bluuebunny/crossref_metadata_2025 huggingface dataset:
Do not underestimate the value of preprints in the social sciences and humanities just because they are un-peer-reviewed
Authors: Vuong Quan-Hoang
Published: September 2019

In this little essay, I describe my experience gained from my own ‘experiments,’ if you like, on the actual value un-peer-reviewed preprints in the social sciences and humanities could possibly benefit their authors.
https://beamers.github.io/autism.html
Authors: Beames Brian
Published: September 2019

https://beamers.github.io/autism.html
A Glance Overview of Light Pollution
Authors: Setiawan Adib Rifqi
Published: September 2019

This work explains at a glance about light pollution as one form of environmental pollution that is less attention and even tends to be underestimated by the public.
Selective publication of findings: Why does it matter, and what should we do about it?
Authors: Kasy Maximilian
Published: September 2019

This essay argues that different justifiable objectives for scientific institutions lead to contradictory recommendations.We need to be explicit about our objectives in order to discuss the tradeoffs between them.Replicability and the validity of conventional statistical inference constitute one such objective, and they indeed require that publication decisions do not depend on findings. This is what motivates much of current reform efforts.Validity of inference is presumably not the only objective, however -- it could easily be achieved by estimates derived from a random number generator.Relevance of findings might be another objective.If our goal is to inform decision makers or to maximize social learning, there is a strong rationale to selectively publish surprising findings.A third objective could be the plausibility of published findings.If there is some uncertainty about the quality of studies and we want to avoid publishing incorrect results, we might want to selectively publish unsurprising findings.How can we resolve the tension between these contradictory recommendations?I will outline one possibility below, proposing a functionally differentiated publication system, with different outlets focusing on different objectives.Measures that are promoted by current reformers, such as pre-analysis plans and registered reports, would have to play a crucial role in such a system.Following these policy proposals, I will take a step back and argue that these debates raise some fundamental questions for statistical theory.In order to coherently discuss these issues, statistical theory needs a model of the work of empirical research that goes beyond the single-agent model of statistical decision theory.We should understand statistics (quantitative empirical research) as a social process of communication and collective learning that involves many different actors with differences in knowledge and expertise, different objectives, and constraints on their attention and time, who engage in strategic behavior.
Structure and kinematics of an extensional growth fold, Hadahid Fault System, Suez Rift, Egypt
Authors: Jackson Christopher Aiden-Lee , Whipp Paul S , Gawthorpe Robert , Lewis Matthew M
Published: September 2019

Normal faulting drives extensional growth folding of the Earth’s upper crust during continental extension, yet we know little of how fold geometry relates to the structural segmentation of the underlying fault. We use field data from the Hadahid Fault System, Suez Rift, Egypt to investigate the geometry and kinematics of a large (30 km long, up to 2.5 km displacement), exceptionally well-exposed normal fault system to test and develop models for extensional growth folding. The Hadahid Fault System comprises eight, up to 5 km long segments that are defined by unbreached or breached monoclines. These segments are soft-linked, hard-linked, or defined by a more subtle along-strike transition in overall structural style. High overlap:separation (O:S) ratios between its segments suggest the Hadahid Fault System comprises a single, now hard-linked structure at-depth. We demonstrate that a progressive loss of at-surface displacement along strike of the Hadahid Fault System results in surface-breaking faults and breached monoclines being replaced by unbreached monoclines developed above blind faults. However, shorter along-strike length-scale variations in structural style also occur, with unbreached monoclines developed between breached monoclines. The origin of this variability is unclear, but might reflect local variations in host rock material properties that drive short length-scale variations in fault propagation-to-slip ratio, and thus the timing and location of fold breaching. We show that folding is a key expression of the strain that accumulates in areas of continental extension, and argue that tectono-sedimentary models for rift development should capture the related structural complexity.
The Potential for Ducted Wind Turbines in an Urban Environment
Authors: Suri Dhruv
Published: September 2019

This article discusses the applicability of Ducted Wind Turbines for decentralized energy generation in an urban environment. Ducted Wind Turbines overcome various constraints posed by urban infrastructure including reduced wind speed, effect of the atmospheric boundary layer as well as lesser space availability. Ducted Wind Turbines present a new way of sourcing energy at a local level, aiding community based models of energy distribution and consumption. The main aim of the present letter is to propose Ducted Wind Turbines as a precursor for energy production in urban, peri-urban as well as rural areas around the world.
Review Jurnal PI Indonesia's Efforts to Achieve Globally Competitive Human Resources
Authors: Widyadhana Felix
Published: September 2019

Human resources (sumber daya manusia) merupakan suatu hal yang sangat penting, terlebih bagi Indonesia untuk beradaptasi dengan era Revolusi Industri 4.0. Review ini membahas tentang upaya-upaya yang dilakukan Indonesia serta apa yang dapat dilakukan untuk menghadapi era Revolusi Industri 4.0.
REVIEW PI KELOMPOK 8 KP C
Authors: 8 Kelompok
Published: September 2019

Keberadaan pabrik gula di tanah Jawa dalam sejarahnya tidaklah lepas dari kebijakan culturestelsel yang diterapkan oleh pemerintah Kolonial Hindia Belanda (Tayibnapis, Sundari, & Wuryaningsih, 2016). Gubernur jenderal Johannes Van Den Bosch mewajibkan desa di Jawa menyisihkan 20% tanahnya untuk di tanami tanaman ekspor seperti kopi,tebu,dan teh. Tebu terutama di tanam di sejumlah karesidenan seperti Surabaya,Pasuruan,dan Besuki.
IMPLEMENTASI GEOGRAPHIC INFORMATION SYSTEM (GIS) SEBAGAI MEDIA PENCARIAN PONDOK PESANTREN DI KOTA PEKANBARU DENGAN METODE DIJKSTRA
Authors: Yunefri Yogi
Published: September 2019

