bluuebunny/crossref_metadata_2025 huggingface dataset:
ANALISIS PARTISIPASI MASYARAKAT TERHADAP PEMBANGUNAN PLTMH BAYANG JANIAH IV NAGARI BAYANG UTARA, KABUPATEN PESISIR SELATAN
Authors: Lalan Helny
Published: March 2019

Pembangunan Infrastuktur PLTMH sedang gencar dilaksanakan di Sumatera Barat. Khususnya di Kabupaten Pesisir Selatan di mana telah teridentifikasi sebanyak 26 titik potensi dari 11 sungai besar dan 7 sungai kecil. Sebanyak 16 titik potensi telah dibangun PLTMH dengan 7 unit yang masih aktif, salah satu diantaranya adalah PLTMH unit Bayang Janiah yang terletak di Kecamatan IV Nagari Bayang Utara, Kabupaten Pesisir Selatan. Keberhasilan pembangunan infrastruktur di daerah akan berkelangsungan dengan baik jika ada partisipasi dari masyarakat. Selain itu ketersediaan air telah diukur dalam penelitian sebelumnya. Dalam penelitian ini akan dilakukan pengukuran tingkat partisipasi masyarakat dengan tujuan mengetahui seberapa besar tingkat partisipasi masyarakat dalam mendukung kegiatan pembangunan PLTMH Bayang Janiah. Untuk mencapai tujuan tersebut maka dilakukan pengumpulan data dengan metode kuesioner pada 38 responden. Kuesioner tersebut menggunakan penilaian skala linket. Ada 4 tahapan pembangunan yang dianailisis yaitu tahap perencanaan, pelaksanaan, pengelolaan dan operasional serta monitoring dan evaluasi. Untuk pengolahan dan analisis data digunakan metode analisis menurut Nasir (2003) untuk mendapatkan tingkat partisipasi masyarakat dan Sugiyono (2008) unutk mendapatkan tingkat keaktifan masyarakat dalam berpartisipasi. Hasil penelitian menyimpulkan bahwa tingkat partisipasi masyarakat pada pembangunan PLTMH tinggi di mana presentase partisipasi lebih dari 65%. Tahap pengelolaan dan operasional merupakan bagian dengan tingkat partisipasi masyarakat tertinggi. Tingkat keaktifan masyarakat, bersifat positif yang artinya masyarakat aktif dalam pembangunan PLTMH. Hal ini yang menyebabkan hingga saat ini, PLTMH Bayang Janiah masih beroperasi dan melayani kebutuhan listrik masyarakat Bayang Janiah Koto Ranah Kecamatan Bayang Utara, Kabupaten Pesisir Selatan.
ANALISA STATUS DAN KONDISI PADANG LAMUN DI KAWASAN PANTAIPANTAI WISATA KOTA PADANG
Authors: Amrullah Mohd. Yusuf , Roza Sri Yenica
Published: March 2019

Ekosistem padang lamun merupakan salah satu potensi sumberdaya pesisir yang dimiliki oleh Kota Padang. Penelitian ini dilaksanakan di Pantai Gunuang Cindakir dan Pantai Nirwana. Tujuan penelitian ini adalah menganalisis kondisi dan status ekosistem padang lamun yang berada di pantaipantai wisata Kota Padang. Adapun metode penelitian ini dilakukan melalui observasi, perhitungan dan pengukuran di lapangan. Pada lokasi penelitian hanya ditemukan satu jenis saja yaitu Thalassia hemprichii dimana tutupan padang lamun, di mana persentase tutupan lamun didapatkan sebesar 13,3�10,5% di Pantai Gunuang Cindakir dan Pantai Nirwana sebesar 13,73�12,99%. Pada kedua lokasi penelitian berada pada kategori rendah (0-25%) dengan kondisi padang lamun adalah miskin (29,9%).
IDENTIFIKASI KESERAGAMAN IKAN GARIANG (GENUS Tor) DI LUBUK LARANGAN BATANG ULAKAN KABUPATEN PADANG PARIAMAN
Authors: M Endryeni , Amrullah Mohd. Yusuf
Published: March 2019

Ikan gariang (Genus Tor) merupakan ikan air tawar lokal di Sumatera Barat dan termasuk ikan yang terancam punah. Upaya konservasi harus dilakukan, salah satunya adalah dengan penentuan jenis spesies ikan garing berdasarkan pendekatan fenetik. Penelitian ini bertujuan untuk mengetahui jenis spesies, klasifikasi serta keseragaman ikan garing yang terdapat di lubuk larangan Batang Ulakan, Kabupaten Padang Pariaman Sumatera Barat. Pengambilan contoh ikan dilakukan secara purposive sampling sebanyak 30 ekor. Pengukuran specimen dengan menggunakan jangka sorong dengan ketelitian 0,01 dengan 4 karakter meristik dan 19 karakter morfometrik dan untuk melihat keseragaman spesies antar specimen menggunakan indeks perbandingan karakter morfometrik, karakter khusus penentu spesies di antara ikan Genus Tor adalah keberadaan dan ukuran cuping pada bibir bawah. Hasil penelitian menunjukan spesimen memiliki cuping bibir bawah tidak mencapai sudut mulut ini merupakan ciri kharakter khusus untuk ikan Genus Tor dengan spesies Tor Douronensis. Data yang diperoleh dianalisis dengan One way ANOVA, hasil penelitian menunjukkan bahwa tidak ada perbedaan yang significant (P<0,005) pada ikan gariang antar lubuk larangan yang terdapat di Batang Ulakan. Hal ini menandakan bahwa ikan lubuk larangan Batang Ulakan, Kabupaten Padang Pariaman Sumatera Barat, merupakan speseis yang sama.
STRATEGI PENGEMBANGAN AGROINDUSTRI SUSU MURNI KAMBING DI KECAMATAN WARINGIN KURUNG KABUPATEN SERANG
Authors: Untirta Suherman , Dina Marisa , Astuti Andjar
Published: March 2019

