriptors generated from PowerMV will be used as features. We feed these features into three different classifiers, namely, random forest, a deep neural network, and a recurring neural network, to build separate predictive models and choosing the best performing model based on the accuracy of predicting novel antituberculosis compound with an anti LprG activity. Additionally, the efficacy of predicted active compounds will be screened using SMARTS filter to choose molecule with drug-like features.

Keywords: antituberculosis drug, classifier, machine learning, molecular descriptors, prediction

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2331 Optimization of the Administration of Intravenous Medication by Reduction of the Residual Volume, Taking User-Friendliness, Cost Efficiency, and Safety into Account

Authors: A. Poukens, I. Sluyts, A. Krings, J. Swartenbroekx, D. Geeroms, J. Poukens

Abstract:

Introduction and Objectives: It has been known for many years that with the administration of intravenous medication, a rather significant part of the planned to be administered infusion solution, the residual volume ( the volume that remains in the IV line and or infusion bag), does not reach the patient and is wasted. This could possibly result in under dosage and diminished therapeutic effect. Despite the important impact on the patient, the reduction of residual volume lacks attention. An optimized and clearly stated protocol concerning the reduction of residual volume in an IV line is necessary for each hospital. As described in my Master’s thesis, acquiring the degree of Master in Hospital Pharmacy, administration of intravenous medication can be optimized by reduction of the residual volume. Herewith effectiveness, user-friendliness, cost efficiency and safety were taken into account. Material and Methods: By usage of a literature study and an online questionnaire sent out to all Flemish hospitals and hospitals in the Netherlands (province Limburg), current flush methods could be mapped out. In laboratory research, possible flush methods aiming to reduce the residual volume were measured. Furthermore, a self-developed experimental method to reduce the residual volume was added to the study. The current flush methods and the self-developed experimental method were compared to each other based on cost efficiency, user-friendliness and safety. Results: There is a major difference between the Flemish and the hospitals in the Netherlands (Province Limburg) concerning the approach and method of flushing IV lines after administration of intravenous medication. The residual volumes were measured and laboratory research showed that if flushing was done minimally 1-time equivalent to the residual volume, 95 percent of glucose would be flushed through. Based on the comparison, it became clear that flushing by use of a pre-filled syringe would be the most cost-efficient, user-friendly and safest method. According to laboratory research, the self-developed experimental method is feasible and has the advantage that the remaining fraction of the medication can be administered to the patient in unchanged concentration without dilution. Furthermore, this technique can be applied regardless of the level of the residual volume. Conclusion and Recommendations: It is recommendable to revise the current infusion systems and flushing methods in most hospitals. Aside from education of the hospital staff and alignment on a uniform substantiated protocol, an optimized and clear policy on the reduction of residual volume is necessary for each hospital. It is recommended to flush all IV lines with rinsing fluid with at least the equivalent volume of the residual volume. Further laboratory and clinical research for the self-developed experimental method are needed before this method can be implemented clinically in a broader setting.

Keywords: intravenous medication, infusion therapy, IV flushing, residual volume

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2330 The Jurisprudential Evolution of Corruption Offenses in Spain: Before and after the Economic Crisis

Authors: Marta Fernandez Cabrera

Abstract:

The period of economic boom generated by the housing bubble created a climate of social indifference to the problem of corruption. This resulted in the persecution and conviction for these criminal offenses being low. After the economic recession, social awareness about the problem of corruption has increased. This has led to the Spanish citizenship requiring the public authorities to try to end the problem in the most effective way possible. In order to respond to the continuous social demands that require an exemplary punishment, the legislator has made changes in crimes against the public administration in the Spanish Criminal Code. However, from the point of view of criminal law, the social change has not served to modify only the law, but also the jurisprudence. After the recession, judges are punishing more severely these conducts than in the past. Before the crisis, it was usual for criminal judges to divert relevant behavior to other areas of the legal system such as administrative law and acquit in the criminal field. Criminal judges have considered that administrative law already has mechanisms that can effectively deal with this type of behavior in order to respect the principle of subsidiarity or ultima ratio. It has also been usual for criminal judges to acquit civil servants due to the absence of requirements unrelated to the applicable offense. For example, they have required an economic damage to the public administration when the offense in the criminal code does not require it. Nevertheless, for some years, these arguments have either partially disappeared or considerably transformed. Since 2010, a jurisprudential stream has been consolidated that aims to provide a more severe response to corruption than it had received until now. This change of opinion, together with greater prosecution of these behaviors by judges and prosecutors, has led to a significant increase in the number of individuals convicted of corruption crimes. This paper has two objectives. The first one is to show that even though judges apply the law impartially, they are flexible to social changes. The second one is to identify the erroneous arguments the courts have used up until now. To carry out the present paper, it has been done a detailed analysis of the judgments of the supreme court before and after the year 2010. Therefore, the jurisprudential analysis is complemented with the statistical data on corruption available.

Keywords: corruption, public administration, social perception, ultima ratio principle

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2329 Identifying Reforms Required in Construction Contracts from Resolved Disputed Cases

Authors: K. C. Iyer, Yogita Manan Bindal, Sumit Kumar Bakshi

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The construction industry is plagued with disputes and litigation in India with many stalled projects seeking dispute resolution. This has an adverse effect on the performance and overall project delivery and impacts future investments within the industry. While construction industry is the major driver of growth, there has not been major reforms in the government construction contracts. The study is aimed at identifying the proactive means of dispute avoidance, focusing on reforms required within the construction contracts, by studying 49 arbitration awards of construction disputes. The claims presented in the awards are aggregated to study the causes linked to the contract document and are referred against the prospective recommendation and practices as surveyed from literature review of research papers. Within contract administration, record keeping has been a major concern as they are required by the parties to substantiate the claims or the counterclaims and therefore are essential in any dispute redressal process. The study also observes that the right judgment is inhibited when the record keeping is improper and due to lack of coherence between documents, the dispute resolution period is also prolonged. The finding of the research will be relevant to industry practitioners in contract drafting with a view to avoid disputes.