Penelitian ini dilaksanakan untuk mempelajari dan mengembangkan Sistem Informasi Geografis dengan metode pengembangan Algoritma Dijkstra pada Kantor Kementrian Agama Kota Pekanbaru. Data dikumpulkan melalui hasil pengamatan dan pengambilan sampel data pondok pesantren di bagian Seksi Pendidikan Diniyah dan Pondok Pesantren untuk dijadkan objek penelitian. Data yang didapat kemudian diolah dan dipelajari berdasarkan klasifikasi pondok pesantren dengan masing-masing teknik yang digunakan. Berdasarkan data tersebut, metode algoritma Dijkstra lebih tepat untuk digunakan untuk membangun aplikasi sistem informasi geografis. Melalui pengujian graph tipe A dan B serta pengujian Black Box dapat diketahui bahwa masing-masing teknik pengujian memiliki kelebihan dan kekurangan. Namun demikian jika dikaitkan dengan studi kasus yang ditemukan di Kantor Kementrian Agama Kota Pekanbaru metode algoritma Dijkstra lebih direkomendasikan untuk studi kasus tersebut karena metode algoritma Dijkstra lebih popular dan banyak digunakan. Sehingga hasil implementasi diharapkan dapat tercapai maksimal.
PPKn
Authors: rahmadhani Rizki
Published: September 2019

Setelah Indonesia lahir maka dibentuk dan disepakati terkait karakteristik negara Indonesia yang didalamnya berisikan identitas nasional Indonesia. Setiap negara memiliki suatu identitas untuk melambangkan keagungan suatu negara.
An Accurate Solution for Credit Valuation Adjustment (CVA) and Wrong Way Risk
Authors: Xiao Tim
Published: September 2019

This paper presents a Least Square Monte Carlo approach for accurately calculating credit value adjustment (CVA). In contrast to previous studies, the model relies on the probability distribution of a default time/jump rather than the default time itself, as the default time is usually inaccessible. As such, the model can achieve a high order of accuracy with a relatively easy implementation. We find that the valuation of a defaultable derivative is normally determined via backward induction when their payoffs could be positive or negative. Moreover, the model can naturally capture wrong or right way risk.
Decision making in slow and rapid reaching: Sacrificing success to minimize effort
Authors: Hesse Constanze , Kangur Karina , Hunt Amelia R.
Published: September 2019

Current studies on visuomotor decision making come to inconsistent conclusions regarding the optimality with which these decisions are made. When executing rapid reaching movements under uncertainty, humans seem to automatically select optimal movement paths that take into account the position of all potential targets (spatial averaging). In contrast, humans rarely employ optimal strategies when making decisions on whether to pursue two action goals simultaneously or prioritise one goal over another. Here, we manipulated whether spatial averaging or pre-selection of a single target would provide the optimal strategy by varying the spatial separation between two potential movement targets as well as the time available for movement execution. Experiment 1 provided a generous amount of time to reach the final target. Participants tended to pre-select the target that was easiest to reach and correct their movement path in-flight if required. In Experiment 2, a strict time limit was set, such that the optimal strategy depended on the separation between the potential targets: for small separations, there was sufficient time to employ averaging strategies, but higher success for larger separations required pre-selecting the final target instead. None of our participants adjusted their movement strategies with spatial separation, however. In Experiment 3, we confirm the bias towards targets that are easiest to reach and show that this comes at the expense of overall task success. The results suggest a strong tendency to minimize immediate movement effort, and a failure to flexibly adjust movement strategies to maximize the probability of success.
Fenny Roshayanti: A Biography of Science Educator for Our Time
Authors: Setiawan Adib Rifqi
Published: September 2019

STEAM is an acronym for Science, Technology, Engineering, Art, Mathematics. STEAM defined as the integration of science, technology, engineering, art, and mathematics into a new cross-disciplinary subject in schools. The concept of integrating subjects in Indonesian schools, generally is not new and has not been very successful in the past. Some people consider STEAM as an opportunity while others view it as having problems. Fenny Roshayanti is science educator and researcher that consider STEAM as an opportunity. She has involved the study of STEAM, as an author, educator, academic advisor, and seminar speaker. This article examines what it has been and continues work from Fenny Roshayanti in the science education. Our exploration uses qualitative methods of narrative approaches in the form of biographical studies. Participants as data sources were selected using a purposive sampling technique which was collected based on retrospective interview and naturalistic observation. Data's validity, reliability, and objectivity checked by using external audit techniques. This work explores the powerful of female’s personal style in developing a form of social influence based on her forms of capital as well as address the positive and negative consequences that may follow while implement and research STEAM in teaching classroom.
Teaching English in Multilingual and Multicultural Contexts in Nepal
Authors: Bhandari Bhim Lal
Published: September 2019

English is being taught in diverse contexts around the globe. Teaching of English in multilingual and multicultural contexts in Nepal is one of the major challenges in ELT. The majority of classes in Nepal consist of linguistic and cultural diversity where students need to have different learning materials, methodologies and learning styles which help them minimize the problems of interaction and comprehension. This article presents both challenges and opportunities of teaching English in multicultural and multilingual contexts. The problems created by linguistically heterogeneous learners and attitude of parents towards multilingual education are the major challenges for its effective implementation. Moreover, the problems of teachers and students are being addressed in this article along with some suggestions for teachers to solve them and make ELT more effective, better and easier.
Ramalin, a Novel Phenyl Hydrazide from the Lichen Ramalina Terebrata; Isolation, Total Synthesis and Biological Activities
Authors: Pandey Durga Prasad , Bhattarai Hari Datta
Published: September 2019