Penelitian ini bertujuan untuk mengidentifikasi faktor internal dan eksternal, mengetahui strategi alternatif yang dapat diterapkan dalam mengembangkan pasar susu kambing murni di PT Jawara Banten Farms. Metode yang digunakan dalam penelitian ini adalah metode survei ke lokasi penelitian yang sengaja ditentukan, terletak di Kabupaten Waringinkurung-Serang, Banten. Jenis data yang digunakan adalah data primer dan sekunder. Metode analisis data adalah (1) matriks IFE dan EFE (2) matriks IE dan (3) matriks SWOT. Hasil penelitian menunjukkan bahwa: Kekuatan utama dalam mengembangkan pasar susu kambing murni adalah pemilik yang aktif dalam mengikuti pameran bisnis. Dan kelemahan utamanya adalah belum efektifnya promosi secara online. Faktor peluang adalah adanya peluang pasar di negara tersebut, dan ancaman yang perlu dihadapi adalah teknologi pesaing yang lebih canggih dan harga yang lebih rendah. Pengembangan strategi alternatif dari strategi SO yang dapat diterapkan dalam mengembangkan pasar susu kambing murni di PT Jawara Banten Farm adalah Mempertahankan citra produk yang baik, Memanfaatkan peran sumber daya di berbagai acara atau seminar untuk mempromosikan bisnis dan produk untuk mengembangkan bisnis, Menambah inovasi produk dengan memberikan berbagai rasa yang menargetkan semua tingkat konsumen, memperluas jaringan dari kerjasama dengan berbagai kafe dan supermarket, pengembangan pasar atau pengenalan produk dimaksimalkan.
RANCANGAN BANGUN KONTROL ARUS RAMP COMPARISON CURRENT CONTROL UNTUK INVERTER SATU FASA PADA PEMBANGKIT LISTRIK TENAGA SURYA
Authors: Nazif Hazlif
Published: March 2019

Dalam penelitian ini, rangkaian kontrol arus ramp comparison current control dibuat dan dianalisa pada sebuah inverter Pembangkit Listrik Tenaga Surya (PLTS). Prototype kontrol arus ramp comparison current control dibuat menggunakan komponen-komponen elektronik. Rangkaian kontrol arus ramp comparison current control yang telah berhasil dibuat sesuai dengan teori. Hasil pengujian dari rangkaian kontrol arus tersebut menunjukkan bahwa nilai THD arus dan THD tegangan tidak sesuai dengan standar IEEE 519-1992. Kontrol arus ramp comparison current control diuji dengan memvariasikan frekuensi atau amplitudo gelombang segitiga sebagai sinyal pemodulasi kontrol arus ramp. Untuk setiap frekuensi dan amplitudo tersebut, kualitas arus keluaran dianalisis dengan melihat distorsi arus yang dihasilkan. Dari hasil pengujian menunjukkan untuk frekuensi gelombang segitiga sebesar 140 Hz, diperoleh THD arus sebesar 51.69%, sementara untuk frekuensi 200 Hz, THD yang diperoleh adalah sebesar 66.19%. Nilai-nilai ini menunjukkan bahwa semakin besar switching frekuensi gelombang segitiga yang diterapkan, maka kualitas arus yang dihasilkan semakin buruk (tinggi distorsi). Sementara itu, pengaruh amplitudo gelombang segitiga menunjukkan semakin tinggi amplitudo gelombang segitiga semakin buruk kualitas daya arus output yang diperoleh, untuk amplitude gelombang sebesar 0.6 Volt pada frekwensi gelombang tetap 140 Hz, THD arus yang dihasilkan adalah sebesar 55%, sementara untuk amplitudo sebesar 0.8 Volt, THD arus yang dihasilkan adalah sebesar 60%.
ANALISIS KEBERANJUTAN USAHATANI PADI VARIETAS KURIAK KUSUIK DI KABUPATEN AGAM, SUMATERA BARAT
Authors: Ayesha Ivonne
Published: March 2019

Padi Kuriak Kusuik sebagai komoditas unggul spesifik lokal, semakin berkurang produksi akibat rendahnya produktivitas dan berkurangnya lahan. Keberlanjutan usahatani padi Kuruik Kusuik perlu diupayakan. Untuk itu dilakukan penelitian dengan tujuan menentukan tingkat keberlanjutan usahatani padi Kuriak Kusuik di Nagari Koto Tangah, Kabupaten Agam, Sumatera Barat. Penentuan lokasi dilakukan secara purposive sampling (sengaja), berdasarkan pemikiran bahwa daerah tersebut memiliki karakter yang erat hubungannya dengan masalah yang diteliti, sehingga cukup relevan dengan tujuan penelitian ini. Data yang digunakan adalah data primer dan sekunder. Data primer merupakan data utama yang diperoleh melalui pengamatan langsung di lapangan (observasi) dan hasil wawancara mendalam (in depth interview) dengan petani, kelompok tani dan. Informan dipilih menggunakan purposive sampling dan identifikasi stakeholders dilakukan dengan metode snowball sampling. Hasil penetian menemukan bahwa 1) Indeks keberlanjutan usahatani padi Kuriak Kusuik untuk aspek biofisik dikategorikan kurang berlanjut dengan nilai 47,12 persen, aspek sosial dan aspek ekonomi cukup berlanjut dengan nilai masing-masing 69,79 persen dan 70,47 persen; 2) Pencapaian indeks keberlanjutan usahatani padi Kuriak Kusuik termasuk pada kategori cukup berlanjut dengan nilai 55,51 persen.
Laboratory preparation and quality control of medicinal composition based on nanosilica and polymethylsiloxane
Authors: Chornoknyzhnyj S. I. , Cheplyaka O. M. , Gerashchenko I. I.
Published: March 2019