Keywords: construction contract, contract administration, contract management, dispute avoidance

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2328 Iron-Metal-Organic Frameworks: Potential Application as Theranostics for Inhalable Therapy of Tuberculosis

Authors: Gabriela Wyszogrodzka, Przemyslaw Dorozynski, Barbara Gil, Maciej Strzempek, Bartosz Marszalek, Piotr Kulinowski, Wladyslaw Piotr Weglarz, Elzbieta Menaszek

Abstract:

MOFs (Metal-Organic Frameworks) belong to a new group of porous materials with a hybrid organic-inorganic construction. Their structure is a network consisting of metal cations or clusters (acting as metallic centers, nodes) and the organic linkers between nodes. The interest in MOFs is primarily associated with the use of their well-developed surface and large porous. Possibility to build MOFs of biocompatible components let to use them as potential drug carriers. Furthermore, forming MOFs structure from cations possessing paramagnetic properties (e.g. iron cations) allows to use them as MRI (Magnetic Resonance Imaging) contrast agents. The concept of formation of particles that combine the ability to transfer active substance with imaging properties has been called theranostic (from words combination therapy and diagnostics). By building MOF structure from iron cations it is possible to use them as theranostic agents and monitoring the distribution of the active substance after administration in real time. In the study iron-MOF: Fe-MIL-101-NH2 was chosen, consisting of iron cluster in nodes of the structure and amino-terephthalic acid as a linker. The aim of the study was to investigate the possibility of applying Fe-MIL-101-NH2 as inhalable theranostic particulate system for the first-line anti-tuberculosis antibiotic – isoniazid. The drug content incorporated into Fe-MIL-101-NH2 was evaluated by dissolution study using spectrophotometric method. Results showed isoniazid encapsulation efficiency – ca. 12.5% wt. Possibility of Fe-MIL-101-NH2 application as the MRI contrast agent was demonstrated by magnetic resonance tomography. FeMIL-101-NH2 effectively shortening T1 and T2 relaxation times (increasing R1 and R2 relaxation rates) linearly with the concentrations of suspended material. Images obtained using multi-echo magnetic resonance imaging sequence revealed possibility to use FeMIL-101-NH2 as positive and negative contrasts depending on applied repetition time. MOFs micronization via ultrasound was evaluated by XRD, nitrogen adsorption, FTIR, SEM imaging and did not influence their crystal shape and size. Ultrasonication let to break the aggregates and achieve very homogeneously looking SEM images. MOFs cytotoxicity was evaluated in in vitro test with a highly sensitive resazurin based reagent PrestoBlue™ on L929 fibroblast cell line. After 24h no inhibition of cell proliferation was observed. All results proved potential possibility of application of ironMOFs as an isoniazid carrier and as MRI contrast agent in inhalatory treatment of tuberculosis. Acknowledgments: Authors gratefully acknowledge the National Science Center Poland for providing financial support, grant no 2014/15/B/ST5/04498.

Keywords: imaging agents, metal-organic frameworks, theranostics, tuberculosis

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2327 Formulation and Evaluation of Glimepiride (GMP)-Solid Nanodispersion and Nanodispersed Tablets

Authors: Ahmed. Abdel Bary, Omneya. Khowessah, Mojahed. al-jamrah

Abstract:

Introduction: The major challenge with the design of oral dosage forms lies with their poor bioavailability. The most frequent causes of low oral bioavailability are attributed to poor solubility and low permeability. The aim of this study was to develop solid nanodispersed tablet formulation of Glimepiride for the enhancement of the solubility and bioavailability. Methodology: Solid nanodispersions of Glimepiride (GMP) were prepared using two different ratios of 2 different carriers, namely; PEG6000, pluronic F127, and by adopting two different techniques, namely; solvent evaporation technique and fusion technique. A full factorial design of 2 3 was adopted to investigate the influence of formulation variables on the prepared nanodispersion properties. The best chosen formula of nanodispersed powder was formulated into tablets by direct compression. The Differential Scanning Calorimetry (DSC) analysis and Fourier Transform Infra-Red (FTIR) analysis were conducted for the thermal behavior and surface structure characterization, respectively. The zeta potential and particle size analysis of the prepared glimepiride nanodispersions was determined. The prepared solid nanodispersions and solid nanodispersed tablets of GMP were evaluated in terms of pre-compression and post-compression parameters, respectively. Results: The DSC and FTIR studies revealed that there was no interaction between GMP and all the excipients used. Based on the resulted values of different pre-compression parameters, the prepared solid nanodispersions powder blends showed poor to excellent flow properties. The resulted values of the other evaluated pre-compression parameters of the prepared solid nanodispersion were within the limits of pharmacopoeia. The drug content of the prepared nanodispersions ranged from 89.6 ± 0.3 % to 99.9± 0.5% with particle size ranged from 111.5 nm to 492.3 nm and the resulted zeta potential (ζ ) values of the prepared GMP-solid nanodispersion formulae (F1-F8) ranged from -8.28±3.62 mV to -78±11.4 mV. The in-vitro dissolution studies of the prepared solid nanodispersed tablets of GMP concluded that GMP- pluronic F127 combinations (F8), exhibited the best extent of drug release, compared to other formulations, and to the marketed product. One way ANOVA for the percent of drug released from the prepared GMP-nanodispersion formulae (F1- F8) after 20 and 60 minutes showed significant differences between the percent of drug released from different GMP-nanodispersed tablet formulae (F1- F8), (P<0.05). Conclusion: Preparation of glimepiride as nanodispersed particles proven to be a promising tool for enhancing the poor solubility of glimepiride.

Keywords: glimepiride, solid Nanodispersion, nanodispersed tablets, poorly water soluble drugs

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2326 Data Security and Privacy Challenges in Cloud Computing

Authors: Amir Rashid

Abstract:

Cloud Computing frameworks empower organizations to cut expenses by outsourcing computation resources on-request. As of now, customers of Cloud service providers have no methods for confirming the privacy and ownership of their information and data. To address this issue we propose the platform of a trusted cloud computing program (TCCP). TCCP empowers Infrastructure as a Service (IaaS) suppliers, for example, Amazon EC2 to give a shout box execution condition that ensures secret execution of visitor virtual machines. Also, it permits clients to bear witness to the IaaS supplier and decide if the administration is secure before they dispatch their virtual machines. This paper proposes a Trusted Cloud Computing Platform (TCCP) for guaranteeing the privacy and trustworthiness of computed data that are outsourced to IaaS service providers. The TCCP gives the deliberation of a shut box execution condition for a client's VM, ensuring that no cloud supplier's authorized manager can examine or mess up with its data. Furthermore, before launching the VM, the TCCP permits a client to dependably and remotely acknowledge that the provider at backend is running a confided in TCCP. This capacity extends the verification of whole administration, and hence permits a client to confirm the data operation in secure mode.