Ramalin, a new L-glutamic acid derivative of phenylhydrazide (Y-glutamyl-N'-(2-hydroxyphenyl) hydrazide, 1) was isolated from the Antarctic lichen, Ramalina terebrata after a series of bioactivity guided fractionation of crude aqueous methanolic extract. Ramalin showed stronger antioxidant activities than commercially available standards, ascorbic acid, trolox, BHA, kojic acid in both, in vitro and in vivo test systems. In addition, ramalin showed no/less toxicity effects against two human cell lines; fibroblast (CCD-986SK) cells and keratinocyte (HaCaT). Thus, realign merits for cosmetic application and industrial scale production were needed. We developed a cost effective total synthesis of ramalin with 71.5% yield and described here.
Teacher Training in Nepal: Issues and Challenges
Authors: Gautam Ganga Ram
Published: September 2019

“No single element is more essential to students’ success than excellence in teaching. Fine buildings, equipment, and textbooks are important, but it is the skill and dedication of the teacher that creates a place of learning.” (Hickok, E. 1998).

The quote highlights the role of teachers and it is generally accepted that teachers are the key actors who contribute to the making of people through education. Teachers are often considered as ‘good people’ and in the context of Nepal especially in the rural areas; it is the teacher who is often consulted for any important work in the community. “The teachers are in the business of making good people, or of enabling their students to become good people. They do this specifically by helping them to become smarter” (Tate, 2007: 1). Thus, preparation of teaching force is, therefore, a key concern of the government throughout the world. It is the teacher who lays the foundation of all the professionals when they attend the elementary and secondary school (Farris and Rieman, 2014). Nepal government too has invested a huge amount of resources in teacher training thinking that training would result effective pedagogic skills among teachers and they could then use those skills in their classrooms so that students will have better achievement. However, while reviewing the available literature on teacher training in Nepal, it shows that very little has been achieved in this area in the last few decades. This article is an attempt to review the impact of teacher training in Nepal and identify the major issues in them so as to find out the ways of improving the teacher training in Nepal.
A Meta-Analysis of Researches on Implementing the Semester System: The Way Ahead?
Authors: Sharma Netra Prasad
Published: September 2019

At present, Tribhuvan University (TU) seems to be in a sort of dilemma as to whether or not the semester system can be implemented in the programmers run by its faculties. Although TU authorities are still in extended discourse with the concerned stakeholders for the expansion of the semester programme, I sense some dilemma in the steps to be taken, the confusion propped by the fact that even the Master’s programmes under the semester system have not been extended horizontally to the campuses other than the Central Departments at Kirtipur and the two other campuses in the valley only in science education. In this context, this article attempts to synthesize the research findings akin to the semester system and, based on the researches reviewed, points out the possible hurdles that need to be taken into consideration in advance and handled with great caution. The article argues that, despite some socioeconomic challenges, the semester system is better than the annual one and that it is the responsibility of all stakeholders to contribute to the implementation and success of the semester programmes.
Teachers’ Engagement in Bringing out the Best in Students
Authors: Rijal Rishi Ram
Published: September 2019

Teaching English is one of the complex and demanding matters because the teachers have to deal with the students of diverse nature, various circumstances and expectations. Like in other professions, teaching cannot be performed within the specified time. It needs much more time to be engaged in for the pre-planning, classroom delivery and post delivery reflections. In this article, the engagement of an English teacher of secondary level to bring out the best in students has been discussed in terms of his planning preparation, delivery, reflection as well as evaluation, training and collaboration with the administration and other colleagues. After the analysis of the data it has been found that English teachers in the Kathmandu valley are over busy; they do not have enough time to make planning, preparation and collaboration with the colleagues.
अछामी लिङ्ग व्यवस्था Achhami Linga Byabstha
Authors: शाही Shahi हर्कबहादुर Harkabahadur
Published: September 2019

अछामी भाषाको परिचय दिई यस भाषाको लिङ्ग व्यवस्था पहिचान गर्नु मूल उद्देश्य रहेको प्रस्तुत लेख गुणात्मक प्रकृतिको रहेको छ । क्षेत्र अध्ययन विधिको उपयोग गरिएको यो अध्ययन वर्णनात्मक रहेको छ । अछामी भाषा बोल्ने सम्पूर्ण अछामी भाषी वक्ता यस अध्ययनको जनसङ्ख्या हुन भने पान्सय दरा (क्षेत्र) का उमेरगत, लिङ्गगत, जातिगत, साक्षर र निरक्षरताका आधारमा २० जना अछामी भाषी वक्तालाई उद्देश्यपूर्ण नमुनाका रूपमा छनौट गरी श्रव्य सामग्रीका माध्यमबाट विभिन्न क्षेत्रमा बोलिने अछामी भाषाका पाठहरू सङ्कलन गरी टुलबक्सको सहायताले इन्टरलिङ्गराइज गरिएको छ । लिप्याङ्कन गरिएका पाठलाई व्याकरण सिद्धान्तका सहायताले अछामी लिङ्गभेदको विश्लेषण गरिएको छ । भारोपेली समूहको अछामी भाषा अछाम जिल्लामा बोलिन्छ । यस भाषामा लेखिएका अभिलेख, साहित्य, व्याकरण र स्नातकोत्तरदेखि विद्यावारिधिसम्मका लोकसाहित्य र भाषाका विविध पक्षमा गरिएका अनुसन्धानले यसको स्वतन्त्र भाषिक अस्तित्व कायम गर्न सघाएको पाइन्छ । अछामी भाषाका लिङ्गभेदको प्रभाव नाम, विशेषण, क्रियाविशेषण र कोटिकरमा रहेको पाइन्छ । यस भाषामा मानवेत्तर गाईमा पनि स्त्रीलिङ्गको भेद पाइनु, मानवीय जना कोटिकरको स्त्रीलिङ्ग जनी हुनु र स्थानिक क्रियाविशेषणमा पनि लिङ्गभेद पाइनु यस भाषाका आफ्ना छुट्टै लिङ्गगत विशेषता हुन् ।
उच्च सिकाइ उपलब्धिका कारक पक्षहरू Uchha Sikai Upalabdhika Karak Pakshyaharu
Authors: पौडेल Poudel नेत्रप्रसाद Netraprasad
Published: September 2019