The prepared ex tempore adsorption composition which consists of nanosilica, polymethylsiloxane, metronidazole and decamethoxin serves as an effective mean for the topical treatment of wounds.

The aim of the study was the development of an optimal pathway for laboratory manufacturing and quality control of this drug.

We used the method of mechanochemical treatment in a ball mill, chemical methods of identification, absorption spectrophotometry in the IR, UV and visible regions, and the method of sowing on plates to determine microbiological purity.

To obtain a uniform powder composition capable wettable in aqueous medium, there is provided a three-step process comprising mechanosorption of metronidazole on nanosilica and, accordingly, of decametoxin – at polymethylsiloxane. The conditions of identification tests and assay of the ingredients of the composition were сlarified and optimized. It was found that microbiological purity of the composition does not yield to known drugs which intended for topical application. Total adsorption activity of the nanocomposition is stated on the absorption of methylene blue, special protein adsorption activity – on the binding of gelatin. The obtained results may be useful for the organization of the recent pharmacy and the future factory production of proposed nanocomposition.
Active pharmaceutical ingredients in dermatological medicines of Ukrainian pharmaceutical market
Authors: Vlasenko I. O. , Davtian L. L.
Published: March 2019

The problem of the diabetic foot is one of the most serious complications of diabetes mellitus. There is still an active search for medicines (drugs) that could be used in the complex treatment of trophic lesions in diabetic foot. The period before the development and launch of the drug into the pharmaceutical market need to make marketing research aimed at ensuring that the future drug is competitive.

The purpose of the work was to analyze the market of dermatological drugs for the treatment of trophic ulcers in order to determine the marketing opportunities for domestic producers.

The research objects were active pharmaceutical ingredients (APIs), which are part of the dermatological registered drugs in Ukraine. Materials for research were official sources of information about drugs registered in Ukraine. Marketing analytical methods were used. To determine the level of tension between manufacturers and the same product, the coefficient of tension.

Number of D preparations registered in Ukraine ‒ 452 trade names (January 2018) was established. Medicines wich prodused by Ukraine are slightly higher (55.3%). In groups D01, D03, D06, D07 and D08 the highest number of APIs is determined, which is 25, 36, 33, 29 and 30, respectively.

Part API is contained in the drug in combination with other API. In the D01 group, only a small amount of API ‒ 7 is present in combination with other substances, and in group D02 ‒ 6, certain APIs are part of the combined drug. In preparations of D03 4 API are in combination. In group D06, 12 APIs are contained in combination drugs. Most of the established API groups D07 (13) are found in the drug in combination. In the D08 group, part of the API (8) is part of a combined drug. There is a combination of APIs antiseptic or antimicrobial activity, anti-inflammatory effect, local anesthetic and wound healing effect. According to the results of the calculation of the tension indices between the manufacturers of analogues of drugs in group D, the highest competition (Kvi ≥ 0.800) was observed in the groups D01 and D03 (for 4 drugs with Kvi ≥ 0.800), D06 (3 drugs), D07 (8 drugs), D08 (7 drugs). An analysis of the competitiveness of analogue manufacturers has shown that Ukrainian manufacturers are not sufficiently competing in the production of modern analogues of dermatological drugs.
Analysis of the availability of medicines for the treatment of servicemen with injury and wound of the brain
Authors: Shmatenko О. P. , Osedlo G. V. , Vlasenko O. M. , Pleshkova O. V.
Published: March 2019

The most important areas that determine the effectiveness of the medical support system at all stages of providing medical assistance to servicemen is the rational use and availability of medicines and pharmaceutical assistance in general. Under the influence of the situation in eastern Ukraine, the instability of the market economy, the existing budget deficit for the military medical service, the availability of certain groups of drugs is of particular relevance, which fully applies to drugs for the pharmacotherapy of injuries and brain injuries.

The purpose of the study is to analyze the availability of medicines for pharmacotherapy of injuries and wounds of the brain.

In conducting the study, the following methods of analysis were used: system-review, bibliographic and marketing.

Analysis of scientific literature data showed that for pharmacotherapy of craniocerebral wounds and injuries such groups of drugs as psychoanaleptics (N06), blood substitutes and perfusion solutions (B05), peripheral vasodilators (C04), calcium antagonists (C08), analgesics (N02) are used. and psycholeptic drugs (N05), etc., which counted 1 300 trade names of drugs.