Keywords: cloud security, IaaS, cloud data privacy and integrity, hybrid cloud

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2325 Governance and Public Policy: The Perception of Civil Society Participation in Brazil and South Africa

Authors: Paulino V. Tavares, Ana L. Romao

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Public governance, in general, is essential to qualify and educate, pedagogically, the decision-making process of the government in relation to the management of resources and the provision of public services, with transparency and active participation of individuals and citizens for the development of a more democratic environment, besides stimulating control and social empowerment, aiming at the development of the collectivity. In this context, the participation of society in the elaboration, execution, and control of public policies is prominent to strengthen public governance itself. With this, using a multidimensional approach with the application of two questionnaires to a universe of twenty Counselors of the Courts of Auditors (Brazil), twenty professionals of public administration (Brazil), twenty Government/Provincial Counselors (South Africa), and twenty South African professionals of public administration, the preliminary results indicate that the participation of civil society, for both countries, is very low in the elaboration, execution, and control of public policies. At the same time, about 70% of the answers obtained indicate, on average, three possible paths to increase the participation of civil society. With this, it is delineated that developing new horizons to strengthen both public policies how social participation is necessary, but, for both, it is important that governments and civil society, in their respective countries, have an awareness of the effective importance of this interaction.

Keywords: Brazil, civil society, participation, South Africa

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2324 When Messages Cause Distraction from Advertising: An Eye-Tracking Study

Authors: Nilamadhab Mohanty

Abstract:

It is essential to use message formats that make communication understandable and correct. It is because; the information format can influence consumer decision on the purchase of a product. This study combines information from qualitative inquiry, media trend analysis, eye tracking experiment, and questionnaire data to examine the impact of specific message format and consumer perceived risk on attention to the information and risk retention. We investigated the influence of message framing (goal framing, attribute framing, and mix framing) on consumer memory, study time, and decisional uncertainty while deciding on the purchase of drugs. Furthermore, we explored the impact of consumer perceived risk (associated with the use of the drug, i.e., RISK-AB and perceived risk associated with the non-use of the drug, i.e., RISK-EB) on message format preference. The study used eye-tracking methods to understand the differences in message processing. Findings of the study suggest that the message format influences information processing, and participants' risk perception impacts message format preference. Eye tracking can be used to understand the format differences and design effective advertisements.

Keywords: message framing, consumer perceived risk, advertising, eye tracking

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2323 Jail Reentry in Rural America: A Quasi-Experimental Examination of a Rural Behavioral Health Reentry Program

Authors: Debra L. Stanley, Gabriela Wasileski

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Offenders face many challenges as they transition from being incarcerated to the community, ranging from housing and employment needs to long standing problems with addictions and mental health issues. A lack of appropriate behavioral health services in the more remote parts of the United States has led to a significant illegal substance abuse problem, housing instability, and unaddressed mental health and trauma issues. High rates of poverty and unemployment exacerbate the growing behavioral health issues, drug overdoses, co-occurring disorders, and crime that are so prevalent across rural communities. This study examines the challenges of rural jail reentry faced by offenders in a treatment capacity. The client-centered evidence-based program is uniquely designed to provide continuity of care that focuses on issues which affect rural communities. Prior to release from jail, individuals go through comprehensive assessment screenings to measure mental health and substance use disorder as well as trauma and prior crime victimization histories; the assessments help to target client-specific services. The quasi-experimental research design tracks clients throughout their recovery and reintegration into the community. Individuals in a rural program often do not have the benefit of easy access or peer mentoring that is so often found in urban recovery programs. Therefore, much of the support is provided through telehealth and e-services. The goal of this study is to explore the nature of rural reentry programs and measures of recidivism, drug overdoses, and other behavioral health needs and successful reentry to include stable housing and employment.

Keywords: jail reentry, rehabilitation, behavioral health, drug abuse, recidivism

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2322 The Suitability of Agile Practices in Healthcare Industry with Regard to Healthcare Regulations

Authors: Mahmood Alsaadi, Alexei Lisitsa

Abstract:

Nowadays, medical devices rely completely on software whether as whole software or as embedded software, therefore, the organization that develops medical device software can benefit from adopting agile practices. Using agile practices in healthcare software development industries would bring benefits such as producing a product of a high-quality with low cost and in short period. However, medical device software development companies faced challenges in adopting agile practices. These due to the gaps that exist between agile practices and the requirements of healthcare regulations such as documentation, traceability, and formality. This research paper will conduct a study to investigate the adoption rate of agile practice in medical device software development, and they will extract and outline the requirements of healthcare regulations such as Food and Drug Administration (FDA), Health Insurance Portability and Accountability Act (HIPAA), and Medical Device Directive (MDD) that affect directly or indirectly on software development life cycle. Moreover, this research paper will evaluate the suitability of using agile practices in healthcare industries by analyzing the most popular agile practices such as eXtream Programming (XP), Scrum, and Feature-Driven Development (FDD) from healthcare industry point of view and in comparison with the requirements of healthcare regulations. Finally, the authors propose an agile mixture model that consists of different practices from different agile methods. As result, the adoption rate of agile practices in healthcare industries still low and agile practices should enhance with regard to requirements of the healthcare regulations in order to be used in healthcare software development organizations. Therefore, the proposed agile mixture model may assist in minimizing the gaps existing between healthcare regulations and agile practices and increase the adoption rate in the healthcare industry. As this research paper part of the ongoing project, an evaluation of agile mixture model will be conducted in the near future.

Keywords: adoption of agile, agile gaps, agile mixture model, agile practices, healthcare regulations

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2321 Biogenic Amines Production during RAS Cheese Ripening

Authors: Amr Amer

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Cheeses are among those high-protein-containing foodstuffs in which enzymatic and microbial activities cause the formation of biogenic amines from amino acids decarboxylation. The amount of biogenic amines in cheese may act as a useful indicator of the hygienic quality of the product. In other words, their presence in cheese is related to its spoilage and safety. Formation of biogenic amines during Ras cheese (Egyptian hard cheese) ripening was investigated for 4 months. Three batches of Ras cheese were manufactured using Egyptian traditional method. From each batch, Samples were collected at 1, 7, 15, 30, 60, 90 and 120 days after cheese manufacture. The concentrations of biogenic amines (Tyramine, Histamine, Cadaverine and Tryptamine) were analyzed by high performance liquid chromatography (HPLC). There was a significant increased (P<0.05) in Tyramine levels from 4.34± 0.07 mg|100g in the first day of storage till reached 88.77± 0.14 mg|100g at a 120-day of storage. Also, Histamine and Cadaverine levels had the same increased pattern of Tyramine reaching 64.94± 0.10 and 28.28± 0.08 mg|100g in a 120- day of storage, respectively. While, there was a fluctuation in the concentration of Tryptamine level during ripening period as it decreased from 3.24± 0.06 to 2.66± 0.11 mg|100g at 60-day of storage then reached 5.38±0.08 mg|100g in a 120- day of storage. Biogenic amines can be formed in cheese during production and storage: many variables, as pH, salt concentration, bacterial activity as well as moisture, storage temperature and ripening time, play a relevant role in their formation. Comparing the obtained results with the recommended standard by Food and Drug Administration "FDA" (2001), High levels of biogenic amines in various Ras cheeses consumed in Egypt exceeded the permissible value (10 mg%) which seemed to pose a threat to public health. In this study, presence of high concentrations of biogenic amines (Tyramine, Histamine, cadaverine and Tryptamine) in Egyptian Ras cheeses reflects the bad hygienic conditions under which they produced and stored. Accordingly, the levels of biogenic amines in different cheeses should be come in accordance with the safe permissible limit recommended by FDA to ensure human safety.