सर्लाही जिल्लास्थित खुटौना गा.वि.स. ओडा नं. १ मा रहेको श्री जनता निम्न माध्यमिक विद्यालयमा गई क्षेत्रकार्यअन्तर्गत प्रामाणिक सूचनाहरू लिएर गरिएको प्रस्तुत अध्ययनबाट विद्यार्थीहरूको उच्च सिकाइ उपलब्धि हासिल गर्नका लागि विषय शिक्षकहरूको सर्वाधिक भूमिका हुने देखियो । सिकाइ उपलब्धिलाई उच्च तुल्याउनका लागि यस विद्यालयले व्यावहारिक शिक्षण, उपलब्ध शैक्षिक सामग्रीहरूको यथोचित प्रयोग, पुस्तकालयको अभावमा समेत थोरै पुस्तकहरू जुटाएर झोले÷घुम्ती पुस्तकालयको व्यवस्था, केही गर्ने अठोट, नियमित गृहकार्य, पृष्ठपोषणर परीक्षा, नतिजाको नियमित विश्लेषण, सबै विषयप्रति प्रअको समान दृष्टिकोण, वृत्तिविकासका लागि शिक्षकहरूलाई आलोपालो अवसर, पारदर्शी मूल्याङ्कन, समस्याहरूको वस्तुगत आकलन र निराकरणका लागि ठोस योजना, योजना र निर्णयहरूको इमानदारी कार्यान्वयन तथा कार्यक्रमिक र नीतिगत तहको सन्तुलित व्यवस्थापन गर्न अधिकतम प्रयत्न गरेको पाइयो । यस विद्यालयले विद्यालयीय सिकाइमा खपत हुने समय, गृहकार्यको सूक्ष्म परीक्षण, तत्काल पृष्ठपोषण तथा प्रभावकारी शिक्षण सिकाइ गरी विशेष चार कुराहरूमा ख्याल गरेको देखियो । बालकको सिक्ने आनीबानी, त्यसमा गुरुहरू र अग्रजहरूको प्रभाव, त्यसबाट उनीहरूको सिकाइ उपलब्धिमा पर्ने असरका बारेमा विद्यालय परिवार सचेत देखियो । प्रधानअध्यापक विद्यालय व्यवस्थापन समितिका सदस्य सचिव तथा भूमिकामूलक नेतृत्व समेत भएका कारण उनले वि.व्य.स. र अन्य सरोकारवालाहरूको माझमा समन्वयकारी भूमिका निर्वाह गरेको पाइयो । सबै बालबलिकाका सबल र दुर्बल पक्षहरूको जानकारी प्राप्त गरी उनीहरूको पढाइ सुधार्ने योजनामा अभिभावकहरूस“ग सहकार्य, आºना कमी कमजोरीहरू हटाउनका लागि प्रधानअध्यापक स्वयम्बाट र अन्य वरिष्ट शिक्षकद्वारा शिक्षकहरूको नियमित कक्षा अवलोकनपछि पृष्ठपोषण दिने, शिक्षकहरूबाट प्रअ र वरिष्ट शिक्षकहरूको कक्षा अवलोकनपछि टिप्पणी गराउने कार्यप्रणाली अवलम्बन गरेको देखियो ।
KONDE - Ein Netzwerk bringt Forschungs- und GLAM-Institutionen zusammen. Ein Projektbericht
Authors: Stigler Johannes , Klug Helmut W.
Published: September 2019

Seit Frühjahr 2017 läuft als Hochschulraum-Strukturmittel-Projekt das „Kompetenznetzwerk Digitale Edition“ (KONDE), das sich den Prämissen der Open Science Community verpflichtet fühlt und darauf zielt, Voraussetzungen für die Etablierung einer nachhaltigen, nationalen Publikationsplattform für Digitale Editionen (DE) für geistes-, sozial- und kulturwissenschaftliche Disziplinen (GSK) zu schaffen. Beiträger*innen der Universitäten Graz, Innsbruck, Klagenfurt, Salzburg und Wien, sowie der Technischen Universität Graz und der Kunstuniversität Graz, gemeinsam mit Fachkolleg*innen der Österreichischen Nationalbibliothek, der Österreichischen Akademie der Wissenschaften und des Adalbert Stifter-Instituts des Landes Oberösterreich haben sich das Ziel ge­setzt, eine Forschungsinfrastruktur für Digitale Editionen aufzubauen und österreichweit vorhandene Kompetenzen in diesem Bereich zu bündeln. Diese Infrastruktur soll keinesfalls nur als Hardware-Lösung oder Sammlung technischer Lösungsansätze verstanden werden, sondern möchte das Thema DE auch aus methodisch-theoretischer Sicht systematisch aufarbeiten und die Arbeits- und Diskussionsergebnisse der einschlägigen Scientific Community in einem interaktiven Weißbuch „Digitale Edition“ zur Verfügung stellen.
PENGARUH PENDIDIKAN KESEHATAN TENTANG MENARCHE TERHADAP PENGETAHUAN SISWI KELAS IV, V DAN VI DI SDN 01 BEKIRING KECAMATAN PULUNG KABUPATEN PONOROGO
Authors: Rohmah Eliya Rohmah
Published: September 2019