The analysis of the pharmaceutical market in recent years has allowed us to single out three main factors (index) affecting the growth of expenditures on drug provision for servicemen, the replacement index; inflation index; innovation index

Analyzing the availability of drugs by price proposals, it was found that the number of inaccessible drugs decreased within five years by more than 30% and amounts to 7.93% or 103 drugs from the total range of drugs for medical support of servicemen with injury and wound of the brain. That is why it is advisable to conclude that the replacement index has almost no effect on reducing the level of drug costs for servicemen/

In the study of the inflation index, it was found that the pricing of domestic drugs depends on the level of inflation, the cost of foreign-made drugs is in direct proportion to the growth of the dollar.

Analysis of the innovation index of the domestic drug market for medical support of servicemen with injury and wound of the brain showed that only 77 original drugs are used for pharmacotherapy, which is 5.92% of the total number of drugs.
Study on the influence of excipients on pharmaco-technological properties of tablet cores of dexketoprofen
Authors: Shoshmina O.V. , Gureyeva S. N. , Vronska L. V.
Published: March 2019

Among the group of nonsteroidal anti-inflammatory drugs, the active substance dexketoprofen trometamol is released. Its pharmacological and pharmacological and technological characteristics are induced in the article. The feasibility of using the wet granulation method in the development of tablets with dexketoprofen is substantiated.

The purpose of this work was selecting the optimal excipients for obtaining a high-quality medicinal product.

The excipients were selected and grouped into 4 functional groups. For the planning of the experiment, a matrix was based on the hyper-Greek-Latin parallelepiped. The tablets were prepared by wet granulation. The effect of the excipients for the granulate, tablet mass and core tablets was studied by such factors as loss on during of the granulate, bulk density of the tablet mass, resistance to crushing, friability, disintegration. The experimental data were subjected to statistical analysis by the method of dispersion analysis. The results were expressed using ranked rows of benefits and bar charts.

The results of the study of the effect of excipients from groups of fillers, disintegrants, sliding, binding substances on the quality of granulate, tablet mass and tablet cores are provided.

The results of the study show that the loss on drying is most influenced by fillers. The quality of the tablet mass depends more on the solution used for wetting, so the nature of the binder and the method of moistening have a determining effect on the bulk density of the tablet mass. Fillers have the most significant effect on the resistance to crushing of the core tablets. The hardness of the dexketoprofen tablet cores characterizes friability, the leading position on the influence is occupied by a group of disintegrants, namely: a mixture of sodium starch and corn starch. The most significant influence on disintegration is exerted by a binder and a moistening method.

The generalized results of the study showed that leaders from the four groups of the excipients are appeared by the influence on the technological indicators of granulate, tablet mass and tablet cores.

In the result of the work the excipients were selected for development of the composition of the tablet cores, their influence on the pharmaco- technological indicators was also investigated. The excipients were selected for further optimization of the composition of the tablets with dexketoprofen, namely: MCC 102, a mixture of sodium starch glycolate and corn starch, corn starch and the use of a 40% dexketoprofen trometamol.
Presentation optimization of research results using the accidential balance method and influence factors that have different equivalents of measurement
Authors: Revyatskyy I. , Barchuk O.
Published: March 2019

The results obtained based on the random balance method are usually presented using scattering diagrams. Their number corresponds to the number of criteria for evaluation, since both impact factors and evaluation criteria can be measured by different units or their values may fall into different ranges of one scale of measurement. In addition, the evaluation criteria may have acceptable limits, and the results obtained in the study may be beyond them. Based on these diagrams it is not convenient to compare the results obtained with each other. Therefore, the aim of the work was to optimize the visual presentation of the results of the study using the random balance method with the factors of influence having different units of measurement, using relative values and their presentation in the same diagram similar to the presentation of the results obtained based on sensitivity analysis.

In the study were analyzed the methods of graphical presentation of results obtained based on the sensitivity analysis and method of random balance, as well as approaches to the construction of diagrams in the MS Excel spreadsheets. The study's objects were the scattering diagrams of the results of the original study. These diagrams showed the influence of quantitative factors (the amount of excipients) on the quality indicators of tablets (time of disintegration of tablets and the resistance to crushing of tablets). The original study was the development of optimal composition and technology of the tablets by direct compression. The composition of tablets was: extract of bilberry leaves and goat’s rue herb and taurine.

We analyzed the construction of matrices of changes in the magnitude of the factors of influence and the values of points along the abscissa axis for constructing a scattering diagram. We substantiated the expediency of using the relative value for the construction of a single diagram for the presentation of all the results of the influence of factors on the criteria of evaluation. The process of constructing a chart based on the type of “histogram with accumulation” is described. The algorithms of construction of data series diagrams (as data sources of the diagram), their representation and methods of calculation of their values are presented. It was proposed to present the series of data using certain graphic images, rather than color shading. This approach allows to see the vector dependence of the change in the value of the criterion on the magnitude of the factor of influence graphically.

The proposed method allows to present on the one diagram the influence of various factors (with different units of measurement or different ranges of values) on several different evaluation criteria, as well as the result of this influence in relation to the admissible limits (standards) of the evaluation criteria.
Analysis of antiviral use efficiency criteria in the complex pharmacotherapy of community acquired pneumonia
Authors: Soloviov S. O. , Dziublyk I. V. , Trokhymchuk V. V.
Published: March 2019

According to modern view, bacterial pathogens are the leading and most common cause of community-acquired pneumonia (CAP), but at the same time the results of numerous microbiological studies conducted in recent years showed that viruses confidently play the next leading role of CAP causes. Today, antiviral therapy is successfully used within the complex therapy of respiratory diseases, which allows reduction of the disease severity and minimizes the risk of complications. The main requirements for the antiviral drug are fully responsive to the new antiviral drug vitaglutam, the active component of which is pentanedioic acid imidazolyl ethanamide, is a low molecular weight compound, an analogue of the natural peptidoamine.