Keywords: Ras cheese, biogenic amines, tyramine, histamine, cadaverine

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2320 Inhibition of 3-Deoxy-D-Arabino-Heptulosonate 7-Phosphate Synthase from Mycobacterium Tuberculosis Using High Throughput Virtual Screening and Molecular Dynamics Studies

Authors: Christy Rosaline, Rathankar Roa, Waheeta Hopper

Abstract:

Persistence of tuberculosis, emergence of multidrug-resistance and extensively drug-resistant forms of the disease, has increased the interest in developing new antitubercular drugs. Developing inhibitors for 3-deoxy-D-arabino-heptulosonate 7-phosphate synthase from Mycobacterium tuberculosis (MtbDAH7Ps), an enzyme involved in shikimate pathway, gives a selective target for antitubercular agents. MtbDAH7Ps was screened against ZINC database, and shortlisted compounds were subjected to induce fit docking. Prime/Molecular Mechanics Generalized Born Surface Area calculation was used to validate the binding energy of ligand-protein complex. Molecular Dynamics analysis for of the lead compounds–MtbDAH7Ps complexes showed that the backbone of MtbDAH7Ps in their complexes were stable. These results suggest that the shortlisted lead compounds ZINC04097114, ZINC15163225, ZINC16857013, ZINC06275603, and ZINC05331260 could be developed into novel drug leads to inhibit DAH7Ps in Mycobacterium tuberculosis.

Keywords: MtbDAH7Ps, Mycobacterium tuberculosis, HTVS, molecular dynamics

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2319 Free Radical Scavenging Activity and Total Phenolic Assessment of Drug Repurposed Medicinal Plant Metabolites: Promising Tools against Post COVID-19 Syndromes and Non-Communicable Diseases in Botswana

Authors: D. Motlhanka, M. Mine, T. Bagaketse, T. Ngakane

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There is a plethora of evidence from numerous sources that highlights the triumph of naturally derived medicinal plant metabolites with antioxidant capability for repurposed therapeutics. As post-COVID-19 syndromes and non-communicable diseases are on the rise, there is an urgent need to come up with new therapeutic strategies to address the problem. Non-communicable diseases and Post COVID-19 syndromes are classified as socio-economic diseases and are ranked high among threats to health security due to the economic burden they pose to any government budget commitment. Research has shown a strong link between accumulation of free radicals and oxidative stress critical for pathogenesis of non-communicable diseases and COVID-19 syndromes. Botswana has embarked on a robust programme derived from ethno-pharmacognosy and drug repurposing to address these threats to health security. In the current approach, a number of medicinally active plant-derived polyphenolics are repurposed and combined into new medicinal tools to target diabetes, Hypertension, Prostate Cancer and oxidative stress induced Post COVID 19 syndromes such as “brain fog”. All four formulants demonstrated Free Radical scavenging capacities above 95% at 200µg/ml using the diphenylpicryalhydrazyl free radical scavenging assay and the total phenolic contents between 6899-15000GAE(g/L) using the folin-ciocalteau assay respectively. These repurposed medicinal tools offer new hope and potential in the fight against emerging health threats driven by hyper-inflammation and free radical-induced oxidative stress.

Keywords: drug repurposed plant polyphenolics, free radical damage, non-communicable diseases, post COVID 19 syndromes

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2318 Synthesis of PVA/γ-Fe2O3 Used in Cancer Treatment by Hyperthermia

Authors: Sajjad Seifi Mofarah, S. K. Sadrnezhaad, Shokooh Moghadam, Javad Tavakoli

Abstract:

In recent years a new method of combination treatment for cancer has been developed and studied that has led to significant advancements in the field of cancer therapy. Hyperthermia is a traditional therapy that, along with a creation of a medically approved level of heat with the help of an alternating magnetic AC current, results in the destruction of cancer cells by heat. This paper gives details regarding the production of the spherical nanocomposite PVA/γ-Fe2O3 in order to be used for medical purposes such as tumor treatment by hyperthermia. To reach a suitable and evenly distributed temperature, the nanocomposite with core-shell morphology and spherical form within a 100 to 200 nanometer size was created using phase separation emulsion, in which the magnetic nano-particles γ-Fe2O3 with an average particle size of 20 nano-meters and with different percentages of 0.2, 0.4, 0.5, and 0.6 were covered by polyvinyl alcohol. The main concern in hyperthermia and heat treatment is achieving desirable specific absorption rate (SAR) and one of the most critical factors in SAR is particle size. In this project all attempts has been done to reach minimal size and consequently maximum SAR. The morphological analysis of the spherical structure of the nanocomposite PVA/γ-Fe2O3 was achieved by SEM analyses and the study of the chemical bonds created was made possible by FTIR analysis. To investigate the manner of magnetic nanocomposite particle size distribution a DLS experiment was conducted. Moreover, to determine the magnetic behavior of the γ-Fe2O3 particle and the nanocomposite PVA/γ-Fe2O3 in different concentrations a VSM test was conducted. To sum up, creating magnetic nanocomposites with a spherical morphology that would be employed for drug loading opens doors to new approaches in developing nanocomposites that provide efficient heat and a controlled release of drug simultaneously inside the magnetic field, which are among their positive characteristics that could significantly improve the recovery process in patients.