Menarche yaitu menstruasi yang pertama kali yang biasanya terjadi pada usia 12-13 tahun, Menarche merupakan peristiwa paling penting pada remaja putri sebagai pertanda siklus masa subur sudah dimulai. Berdasarkan dari hasil studi pendahuluan pada bulan November 2016 terhadap 10 siswi di SDN 01 Bekiring didapatkan dari 10 responden mengatakan yang belum pernah menstruasi didapatkan 8 siswi (80%) belum mengetahui tentang menarche dan belum pernah diberikan pendidikan tentang menarche

Tujuan penelitian ini adalah untuh menganalisis adanya pengaruh pendidikan kesehatan tentang menarche terhadap pengetahuan siswi kelas IV, V dan VI di SDN 01 Bekiring  Kecamatan Pulung Kabupaten Ponorogo. Metode penelitian yang digunakan adalah pre-exsperimental design dengan pendekatan one group pretest posttes.  Populasi terdiri dari 40 siswi kelas IV, V dan VI. Sampel dalam penelitian ini adalah siswi yang hadir saat penelitian sebanyak 31 siswi. Sampling menggunakan  teknik purposive sampling. Dengan Instrumen untuk variabel pendidikan kesehatan dalam penelitian ini adalah leaflet, LCD dan SAP.

Hasil penelitian menunjukkan sebelum diberikan  pendidikan kesehatan  54,8% responden memiliki pengetahuan cukup, dan sesudah diberi pendidikan kesehatan 58,1% berpengetahuan baik. Sedangkan dari hasil uji statistik paired T-Test tersebut terlihat bahwa nilai signifikan sebesar 0,000. Yang  artinya “ada pengaruh pendidikan kesehatan tentang menarche terhadap pengetahuan siswi kelas IV, V  dan  VI di SDN 01 Bekiring, Kec. Pulung Kab. Ponorogo”. Disarankan untuk petugas puskesmas, untuk mengadakan penyuluhan tentang menarche ke sekolah yang lain.

Kata kunci: pendidikan nkesehatan, menarche, pengetahuan
Technology administration active substance in the ointment base
Authors: Trochimchuk V. V. , Shmatenko V. V. , Tarasenko V. O. , Drozdova A. O.
Published: September 2019

The problem of expanding the range of medicines that are used for the topical treatment of wound process, remains an important challenge for practical military medicine. In this aspect, there are topical ointments combining development for use in the first phase of wound process, which has a complex influence on the pathological processes and exhibits antibacterial, anti-inflammatory and local anesthetic activity.

The aim of the study was substantiation of technological route of administration of the active pharmaceutical ingredients in the ointment base, depending on the antimicrobial activity of model compositions.

The study included a model sample of ointment bases, cooked on a hydrophilic carrier containing active pharmaceutical ingredients – ofloxacin, nimesulide and lidocaine.

Microbiological studies were performed by difution on solid agar medium, which is based on the ability of substances to inhibit the growth antibakterial microorganisms.

Comparative analysis of experimental studies showed that the samples of ointments, which are based whith the active pharmaceutical ingredients ofloxacin, nimesulide and lidocaine was injected as a solution in DMSO showed the highest antimicrobial activity.

As a result of study on the antimicrobial activity of ointments model samples determined that the optimal method of administering the basis AFI – ofloxacin, nimesulide and lidocaine – a method of administering them in the form of a solution in DMSO.
Synthesis, antibacterial and antifungal activity of 1-[4-(1,1,3,3-tetramethylbutyl)phenoxy]-3-dialkylamino-2-propanol quaternary salts
Authors: Korotkii Y. V. , Vrynchanu N. A. , Dronova M. L. , Suvorova Z. S. , Smertenko O. A.
Published: September 2019

The emergence and spread of resistant strains of pathogens as well as reduction of the efficacy of current antimicrobial agents requires the development of novel antimicrobial compounds.

The aim of the present study was synthesis and evaluation of antimicrobial activity of new arylaliphatic aminopropanols.

The objects of the present study were 1-[4-(1,1,3,3-tetramethylbutyl)phenoxy]-3-dialkylamino-2-propanol quaternary salts (compounds I–XIV).

Compounds synthesis was carried out by heating of precursor epoxide and excessive amount of appropriate amines in isopropanole, followed by treatment with excess of alkyl halides. Methods of elemental analysis, IR- and PMR-spectroscopy were used for confirmation of chemical structure. Antimicrobial activity against Staphylococcus аureus АTCC 25923, Escherichia coli ATCC 25922, Pseudomonas aeruginosa АТСС 27853 and Candida albicans NCTC 885/653 was determined by a broth dilution method and evaluated via minimum inhibitory concentration (MIC).

Our investigation of antibacterial and antifungal activity of 1-[4-(1,1,3,3-tetra methylbutyl)phenoxy]-3-dialkylamino-2-propanol quaternary salts showed that compounds possess narrow spectrum, as well as broad spectrum action. Significant antimicrobial activity of the novel aryl aliphatic aminoalcohols indicates their potential usage as a component of new antimicrobial drugs.
Structural and adsorptive properties of silica-alumina and clay materials of mineral and synthetic origin
Authors: Gerashchenko I. I. , Voitko I. I. , Vasilieva A. V.
Published: September 2019

Location on territory of Ukraine of great deposits of aluminosilicates together with good facilities for their processing and standardization promotes the study of this raw material, results of which could be useful for the developers of enterosorbents. For search the specific sorptive activity a comparative examination of several materials of silica-alumina and clay nature has been carried out in this work.