The aim of the work. Mathematical modeling and analysis of clinical and laboratory indicators dynamics of CAP with additional antiviral pharmacotherapy based on pentanedioic acid imidazolyl ethanamide.

In the study, it was used retrospective data of 106 patients with mild form of CAP of viral and bacterial etiology. Patients were randomly divided into two groups. In the 1st main group (50 patients), antibacterial therapy was combined with the antiviral drug vitaglutam. Analysis of antiviral therapy efficiency was provided by grouping of patients and determination of their distribution by gradations of clinical and laboratory indicators, as well as the construction of a mathematical model of their dynamics.

According to modeling results, the rate of body temperature normalization, which was higher in patients taking vitaglutam, was a clear criterion for the efficiency of antiviral therapy. With additional antiviral therapy, the dynamics of sputum in the lungs was less intense. Positive clinical changes were accompanied by an improvement in the clinical blood analysis indicators, namely, more significant was the dynamics of ESR decrease. At the same time, dynamics of leukocytes number in patients’ blood was approximately the same in both groups.

Analysis of dynamics of clinical and laboratory indicators using the proposed mathematical model suggests that additional prescription of vitaglutam to empirical stepwise antibiotic therapy can significantly reduce the time to achieve clinical and laboratory results of treatment of patients with CAP of viral and bacterial etiology.
Synthesis and physical-chemical properties of 8-bromo-3-methyl-7-α-methylbenzylxanthine derivatives
Authors: Ivanchenko D. G.
Published: March 2019

The level of modern pharmaceutical science development is determined by the introduction in medical practice of new effective and non-toxic drugs. The problem of new drugs search depends on the presence in the arsenal of pharmacologists significant amount of original and promising bioactive compounds. In this aspect a special role is given to synthetic compounds of natural origin, which are successfully used in medical practice. Recent researches of national and foreign scientists suggest significant perspective synthetic xanthine derivatives in the creation of new drugs with various effects.

The aim of this paper is synthesis of 8-bromo-3-methyl-7-α-methylbenzylxanthine derivatives, unspecified in scientific papers earlier, and to study their physical and chemical properties.

The melting point has been determined by open capillary method on the device PTP (M). Elemental analysis has been performed on the device Elementar Vario L cube. NMR spectra have been taken using spectrometer Bruker SF-200.

Synthesis of 8-bromo-3-methyl-7-α-methylbenzylxanthine was performed through boiling of 8-bromo-3-methylxanthine together with α-methylbenzylchloride. Having applied the reaction of the latter with an excess of a primary or secondary heterocyclic amine in the methoxyethanol environment, a range of corresponding 8-aminosubstituted 3-methylxanthine has been obtained. The heating of initial syntone with an excess of hydrazine hydrate in aqueous dioxane environment leads to the formation of 8-hydrazinoxanthine. Corresponding 8-(indolon-2-ylidene-3)-hydrazinoxanthines have been obtained through short-time heating up 8-hydrazinoxanthine with N-substituted isatin in aqueous dioxane environment. Structure of synthesized compounds has been definitely proved by NMR-spectroscopy.

Simple laboratory method has been elaborated to synthesize 8-bromo-3-methyl-7-α-methylbenzylxanthine, which is initial compound for further chemical modification of xanthine molecule. Reactions of 8-bromo-3-methyl-7-α-methylbenzylxanthine with N-containing nucleophiles have been investigated. This allowed to obtain the previously undescribed 8-amino- and 8-hydrazinosubstituted 3-methyl-7-α-methylbenzylxanthine. Physical and chemical properties of new synthesized compounds have been studied. A synthetic perspective of the obtained substances has been shown.
Study acute toxicity of 4-(R-amino)-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazole-3-thiol in vivo
Authors: Safonov A. A.
Published: March 2019

Typically, the system is already known are used as the core for a new substance, which have already proved themselves as potential drugs. So one of these is 1,2,4-triazole ring.

The purpose was to study acute toxicity of 4-((R-iden)amino)-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazole-3-thiols and identify possible patterns acute toxicity of the chemical structure of indicators derivatives. In the study of acute contact toxicity was used spreadsheet rapid method for Prozorovsky V. B.

Analysis of the results of studies acute toxicity of 1,2,4-triazole derivatives showed that all substances are relate to the 4th class of toxicity according to K. K. Sidorov. Their toxicity is in the range 357 ± 28–1 250 ± 220 mg/kg.

Introduction in a molecule 4-amino-5-(thiophene-2-ylmethyl)-4H-1,2,4-triazole-3-thiol nitrobenzylidene, dimethylaminobenzylidene, 2-chloro-6-fluorobenzylidene substituent leads to a reduction of acute toxicity to the 566–576 mg/kg. Replacement of 2-chloro-6-fluorobenzylidene radical in a molecule 4-((2-chloro-6-fluorobenzylidene)amino)-5-(thiophene-2-ylmethyl)-4H-1,2,4-triazole-3-thiol at 4-fluorobenzylidene, 3,4-difluorobenzylidene, 4-methoxybenzylidene, 3,5-dimethoxybenzylidene leads to further reduce toxicity.