Keywords: nanocomposite, hyperthermia, cancer therapy, drug releasing

Procedia PDF Downloads 289
2317 Liposome Loaded Polysaccharide Based Hydrogels: Promising Delayed Release Biomaterials

Authors: J. Desbrieres, M. Popa, C. Peptu, S. Bacaita

Abstract:

Because of their favorable properties (non-toxicity, biodegradability, mucoadhesivity etc.), polysaccharides were studied as biomaterials and as pharmaceutical excipients in drug formulations. These formulations may be produced in a wide variety of forms including hydrogels, hydrogel based particles (or capsules), films etc. In these formulations, the polysaccharide based materials are able to provide local delivery of loaded therapeutic agents but their delivery can be rapid and not easily time-controllable due to, particularly, the burst effect. This leads to a loss in drug efficiency and lifetime. To overcome the consequences of burst effect, systems involving liposomes incorporated into polysaccharide hydrogels may appear as a promising material in tissue engineering, regenerative medicine and drug loading systems. Liposomes are spherical self-closed structures, composed of curved lipid bilayers, which enclose part of the surrounding solvent into their structure. The simplicity of production, their biocompatibility, the size and similar composition of cells, the possibility of size adjustment for specific applications, the ability of hydrophilic or/and hydrophobic drug loading make them a revolutionary tool in nanomedicine and biomedical domain. Drug delivery systems were developed as hydrogels containing chitosan or carboxymethylcellulose (CMC) as polysaccharides and gelatin (GEL) as polypeptide, and phosphatidylcholine or phosphatidylcholine/cholesterol liposomes able to accurately control this delivery, without any burst effect. Hydrogels based on CMC were covalently crosslinked using glutaraldehyde, whereas chitosan based hydrogels were double crosslinked (ionically using sodium tripolyphosphate or sodium sulphate and covalently using glutaraldehyde). It has been proven that the liposome integrity is highly protected during the crosslinking procedure for the formation of the film network. Calcein was used as model active matter for delivery experiments. Multi-Lamellar vesicles (MLV) and Small Uni-Lamellar Vesicles (SUV) were prepared and compared. The liposomes are well distributed throughout the whole area of the film, and the vesicle distribution is equivalent (for both types of liposomes evaluated) on the film surface as well as deeper (100 microns) in the film matrix. An obvious decrease of the burst effect was observed in presence of liposomes as well as a uniform increase of calcein release that continues even at large time scales. Liposomes act as an extra barrier for calcein release. Systems containing MLVs release higher amounts of calcein compared to systems containing SUVs, although these liposomes are more stable in the matrix and diffuse with difficulty. This difference comes from the higher quantity of calcein present within the MLV in relation with their size. Modeling of release kinetics curves was performed and the release of hydrophilic drugs may be described by a multi-scale mechanism characterized by four distinct phases, each of them being characterized by a different kinetics model (Higuchi equation, Korsmeyer-Peppas model etc.). Knowledge of such models will be a very interesting tool for designing new formulations for tissue engineering, regenerative medicine and drug delivery systems.

Keywords: controlled and delayed release, hydrogels, liposomes, polysaccharides

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2316 Fabrication and Characterization of Folic Acid-Grafted-Thiomer Enveloped Liposomes for Enhanced Oral Bioavailability of Docetaxel

Authors: Farhan Sohail, Gul Shahnaz Irshad Hussain, Shoaib Sarwar, Ibrahim Javed, Zajif Hussain, Akhtar Nadhman

Abstract:

The present study was aimed to develop a hybrid nanocarrier (NC) system with enhanced membrane permeability, bioavailability and targeted delivery of Docetaxel (DTX) in breast cancer. Hybrid NC’s based on folic acid (FA) grafted thiolated chitosan (TCS) enveloped liposomes were prepared with DTX and evaluated in-vitro and in-vivo for their enhanced permeability and bioavailability. Physicochemical characterization of NC’s including particle size, morphology, zeta potential, FTIR, DSC, PXRD, encapsulation efficiency and drug release from NC’s was determined in vitro. Permeation enhancement and p-gp inhibition were performed through everted sac method on freshly excised rat intestine which indicated that permeation was enhanced 5 times as compared to pure DTX and the hybrid NC’s were strongly able to inhibit the p-gp activity as well. In-vitro cytotoxicity and tumor targeting was done using MDA-MB-231 cell line. The stability study of the formulations performed for 3 months showed the improved stability of FA-TCS enveloped liposomes in terms of its particles size, zeta potential and encapsulation efficiency as compared to TCS NP’s and liposomes. The pharmacokinetic study was performed in vivo using rabbits. The oral bioavailability and AUC0-96 was increased 10.07 folds with hybrid NC’s as compared to positive control. Half-life (t1/2) was increased 4 times (58.76 hrs) as compared to positive control (17.72 hrs). Conclusively, it is suggested that FA-TCS enveloped liposomes have strong potential to enhance permeability and bioavailability of hydrophobic drugs after oral administration and tumor targeting.

Keywords: docetaxel, coated liposome, permeation enhancement, oral bioavailability

Procedia PDF Downloads 399
2315 Quality by Design in the Optimization of a Fast HPLC Method for Quantification of Hydroxychloroquine Sulfate

Authors: Pedro J. Rolim-Neto, Leslie R. M. Ferraz, Fabiana L. A. Santos, Pablo A. Ferreira, Ricardo T. L. Maia-Jr., Magaly A. M. Lyra, Danilo A F. Fonte, Salvana P. M. Costa, Amanda C. Q. M. Vieira, Larissa A. Rolim

Abstract:

Initially developed as an antimalarial agent, hydroxychloroquine (HCQ) sulfate is often used as a slow-acting antirheumatic drug in the treatment of disorders of connective tissue. The United States Pharmacopeia (USP) 37 provides a reversed-phase HPLC method for quantification of HCQ. However, this method was not reproducible, producing asymmetric peaks in a long analysis time. The asymmetry of the peak may cause an incorrect calculation of the concentration of the sample. Furthermore, the analysis time is unacceptable, especially regarding the routine of a pharmaceutical industry. The aiming of this study was to develop a fast, easy and efficient method for quantification of HCQ sulfate by High Performance Liquid Chromatography (HPLC) based on the Quality by Design (QbD) methodology. This method was optimized in terms of peak symmetry using the surface area graphic as the Design of Experiments (DoE) and the tailing factor (TF) as an indicator to the Design Space (DS). The reference method used was that described at USP 37 to the quantification of the drug. For the optimized method, was proposed a 33 factorial design, based on the QbD concepts. The DS was created with the TF (in a range between 0.98 and 1.2) in order to demonstrate the ideal analytical conditions. Changes were made in the composition of the USP mobile-phase (USP-MP): USP-MP: Methanol (90:10 v/v, 80:20 v/v and 70:30 v/v), in the flow (0.8, 1.0 and 1.2 mL) and in the oven temperature (30, 35, and 40ºC). The USP method allowed the quantification of drug in a long time (40-50 minutes). In addition, the method uses a high flow rate (1,5 mL.min-1) which increases the consumption of expensive solvents HPLC grade. The main problem observed was the TF value (1,8) that would be accepted if the drug was not a racemic mixture, since the co-elution of the isomers can become an unreliable peak integration. Therefore, the optimization was suggested in order to reduce the analysis time, aiming a better peak resolution and TF. For the optimization method, by the analysis of the surface-response plot it was possible to confirm the ideal setting analytical condition: 45 °C, 0,8 mL.min-1 and 80:20 USP-MP: Methanol. The optimized HPLC method enabled the quantification of HCQ sulfate, with a peak of high resolution, showing a TF value of 1,17. This promotes good co-elution of isomers of the HCQ, ensuring an accurate quantification of the raw material as racemic mixture. This method also proved to be 18 times faster, approximately, compared to the reference method, using a lower flow rate, reducing even more the consumption of the solvents and, consequently, the analysis cost. Thus, an analytical method for the quantification of HCQ sulfate was optimized using QbD methodology. This method proved to be faster and more efficient than the USP method, regarding the retention time and, especially, the peak resolution. The higher resolution in the chromatogram peaks supports the implementation of the method for quantification of the drug as racemic mixture, not requiring the separation of isomers.