The X-ray phase analysis, a measuring of specific surface area by the low temperature adsorption–desorption of nitrogen and the method of isotherm of adsorption have been used.

It is shown that silica-alumina and clay materials have much less specific surface as compared to silica gel Syloid® 244 FP and carbon sorbent SCN. The sorbents of montmorillonite type (smectite, saponite) are characterized by the highest adsorptive capacity in relation to methylene blue and congo red dyes. Synthetic zeolites NaA and NaX effectively absorb the ions of zinc from solution, significantly overcoming Syloid® 244 FP and SCN which were taken as preparations of comparison. Therefore, on the basis of NaA and NaX the selective enterosorbents for elimination from the organism of toxic metals could be created.
Evaluation of factions antigens disintegration fungal cells Candida albicans and Candida tropicalis if advised candidiasis
Authors: Rybalkin M. V. , Filimonova N. I. , Strilets O. P. , Strelnikov L. S.
Published: September 2019

Candidiasis – one of the most common fungal diseases humanity has ever faced. Etiological factors of the disease are most often Candida albicans and Candida tropicalis. To fight Candida infection has been actively conducting research on vaccine development, as in the CIS countries and in the countries of Europe and America. In the context of this research have shown trends of development of combined subunit vaccines based on the fungi Candida. Authors at the National University of Pharmacy at the Department of Biotechnology and Microbiology, Virology and Immunology developed a method of disintegration of cells of fungi C. albicans and C. tropicalis using ultrasound.

The objective of our work was the experimental evaluation of fungal cell antigen fractions C. albicans and C. tropicalis in the prevention and treatment of candidiasis.

Fungal cells from C. albicans and C. tropicalis were isolated proteins and polysaccharides using an ultrasonic disintegrator when extending wave of 22 kHz and 15 min exposure. Filtered through a membrane «Vladipor» IPA-MA № 3, which provides shutoff of the biological material with a size of 10 kDa.Obektom study were fractions dezintegrata fungal cell C. albicans and C. tropicalis molecular size and greater than 10 kDa. Mice were intramuscularly twice at an interval of 14 days were injected into the upper portion of the right hind paw of 0.2 ml of separately investigated fractions at a protein concentration for C. albicans 3 mg/ml for C. tropicalis 5 mg/ml. After 1 month, for one group, and after 3 months for a second group of test animals after the second injection, the animals carried abdominal infection. After 14 days the animals were carried out inspection and measured results

The studies found that the fraction of cells dezintegrata fungi C. albicans and C. tropicalis with a molecular size of 10 kDa at double intramuscular injection of 0.2 ml provides 100% efficacy in the prevention of Candida infections.
Synthesis of new potential biological active substances among 3-mercapto-4-amino-5-benzyl-1,2,4-triazol-4H derivatives
Authors: Saidov N. B. , Georgiyants V. A. , Garnaya N. V.
Published: September 2019

Conventional approaches to the formation of 1,2,4-triazole ring allow to introduce different substituents into the heterocyclic ring during the synthesis of key intermediates stage. In continuation of previous studies the synthesis of 3-mercapto-4-amino-5-benzyl-1,2,4-triazole-4H derivatives is described.

The aim of investigation was synthesis of a series of new derivatives of 3-mercapto-4-amino-5-benzyl-1,2,4-triazole, proving their structure by physico-chemical methods and planning of pharmacological screening using PASS.

Phenylacetic acid ethyl ester has been used for the synthesis as starting substance. It was subjected to hydrazinolysis to receive an appropriate hydrazide. In the next stage substance obtained was processed with hydrogen disulfide and appropriate potassium ditiokarbaminat has been received, which by reaction with an excess of hydrazine hydrate has been cyclised into a target 3-mercapto-4-amino-5-benzyl-1,2,4-triazol-4H. The first stage of chemical transformation reactions of key intermediate was its alkylation with chloroacetanilides under alkaline catalysis. By Paal–Knorr reaction the amino group in the synthesized alkylthio-4-amino-5-benzyl-1,2,4-triazole-4H was modified into pyrrole ring by the action of 2,5-dimethoxytetrahydrofuran in acetic acid medium.

The structure of the compounds synthesized has been proved by 1H NMR spectroscopy. The successful alkylation of mercapto group indicates the disappearance of its proton signal at the spectra and appearance of the acetanilide residues protons signals. Modification of the amino derivatives into corresponding pyrrolyl substituted has been accompanied by the appearance of the triplet signals of magnet equivalent methyne protons of the pyrrole ring (protons at positions 3.4) at 6.30 ppm. The signals of the second pyrrole protons pair overlap with other aromatic protons signals.

For the planning of pharmacological screening previous prognosis of the potential pharmacological activity spectrum has been carried out using software PASS. The prognosis showed that for all pyrrolyl substituted substances predominant in the spectrum of action was the influence on the central nervous system, and the probability of the activity of their synthetic precursors mainly limited to moderate antioxidant properties.
A relational database with pharmaceutical information: problems of creation and primary filling for provision of a qualitative statistical processing
Authors: Rervyatskyy I. Yu.
Published: September 2019

The disclosure of pharmaceutical information is not intended to provide the possibility of further automated processing of the data provided by independent experts, and, accordingly, the choice of the methods of presentation is aimed to optimize visual perception by users.