Introduction methyl radical in a molecule 4-(benzylidene)amino)-5-(thiophene-2-ylmethyl)-4H-1,2,4-triazole-3-thiol and 4-((4-fluorobenzylidene)amino)-5-(thiophene-2-ylmethyl)-4H-1,2,4-triazole-3-thiol resulting to increased toxicity.

It was established that the most toxic substance among the test compounds is 4-amino-5-(thiophen-2-ylmethyl)-4H-1,2,4-triazole-3-thiol. Its LD50 is 357 ± 28 mg/kg and the least toxic compound 4-((3,4-difluorbenzylidene)amino)-5-(thiophen-2-ilmethyl)-4H-1,2,4-triazole-3-thiol, LD50 1 250 ± 220 mg/kg.
Development of recommendations on creating local formulary drug list for children affected with gastritis and duodenitis
Authors: Trokhymchuk V. V. , Vyshnytska I. V.
Published: March 2019

An urgent task is to carry out regular quality control  and rational prescribing of drugs, changes to the drug formulary lists for the purpose of positive influence on the processes of pharmaceutical provision, especially children affected with gastritis and duodenitis.

The aim of the work was to create a list of the recommended groups of drugs for further development of the local insurance and formulary drug lists used for treatment of children with gastritis and duodenitis using modern information technologies. Methods of peer reviews, questionnaires, direct observation, modeling, and information analysis were used in the process. The objects of study were regulatory and legislative documents, medication treatments sheets, price lists of wholesale pharmaceutical companies, forms of expert assessments.

Science-based guidelines for the assessment of the economic costs for the inclusion of medicines in local formulary drug lists of health care institutions to help children with gastritis and duodenitis in the acute stage, in specialized hospitals, taking into account peculiarities of the disease under study at the regional level were formed.

According to the results of a comprehensive study of pharmaceutical provision for treatment of children with gastritis and duodenitis, in addition to an expert evaluation of medicines, recommendations for the creation of a local formulary drug list were made and recommended list of drug groups was determined by 15 INN drugs to be used in the development of a local drug formulary list for pharmacotherapy of the pathology under study.
Synthesis and biological properties of 7-(2-hydroxy-3-m-ethylphenoxypropyl-1-)theophilline derivatives
Authors: Ivanchenko D. G.
Published: March 2019

Various origin antibiotics and many other chemotherapeutic agents, which are based on the heterocyclic compound, found wide application in the treatment of infectious diseases. Purine derivatives have long been used in medical practice as antiviral agents (acyclovir, gancyclovir, etc.), and further research to find new antimicrobial and antiviral agents in the row of purine derivatives are justified and perspective.

The aim of this paper is to elaborate simple laboratory methods of 7,8-disubstituted theophylline synthesis, unspecified in scientific papers earlier, and to study their physical and chemical properties.

The melting point has been determined by open capillary method on the device PTP (M). Elemental analysis has been performed on the device Elementar Vario L cube. NMR spectra have been taken using spectrometer Bruker SF-400.

For the initial screening study of the newly-synthesized substances benchmark testing-cultures of both gram-positive and gram-negative bacteria have been used, which belong to clinically significant groups of infections agents which are differing by their morpho-physiological properties.

Heating of 8-bromotheophilline with m-ethylphenoxymethyloxyrane in propanol-1 environment results in formation of 8-bromo-7-(2-hydroxy-3-m-ethylphenoxypropyl-1-)theophylline. Its reactions with primary and secondary amines proceed at boiling in aqueous dioxane environment to form the corresponding 8-aminoderivatives. The heating of initial syntone with 2-ethylpiperidine leads to the formation of oxazoline xanthine.

By applying such computer programs as ALOGPS, DRAGON, GUSAR and ACD/Percepta Platform was established viability of further biological and toxicological in vitro and in vivo research.

Simple laboratory method has been elaborated to synthesize 8-bromo-7-(2-hydroxy-3-m-ethylphenoxypropyl-1-)theophylline, which is initial compound for further synthesis of various theophylline N-, O-, S-substituted.

Reactions of 8-bromo-7-(2-hydroxy-3-m-ethylphenoxypropyl-1-)theophylline with primary and secondary amines have been investigated. As a result 8-aminosubstituted of 7-(2-hydroxy-3-m-ethylphenoxypropyl-1-)theophylline and 6,8-dimethyl-2-m-ethylphenoxymethyl-2,3-dihydro-1,3-oxazolo[2,3-f]theophylline have been synthesized. NMR-spectral characteristics of new synthesized compounds have been studied.

Molecular and pharmacological descriptors (LogP, TPSA, A) to forecast properties of the obtained substances have been calculated, in addition to acute toxicity index. The perspective of the obtained substances using as antistaphylococcal and antifungal agents has been shown.
Development of emulgel technology with saw palmetto extracts and of japanese sophora tincture for androgenetic alopecia treatment
Authors: Yarema I. O. , Feodorovska M. I. , Polovkо N. P.
Published: March 2019

Androgenic alopecia is a hair disease caused by an excessive influence of androgens on hair follicles, whose treatment requires long-term use of systemic and / or local action drugs. In Ukrainian pharmaceutical market for the androgenic alopecia treatment synthetic drug minoxidil is presented, which in the local long-term application causes many side effects. Therefore, the drugs development of plant origin is important.