Keywords: analytical method, hydroxychloroquine sulfate, quality by design, surface area graphic

Procedia PDF Downloads 628
2314 Chitosan-Aluminum Monostearate Dispersion as Fabricating Liquid for Constructing Controlled Drug Release Matrix

Authors: Kotchamon Yodkhum, Thawatchai Phaechamud

Abstract:

Hydrophobic chitosan-based materials have been developed as controlled drug delivery system. This study was aimed to prepare and evaluate chitosan-aluminum monostearate composite dispersion (CLA) as fabricating liquid for construct a hydrophobic, controlled-release solid drug delivery matrix. This work was attempted to blend hydrophobic substance, aluminum monostearate (AMS), with chitosan in acidic aqueous medium without using any surfactants or grafting reaction, and high temperature during mixing that are normally performed when preparing hydrophobic chitosan system. Lactic acid solution (2%w/v) was employed as chitosan solvent. CLA dispersion was prepared by dispersing different amounts of AMS (1-20% w/w) in chitosan solution (4% w/w) with continuous agitation using magnetic stirrer for 24 h. Effect of AMS amount on physicochemical properties of the dispersion such as viscosity, rheology and particle size was evaluated. Morphology of chitosan-AMS complex (dispersant) was observed under inverted microscope and atomic force microscope. Stability of CLA dispersions was evaluated after preparation within 48 h. CLA dispersions containing AMS less than 5 % w/w exhibited rheological behavior as Newtonian while that containing higher AMS amount exhibited as pseudoplastic. Particle size of the dispersant was significantly smaller when AMS amount was increased up to 5% w/w and was not different between the higher AMS amount system. Morphology of the dispersant under inverted microscope displayed irregular shape and their size exhibited the same trend with particle size measurement. Observation of the dispersion stability revealed that phase separation occurred faster in the system containing higher AMS amount which indicated lower stability of the system. However, the dispersions were homogeneous and stable more than 12 hours after preparation that enough for fabrication process. The prepared dispersions had ability to be fabricated as a porous matrix via lyophilization technique.

Keywords: chitosan, aluminum monostearate, dispersion, controlled-release

Procedia PDF Downloads 379
2313 Effect of Oral Administration of "Gadagi" Tea on Activities of Some Antioxidant Enzymes in Rats

Authors: A. M. Gadanya, M. S. Sule

Abstract:

Effect of oral administration of Gadagi tea on some antioxidant enzymes was assessed in healthy male albino rats. The rats were grouped and administered with standard doses of the 3 types of Gadagi tea i.e. Sak, Sada and Magani for a period of four weeks. Animals that were not administered with the tea constituted the control group. At the end of fourth week, the animals were sacrificed and their serum superoxide dismutase (SOD), glutathione reductase (GR) and catalase (CAT) activities were determined. The activities of the enzymes were also determined in the brain, liver, kidney and intestine homogenates of the rats. Mean SOD activity in brain of rats orally administered with “sada” was found to be significantly higher (P < 0.05) than that of the control group. Mean CAT activity in the intestine of rats orally administered with “magani” was found to be significantly higher (P < 0.05) than that of the control group and the experimental groups of Sak and Sada at standard dose level. Thus, all the “Gadagi” tea preparations studied at standard dose level could stimulate antioxidant enzymes, especially SOD in brain and CAT in intestine (by Sada) and CAT in intestine (by Magani).

Keywords: “Gadagi” tea, superoxide dismutase, catalase, glutathione reductase

Procedia PDF Downloads 454
2312 QSAR and Anti-Depressant Studies of Some Novel Phenothiazine Derivatives

Authors: D. L. Tambe, S. Dighe Nachiket

Abstract:

Objective: Depression is a common but serious illness and the phenothiazine derivatives shows prominent effect against the depression hence work was undertaken to validate this use scientifically. Material and Methods: Synthesis of phenothiazine derivatives are done by the substitution of various groups, but the basic scheme of synthesis is started with synthesis of 4-(Cyclohexylidene) Benzoic acid using PABA. After that with the further six step of synthesis of 3-(10H-phenothiazin-2-yl)-N, 5-diphenyl-4H-1, 2, 4-triazol-4-amine is done which is final product. Antidepressant activity of all the synthesized compounds was evaluated by despair swim test by using Sprague Dawley Rats. Standard drug imipramine was used as the control. In the despair swim test, all the synthesized derivatives showed antidepressant activity. Results: Among the all phenothiazine derivatives four compounds (6.6-7.2 (14H –phenyl ), 9.43 (1H OH), 8.50 (1H NH phenothiazine),6.85-8.21(14H phenyl), 8.50 (1H NH phenothiazine), 11.82 (1H – OH), 6.6-7.2 (8H –phenyl ), 9.43 (1H OH), 8.50 (1H NH phenothiazine), 4.2 (1H NH) and 6.85-8.21(8H phenyl), 8.50 (1H NH phenothiazine), 3.9 (1H NH) 11.82 (1H – OH) showed significant antidepressant activity comparing with control drug imipramine. Conclusion: Various Novel phenothiazine derivatives show more potent antidepressant activity and it plays more beneficial role in human health for the treatment of depression.