The aim of the work was to analyze in the internet-sources the availability of information in the appropriate format for automatic filling of the relational database. The subjects of the study were: ATC: ICD-10 (International Classification of Diseases); content of EF 9.8; classification of dosage forms by the Ministry of Health of Ukraine, FDA (Food and Drug Administration, USA), EMA (European Medicines Agency) and EphMRA (European Pharmaceutical Market Research Association). Methods used are review of information with the corresponding structure in the internet, processing of the information found using computer code.

Approbation was carried out on the basis of the digital online system «Likypedia» (http://likypedia.zzz.com.ua; http://facebook.com/likypedia).

The basic goals for the quality of the results of statistical processing of pharmaceutical information are formed. To achieve them, a list of required information for the initial download to the relational database is defined. The sources of the received information which was used for initial loading to the relational database are presented. The multicomponent record of pharmaceutical information is described.

The list of dosage forms was formed on the basis of own practical experience, trends in the indication on packaging of medicines by manufacturers, electronic databases of pharmaceutical wholesalers, the titles of articles given in the EF 9.8 edition. Information from different sources about pharmaceutical dosage forms was analyzed and divided into five information blocks: made by manufacturer; its characteristic; for DF, which will be prepared with DF produced by the manufacturer; its characteristic; way of using DF.

A variant has been developed and presented for structuring the information record of the drug dose in the relational database in several variants, which makes it possible to further carry out automated calculations, optimize the selection and sorting of data.
In silico screening of drug-like molecules for the treatment of cardiovascular diseases on the basis of five-membered privileged heterocycles
Authors: Drapak І. V.
Published: September 2019

Among various heterocyclic systems, the derivatives of five-membered heterocycles are of special interest. Most of the above mentioned heterocycles are treatred as so-called privileged structures in modern medicinal chemistry. In silico screening among five-membered heterocycles of molecules for the treatment of cardiovascular diseases is actual.

The aim of the work was the search for synthetic drug-like molecules based on functionalized five-membered heterocycles and related heterocyclic systems as an element of the theoretical platform for rational design of compounds acting on the cardiovascular system, and prediction of their possible mechanism of action.

The objects of the study were derivatives of uncondensed and condensed five-membered heterocycles. In the work, in silico approaches were applied using the programs: Hyper-Chem, PASS, AutoDock, PROTOX.

Based on the previous studies, focused sub-libraries of small synthetic drug-like molecules based on functionalized five-membered heterocycles and related heterocyclic systems have been selected. The compounds were divided on 12 groups. The optimization of the compound structures, the drug-like parameters calculation were carried out. The activity prediction, the acute toxicity level and docking studies to probable bio-targets which are related with cardiovascular drug mechanism of action have been carried out. It was shown that thiazole and thiadiazole based compounds possessed the highest calculated affinity levels to selected bio-targets. This is consistent with PASS-based prediction data.

Diverse functionalized derivatives of five-membered heterocycles (thiazole, thiazolidine, thiadiazole, pyrazole, thiophene, triazole)  and related fused heterocycles have been grouped in focused sub-libraries of compounds. it has been established that thiazole and thiadiazole based compounds are promising objects for directed synthesis and further modification as potential cardiovascular agents based on the prediction of biological activity, the calculation of affinity to potent bio-targets, and the prediction of the drug-like features and acute toxicity level. The prognostic values of the parameters of the above mentioned groups of compounds may be used as the element of theoretical platform for the search and de novo design of potential drugs for the treatment of cardiovascular diseases.
Luminescent determination of residues of trazodon hydrochloride and melatonin after cleaning pharmaceutical equipment
Authors: Voitiuk O. D. , Yegorova A. V. , Scrypynets Yu. V. , Kashutskуy S. N. , Antonovich V. P.
Published: September 2019

A prerequisite for ensuring the quality of medicines is their production in accordance with the rules of GMP (Good Manufacturing Practice for Medicinal Products), one of the most important requirements of which is equipment cleaning. In many cases, the same equipment is used in the production of various preparations. Therefore, to prevent contamination of each of the following drugs, the previous one, it is very important to carry out an effective equipment cleaning procedure with a mandatory assessment of its purity.

The purpose of this study was to develop simple, express, selective methods for luminescent determination of residual quantities of APIs of trazodone hydrochloride (TG) and melatonin (MT) in washes to control the completeness of their removal when cleaning process equipment.

The excitation and luminescence spectra were recorded using a Cary Eclipse "Varian" spectrofluorimeter (Australia) with a xenon lamp 150 W. Electronic absorption spectra were recorded on a UV-2401 PC spectrophotometer «Shimadzu» (Japan).

The electronic absorption spectra of TG and MT have absorption bands in the UV spectral region. It was established experimentally that the excitation spectra of TG and MT are similar to their absorption spectra (λex = 318 nm (TG) and λem = 274 nm (MT)). The effect on the luminescence intensity of TG and MT of methanol, ethanol, acetonitrile, dimethylformamide, dimethylsulfoxide, propanol (50 v/v) was studied. It is established that the maximum luminescence is observed in water.

The methods were validated according to the following parameters: specificity, linearity, accuracy, limit of quantitation. The degree of extraction of trazodone hydrochloride and melatonin from applicators and surfaces of pharmaceutical equipment is more than 90%. The developed methods can be recommended for determining the residual amounts of trazodone hydrochloride and melatonin while monitoring the quality of the cleaning of pharmaceutical equipment.
The research of anti-inflammatory activity of 5-(5-bromofuran-2-yl)-4-ethyl-1,2,4-triazole-3-thion S-derivatives
Authors: Pruglo Ye. S.
Published: September 2019

The studing of  anti-inflammatory activity of the novel compounds may give rise to the using of safer and more active drugs in the treatment of diseases which are shown NSAIDs.