Taking into account of the androgenic alopecia pathogenesis, it was developed the emulgel composition and technology, which has Saw Palmetto extract and Sophora Japonica tincture as active ingredients. Their main biological active substances applying topically provide anti-androgenic, venotonic and follicles protective action.

The qualities of dermatological remedies in large measure are influenced by their technological process. Therefore, the purpose of this investigation was the development of a rational emulgel technology with Saw Palmetto extract and Sophora Japonica tincture for the androgenic alopecia prevention and treatment.

Samples of emulgel were manufactured with applying of different technological methods, namely: the method of emulsification, temperature, rate and duration of stirring. Prepared samples were controlled by uniformity, dispersion degree (with microscope Delta Optical Genetic Pro, Poland), pH (with pH-meter 150 MI, Russia) and structure viscosity (with rotational viscometer Brookfield VR-3000, Myr VISKOTECH, Spain).

The optimal temperature for the emulgel preparation is 60 °C, since the melting temperature of cetyl alcohol (the most refractory component of the formulation) is 52 °C. When choosing the emulsifying method it was found that sequential addition of hydrophilic and oil phases to emulgators provided the highest dispersion and optimally rheological properties of the emulgel.

The best homogenization speed, providing a high degree of dispersion and structural viscosity in the range 3 200–3 400 mPas, is 2 000 rev/min. The intensive size reduction of the dispersed phase was observed for 30 min stirring.

As a result of investigation, it was established that the best method of emulsification was the sequential adding of oil and aqueous phase to the mixture of emulsifiers at the temperature – 60 °C, the speed – 2 000 rev/min for 30 min.
Synthesis and physicochemical research of some 2-((5-((theophylline-7'-yl)methyl)-4-R-4H-1,2,4-triazole-3-yl)thio)acetohydrazide ylidenderivatives
Authors: Gotsulya A. S. , Knyazevich P. S. , Panasenko O. I. , Knysh Е. G.
Published: March 2019

The rapid development pace of the pharmaceutical science constantly increases the demand for new kind of medicine featured with high biological activity and non-toxicity at the same time. Setting the aim to enlarge the amount of scientific findings in the domain of biologically active substances, 1,2,4-triazole and theophylline were used as the starting material. These compounds form the basis for the majority of drugs, such as diuretics, antifungal and antibacterial medicaments. The combination of heterocycles put under research demonstrate a repeated probability increase in the variety of activities. Therefore, the relevance of the following study is determined by valuable properties of these substances. Besides that, the presence of a hydrazide element accounts for a high probability level of antimicrobial, particularly anti-tuberculosis activity.

 In order to identify optimal conditions for the synthesis and physicochemical property research, 2-((5-((theophylline-7'-yl)methyl)-4-R-4H-1,2,4-triazole-3-yl)thio) acetohydrazide ylidenderivatives were obtained.

The process of production was carried out through long chain reactions, using the sodium salt of theophylline as a substrate. The conversion is well known being described in many papers. Hydrazide was taken as the starting compound. It was dissolved in water-alcoholic medium while separately, aldehyde was dissolved or mixed in ethyl alcohol as well. The resulting solutions were decanted. The precipitate formed immediately or after a certain period of time, which is likely due to the state of matter of the starting aldehyde.

10 compounds (light-yellow crystalline materials with sharp melting point) were synthesized after that. Their structures and physicochemical properties were confirmed with modern methods of analysis. It is established that the reaction proceeds rapidly with a yield of 77‒95% in water-alcoholic medium at a temperature of about 80 °C.
Synthesis and structural features of 5-(4-(tert-butyl) phenyl)-4-((R)amino)-4H-1,2,4-triazole-3-thiols
Authors: Aksyonova-Seliuk I. I. , Panasenko O. I. , Knysh E. G.
Published: March 2019

Chemistry of heterocyclic compounds is one of the most popular sector in organic chemistry. Scientists allocate among them a class of derivatives of 1,2,4-triazole. This class of compounds attracts attention his broad spectrum of biological activity. There are antiviral, anti-inflammatory, anti-tubercular, antimicrobial, antioxidant, actoprotective, anti-cancer and other activities. The derivatives of 1,2,4-triazole have one more important advantage. It is low toxicity. This properties do this class of derivatives promising for researches their chemical structure and biological activity and purposeful search of biologically active substances.

The purpose of the work is synthesis of 5-(4-(tert-butyl)phenyl)-4-((R)amino)-4H-1,2,4-triazoles-3-thiols from appropriate ylidene derivatives of 4-amino-5-(4 (tert-butyl)phenyl)-4H-1,2,4-triazoles-3-thiol and research of their physical and chemical properties.

The objects of research were 10 new compounds, derivatives of 4-amino-5-(4-(tert-butyl)phenyl)-4H-1,2,4-triazoles-3-thiol. These compounds are the crystal substances which are odorless, insoluble in water and soluble in organic solvents. Investigation of the physical and chemical properties of this compounds was carried out according to the methods listed in the State Pharmacopoeia of Ukraine. The melting temperature of synthesized compounds was determined by device OptiMelt Stanford Research Systems MPA100. The structure of the compound was confirmed by 1H-NMR spectroscopy (Mercury 400) and gas chromatography-mass spectrometry (Agilent 1260 Infinity HPLC).