Keywords: antidepressant activities, despair swim test, phenothiazine, Sprague Dawley Rats

Procedia PDF Downloads 372
2311 Directors’ Duties, Civil Liability, and the Business Judgment Rule under the Portuguese Legal Framework

Authors: Marisa Catarina da Conceição Dinis

Abstract:

The commercial companies’ management has suffered an important material and legal transformation in the last years, mainly related to the changes in the Portuguese legal framework and because of the fact they were recently object of great expansion. In fact, next to the smaller family businesses, whose management is regularly assumed by partners, companies with social investment highly scattered, whose owners are completely out from administration, are now arising. In those particular cases, the business transactions are much more complex and require from the companies’ managers a highly technical knowledge and some specific professionals’ skills and abilities. This kind of administration carries a high-level risk that can both result in great success or in great losses. Knowing that the administration performance can result in important losses to the companies, the Portuguese legislator has created a legal structure to impute them some responsibilities and sanctions. The main goal of this study is to analyze the Portuguese law and some jurisprudence about companies’ management rules and about the conflicts between the directors and the company. In order to achieve these purposes we have to consider, on the one hand, the legal duties directly connected to the directors’ functions and on the other hand the disrespect for those same rules. The Portuguese law in this matter, influenced by the common law, determines that the directors’ attitude should be guided by loyalty and honesty. Consequently, we must reflect in which cases the administrators should respond to losses that they might cause to companies as a result of their duties’ disrespect. In this way is necessary to study the business judgment rule wich is a rule that refers to a liability exclusion rule. We intend, in the same way, to evaluate if the civil liability that results from the directors’ duties disrespect can extend itself to those who have elected them ignoring or even knowing that they don´t have the necessary skills or appropriate knowledge to the position they hold. To charge directors’, without ruining entrepreneurship, charging, in the same way, those who select them reinforces the need for more responsible and cautious attitudes which will lead consequently to more confidence in the markets.

Keywords: business judgment rule, civil liability of directors, duty of care, duty of care, Portuguese legal framework

Procedia PDF Downloads 335
2310 Evaluation of in vitro Inhibitory Effect of Enoxacin on Babesia and Theileria Parasites

Authors: Mosaab A. Omar, Mohammad Saleh Al-Aboody, Mohmed A. Rizk, Shimaa M. Elsayed, Ahmed ElSify, Naoaki Yokoyama, Ikuo Igarashi

Abstract:

Enoxacin is a broad-spectrum 6-fluoronaphthyridinone antibacterial agent (fluoroquinolones) structurally related to nalidixic acid used mainly in the treatment of urinary tract infections and gonorrhea. Also, it has been shown recently that it may have cancer inhibiting effect. The primary antibabesial effect of Enoxacin is due to inhibition of DNA gyrase subunit A, and DNA topoisomerase. In the present study, enoxacin was tested as a potent inhibitor against the in vitro growth of bovine and equine Piroplasms. The in vitro growth of five Babesia species that were tested was significantly inhibited (P<0.05) by micromolar concentrations of enoxacin (IC50 values= 13.5, 7.2, 7.5, and 24.2 µM for Babesia bovis, Babesia bigemina, Babesia caballi, and Theileria equi, respectively). Enoxacin IC50 values for Babesia and Theileria parasites were satisfactory as the drug is a potent antibacterial drug with minimum side effects. Therefore, enoxacin might be used for the treatment of Babesiosis and Theileriosis especially in case of mixed infections with bacterial diseases or in the case of animal sensitivity against diminazin toxicity.

Keywords: enoxacin, Babesia, Theileria, IC50 and dimenazin

Procedia PDF Downloads 455
2309 Preparation, Solid State Characterization of Etraverine Co-Crystals with Improved Solubility for the Treatment of Human Immunodeficiency Virus

Authors: B. S. Muddukrishna, Karthik Aithal, Aravind Pai

Abstract:

Introduction: Preparation of binary cocrystals of Etraverine (ETR) by using Tartaric Acid (TAR) as a conformer was the main focus of this study. Etravirine is a Class IV drug, as per the BCS classification system. Methods: Cocrystals were prepared by slow evaporation technique. A mixture of total 500mg of ETR: TAR was weighed in molar ratios of 1:1 (371.72mg of ETR and 128.27mg of TAR). Saturated solution of Etravirine was prepared in Acetone: Methanol (50:50) mixture in which tartaric acid is dissolved by sonication and then this solution was stirred using a magnetic stirrer until the solvent got evaporated. Shimadzu FTIR – 8300 system was used to acquire the FTIR spectra of the cocrystals prepared. Shimadzu thermal analyzer was used to achieve DSC measurements. X-ray diffractometer was used to obtain the X-ray powder diffraction pattern. Shake flask method was used to determine the equilibrium dynamic solubility of pure, physical mixture and cocrystals of ETR. USP buffer (pH 6.8) containing 1% of Tween 80 was used as the medium. The pure, physical mixture and the optimized cocrystal of ETR were accurately weighed sufficient to maintain the sink condition and were filled in hard gelatine capsules (size 4). Electrolab-Tablet Dissolution tester using basket apparatus at a rotational speed of 50 rpm and USP phosphate buffer (900 mL, pH = 6.8, 37 ˚C) + 1% Tween80 as a media, was used to carry out dissolution. Shimadzu LC-10 series chromatographic system was used to perform the analysis with PDA detector. An Hypersil BDS C18 (150mm ×4.6 mm ×5 µm) column was used for separation with mobile phase comprising of a mixture of ace¬tonitrile and phosphate buffer 20mM, pH 3.2 in the ratio 60:40 v/v. The flow rate was 1.0mL/min and column temperature was set to 30°C. The detection was carried out at 304 nm for ETR. Results and discussions: The cocrystals were subjected to various solid state characterization and the results confirmed the formation of cocrystals. The C=O stretching vibration (1741cm-1) in tartaric acid was disappeared in the cocrystal and the peak broadening of primary amine indicates hydrogen bond formation. The difference in the melting point of cocrystals when compared to pure Etravirine (265 °C) indicates interaction between the drug and the coformer which proves that first ordered transformation i.e. melting endotherm has disappeared. The difference in 2θ values of pure drug and cocrystals indicates the interaction between the drug and the coformer. Dynamic solubility and dissolution studies were also conducted by shake flask method and USP apparatus one respectively and 3.6 fold increase in the dynamic solubility were observed and in-vitro dissolution study shows four fold increase in the solubility for the ETR: TAR (1:1) cocrystals. The ETR: TAR (1:1) cocrystals shows improved solubility and dissolution as compared to the pure drug which was clearly showed by solid state characterization and dissolution studies.