To further study the pharmacological properties of the synthesized c compounds were studied for acute toxicity and anti-inflammatory activity of 5-thio derivates of 3-(5-вromofuran-2-yl)-4-ethyl-(4H)-1,2,4-triazole at white rats by formalin method of acute edema.

After investigation of anti-inflammatory activity in vivo of first synthesized 1,2,4-triazole derivatives it was found that potassium salt of 2-(4-ethyl-5-(5-bromfuran-2-yl)-1,2,4-triazoles 3-iltio) acetic acid (Compound 24) had the most significant anti-inflammatory activity. This compound suppressed the formation of edema quotes of rats at 59.87% and was more active than the reference drug diclofenac at 15.13%.

There were established the patterns regarding chemical structure and pharmacological action of these substances. So replacing of bromine atom at the dimethylamino group in the para-position of the phenyl radical in the molecule of N'-(4-brombenzyliden)-2-((5-(5-bromfuran-2-yl)-4-ethyl-4H-1,2,4-triazole-3-yl)tio)acetic hydrazid (Compound 36) was accompanied by appearence of the anti-inflammatory action.

It was revealed that in the number from the ammonium salt (Compound 30) to monoethanolamonium salt (Compound 23) and to the morpholinum salt (Compound 22) it was observed an increase of inflammation and probably growing number of pro-inflammatory mediators released.
Relationship of antimicrobial activity and chemical structure of the arylaliphatic aminoalcohol derivatives
Authors: Dronova M. L. , Suvorova Z. S. , Korotkyi Yu. V.
Published: September 2019

Arylaliphatic aminoalcohols appeared to be the new promising class of compounds for the development of antibacterial and antifungal agents. The aim of the presented study was to analyze the «chemical structure-antimicrobial activity» relationship for further activity-directed synthesis of compounds of this class.

The antimicrobial activity of the compounds was investigated by serial broth dilution method. Primary analysis of the effect of substituents’ structure on the ability of the derivatives to inhibit the growth of test-microorganisms was carried out by empirical method. Molecular structural characteristics of arylaliphatic aminoalcohols (surface area, volume, partition coefficient logP and dipole moment) were calculated by means of «Hyperchem 8.0.8» software. Relationship between the antimicrobial activity against Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Candida albicans and molecular characteristics was investigated by correlation analysis using the Spearman test. Statistical processing was performed by «StatSoft Statistica 6.0», the data obtained were evaluated using Chaddock scale.

The data obtained suggest, that the presence of both antibacterial and antifungal activity in arylaliphatic aminoalcohols depends on the amino group structure and composition of aryl(alkyl)oxy-radical (4-(1,1,3,3-tetramethylbutyl)phenyl, 1-adamantyl, 4-(1-adamantyl)phenyl, 4-phenyl-phenyl or 2,4-ditretbutyl phenyl). The correlation analysis revealed an inverse relationship between the antimicrobial action and surface area, volume, and lipophilicity of compounds. The tightest correlation was found between these parameters and antistaphylococcal activity. Our results indicate the promises of the synthesis, directed to the reducing of the molecule size and lipophilicity of tetramethylbutylphenyl aminoalcohols, for further development of broad-spectrum antimicrobial agents.
AN IMAGE PROCESSING RESEARCH CONSISTENT WITH STANDARD PHOTOGRAPHS TO DETERMINE PILLING GRADE OF WOVEN FABRICS
Authors: TELLİ Abdurrahman
Published: September 2019

In this study, MATLAB 2018a software was used
to evaluate pilling grade of woven fabrics objectively. Experimental works were
carried out on the EMPA W3 standard photographs and accordingly two woven
fabrics. Equations were built based on the measurements of pill characteristics
and textural parameters of these photographs with the help of curve fitting
method after image processing steps. Intervals were generated for each fabric
by using slope of these equations and quantitative parameters obtained from the
original fabric. Furthermore, fabrics that were provided pilling formation at
different test turns were evaluated subjectively by expert operators. Objective
results corresponding to each parameter were analyzed comparatively with these
subjective results. The developed method was successful by using mean of matrix elements
from textural parameters and total area from pill characteristics.
Invasive plants of the Kampinos National Park outskirts – the current state and threats to the protected area
Authors: BOMANOWSKA ANNA , KIRPLUK IZABELLA , OTRĘBA ANNA
Published: September 2019

Studies aimed at the identification of the range and the ways of spread of invasive alien plants in the Kampinos National Park (KNP) outskirts were carried out between 2012 and mid 2018. Special emphasis was placed on surveying the sites of the invasive species and diagnosing potential threats posed to the natural and semi-natural vegetation of the national park by them in rural areas. A floristic survey was carried out on the majority (93 localities) of settlement areas in the vicinity of KNP, in its buffer zone, frequently near the border of the park. Thirty-nine invasive taxa were found which may potentially pose a threat to the ecosystems of KNP. The most frequently identified species included trees and shrubs: Acer negundo, Rhus typhina, Robinia pseudoacacia, Partenocissuss inserta, and herbaceous plants: Conyza canadensis, Erigeron annuus, Solidago serotinoides, S. canadensis. Species encroaching from the settlement areas to semi-natural and natural communities include Bidens frondosa, Echinocystis lobata, Impatiens glandulifera, I. parviflora, Juncus tenuis, Lupinus polyphyllus, Reynoutria japonica, R. xbohemica and Solidago serotinoides. Most of them are species from the highest (III and IV) classes of invasiveness in Poland. The close distance to the Warsaw conurbation, and the road network developed around KNP has certainly affected the number of alien species recorded in the analysed area. Urbanized lands neighbouring the Park are still probably a source from where alien plants disperse to the protected area.