Keywords: dynamic solubility, Etraverine, in vitro dissolution, slurry method

Procedia PDF Downloads 333
2308 Effect of Endurance Exercise Training on Blood Pressure in Elderly Female Patients with Hypertension

Authors: Elham Ahmadi

Abstract:

This study is conducted with the aim of investigating the effect of moderate physical activity (60% of maximal heart rate-MHR) on blood pressure in an elderly female with hypertension. Hypertension is considered a modifiable risk factor for cardiovascular disease through physical activity. The purpose and significance of this study were to investigate the role of exercise as an alternative therapy since some patients exhibit sensitivity/intolerance to some drugs. Initially, 65 hypertensive females (average age = 49.7 years) (systolic blood pressure, SBP >140 mmHg and/or diastolic blood pressure, DBP>85 mmHg) and 25 hypertensive females as a control group (average age = 50.3 years and systolic blood pressure, SBP >140 mmHg and/or diastolic blood pressure, DBP>85 mmHg) were selected. The subjects were divided based on their age, duration of disease, physical activity, and drug consumption. Then, blood pressure and heart rate (HR) were measured in all of the patients using a sphygmomanometer (pre-test). The exercise sessions consisted of warm-up, aerobic activity, and cooling down (total duration of 20 minutes for the first session up to 55 minutes in the last session). At the end of the 12th session (mid-test) and final session (24th session), blood pressure was measured for the last time (post-test). The control group was without any exercise during the study. The results were analyzed using a t-test. Our results indicated that moderate physical activity was effective in lowering blood pressure by 6.4/5.6–mm Hg for SBP and 2.4/4.3mm Hg for DBP in hypertensive patients, irrespective of age, duration of disease, and drug consumption ( P<.005). The control group indicates no changes in BP. Physical activity programs with moderate intensity (approximately at 60% MHR), three days per week, can be used not only as a preventive measure for diastolic hypertension (DBP>90 mmHg high blood pressure) but also as an alternative to drug therapy in the treatment of hypertension, as well.

Keywords: endurance exercise, elderly female, hypertension, physical activity

Procedia PDF Downloads 86
2307 Characteristics of Bio-hybrid Hydrogel Materials with Prolonged Release of the Model Active Substance as Potential Wound Dressings

Authors: Katarzyna Bialik-Wąs, Klaudia Pluta, Dagmara Malina, Małgorzata Miastkowska

Abstract:

In recent years, biocompatible hydrogels have been used more and more in medical applications, especially as modern dressings and drug delivery systems. The main goal of this research was the characteristics of bio-hybrid hydrogel materials incorporated with the nanocarrier-drug system, which enable the release in a gradual and prolonged manner, up to 7 days. Therefore, the use of such a combination will provide protection against mechanical damage and adequate hydration. The proposed bio-hybrid hydrogels are characterized by: transparency, biocompatibility, good mechanical strength, and the dual release system, which allows for gradual delivery of the active substance, even up to 7 days. Bio-hybrid hydrogels based on sodium alginate (SA), poly(vinyl alcohol) (PVA), glycerine, and Aloe vera solution (AV) were obtained through the chemical crosslinking method using poly(ethylene glycol) diacrylate as a crosslinking agent. Additionally, a nanocarrier-drug system was incorporated into SA/PVA/AV hydrogel matrix. Here, studies were focused on the release profiles of active substances from bio-hybrid hydrogels using the USP4 method (DZF II Flow-Through System, Erweka GmbH, Langen, Germany). The equipment incorporated seven in-line flow-through diffusion cells. The membrane was placed over support with an orifice of 1,5 cm in diameter (diffusional area, 1.766 cm²). All the cells were placed in a cell warmer connected with the Erweka heater DH 2000i and the Erweka piston pump HKP 720. The piston pump transports the receptor fluid via seven channels to the flow-through cells and automatically adapts the setting of the flow rate. All volumes were measured by gravimetric methods by filling the chambers with Milli-Q water and assuming a density of 1 g/ml. All the determinations were made in triplicate for each cell. The release study of the model active substance was carried out using a regenerated cellulose membrane Spectra/Por®Dialysis Membrane MWCO 6-8,000 Carl Roth® Company. These tests were conducted in buffer solutions – PBS at pH 7.4. A flow rate of receptor fluid of about 4 ml /1 min was selected. The experiments were carried out for 7 days at a temperature of 37°C. The released concentration of the model drug in the receptor solution was analyzed using UV-Vis spectroscopy (Perkin Elmer Company). Additionally, the following properties of the modified materials were studied: physicochemical, structural (FT-IR analysis), morphological (SEM analysis). Finally, the cytotoxicity tests using in vitro method were conducted. The obtained results exhibited that the dual release system allows for the gradual and prolonged delivery of the active substances, even up to 7 days.

Keywords: wound dressings, SA/PVA hydrogels, nanocarrier-drug system, USP4 method

Procedia PDF Downloads 137
2306 The Effect of the Contributory Pension Scheme on Employees’ Performance

Authors: Oladipo Jimoh Ayanda, Fashagba Mathew Olasehinde

Abstract:

Pension is a post retirement benefit paid to employees after retirement to cushion the effects of severance from monthly emoluments. It serves the dual purpose of providing financial succour to retired employees as well as motivating employees currently in service to greater performance on duty. However, the scheme, as operated in Nigeria, is prone to some pitfalls such as delayed and irregular payments, inadequate budgetary provisions, employee sufferings and deaths arising from the rigors of verification exercises, among others. This necessitated the replacement of the old scheme with the contributory pension scheme through an enabling law in 2004. The implementation of the new scheme has its own challenges especially in connection with administration. These challenges pose a fundamental problem of establishing a nexus between pension benefits and work performance which represent the focus of the study. The study objectives were to: determine the effect of contributory pension scheme on employees’ performance. The study population consisted of National Universities Commission recognized public and private universities in the South West Nigeria. Multi-stage sampling method involving stratified sampling and systematic sampling was used in selecting 359 respondents while data were collected through questionnaire administration. The procedure for analyzing the data included descriptive statistic, normal distribution test and cross-tabulation (gamma coefficient). The findings of the study showed that the existence of the scheme positively enhances employees’ performance as indicated by normal distribution test with Z-score (10.169) which is greater than the table value (1.96) at 0.05 level. The study concluded that the scope for enhancing employee current job performance can be quite elastic if future retirement benefits are guaranteed through proper and efficient administration and management of the contributory pension scheme. The study recommended that certain factors such as employers’ commitment which account for different levels of confidence between public and private universities should be looked into in order to improve confidence across board while the provisions of the scheme as they affect the PFAs should be properly monitored to ensure compliance.

Keywords: pension, retirement, performance, employees, benefit

Procedia PDF Downloads 313