10 new compounds, derivatives of 4-amino-5-(4-(tert-butyl)phenyl)-4H-1,2,4-triazoles-3-thiol, were synthesized in a study. The chemical structure of the new compounds was confirmed by modern instrumental methods of analysis. Results of the done work can be use in the future search of biologically active substances.
Study of influence of the surface-active substances concentration on releasing of praziquantel from the rectal suppository
Authors: Romanina D. M. , Berdey I. I. , Gladishev V. V. , Lisyanska G. P.
Published: March 2019

Acne dermatosis (rosacea, perioral dermatitis, seborrheic dermatitis etc.) are one of the most actual problem in dermatology. Praziquantel is an antiparasitic medication effective towards trematodes, cestodes. Investigations developed by domestic scientists revealed antidemodicosis activity of praziquantel. Use of semisolid dosage forms for rectal administration will allow to increase its efficacy and minimize the risks of adverse reactions.

On the department of technology of medications Zaporizhzhia State Medical University research of development of praziquantel rectal dosage form for therapy of acne dermatosis, complicated with demodicosis, and its technology is carried out. As a result of biopharmaceutical investigations it was determined that combination of excipients – the base (confectionary fat 60%, 10% paraffin, 30% cocoa butter) and surfactant (distilled monoglycerides) provides with the optimal praziquantel releasing.

The aim of this work is study of excipient using in manufacturing of suppository (bases and surfactants) influence on the biopharmaceutical characteristics of praziquantel rectal dosage form.

Investigation was carried out by the one-factors dispersive analysis with repeated observations By way of a parameter of optimization praziquantel releasing was chosen as the first step of bioavailability investigation. Praziquantel releasing from suppository was studied by the equilibrium dialysis by Kruvchinsky’s method at temperature 37 ± 0,5 °С through a cellophane semipermeable membrane «Kuprofan» film using Franz diffusion cell apparatus. Ethyl alcohol was chosen as a dialysis medium considering the solubility of praziquantel. Concentration of released praziquantel after 30 minutes of the dialysis was determined by spectrophotometric analysis.

As a result of biopharmaceutical investigation of praziquantel suppositories it was determined that surface-active substances (distilled monoglycerides) concentration has a statistically significant influence on its releasing from rectal dosage form. It was ascertained that 0,5% concentration of distilled monoglycerides provides with the optimal releasing of praziquantel from rectal suppositories.
Synthesis and hypoglycemic activity of 7-n-butyl-3-methyl-8-thioxanthine derivatives
Authors: Romanenko M. I. , Ivanchenko D. G. , Sharapova T. A. , Bilay I. M. , Aleksandrova K. V.
Published: March 2019

According to the International Diabetes Federation in 2015 were registered 59.8 million patients with diabetes in Europe. Synthetic drugs are widely applied in addition to a variety of insulins to normalize blood glucose level. It should be noted that the oral anti-diabetic drugs are the common therapeutic agents for the treatment of diabetes mellitus type II, and therefore the search for new non-toxic hypoglycemic agents is one of the most urgent problems of modern pharmaceutical science. It is known that 7,8-disubstituted xanthine derivatives exhibit hypoglycemic activity.

The aim of this work lies in developing unique method to synthesize undocumented in other scientific papers 7-n-butyl-3-methyl-8-thioxanthine derivatives and also studying of their hypoglycemic activity.

Acute toxicity of synthesized compounds has been studied with the application of Prozorovsky’s method. The glucose homeostasis characteristic has been performed on carbohydrate tolerance that has been determined by the glucose load test on the control group and on the intact rats.

The reactions of 7-n-butyl-3-methyl-8-thioxanthine with benzylchlorides, bromoketones, esters and an amide of chloroacetic acid have been studied. Reactions of mentioned syntons proceed smoothly in aqueous propanol-2 environment and lead to the formation of the corresponding 8-benzyl-, benzoylmethylthioxanthines and xanthinyl-8-thioacetic acid derivatives.

Accessible laboratory method has been elaborated to synthesize unspecified in scientific papers earlier 8-thiosubstituted 7-n-butyl-3-methylxanthine by reacting 7-n-butyl-3-methyl-8-thioxanthine with benzylchlorides, bromoketones, esters and an amide of chloroacetic acid, their structure having been proved by NMR-spectroscopy data. The acute toxicity of synthesized compounds has been studied. It has been established that LD50 is in the range 820–2477 mg/kg, i. e. obtained substances are low-toxic and practically non-toxic according to Sidorov’s classification. Also the study of hypoglycemic activity of synthesized compounds has been carried out. A significant perspective for further research to find the original antidiabetic agents has been shown by bioassay results. It has been found that 7-n-butyl-3-methylxanthinyl-8-thioacetamide is more active than reference substances.
Analisis Pengaturan Standardisasi Produk di Indonesia Ditinjau dari Ketentuan Technical Barriers To Trade (TBT) Agreement
Authors: Sukananda Satria
Published: March 2019

Indonesia sebagai negara anggota World Trade Organization terikat untuk tunduk pada persetujuan-persetujuan multilateral terkait perdagangan internasional termasuk tentang Technical Barriers to Trade (TBT) Agreement. teknis Ketentuan TBT Agreement bekerja melalui tiga konsep yaitu regulasi teknis, standar dan prosedur penilaian kesesuaian dan berlaku untuk semua produk. Standardisasi yang cenderung protektif dapat diterapkan untuk melindungi kepentingan nasional, namun menghambat ekspor Negara-Negara mitra dagang ke Indonesia. Begitu pula sebaliknya, jika program standardisasi diterapkan, aliran barang dan jasa impor akan mengancam kepentingan umum. Rumusan masalah penelitian ini yaitu bagaimana pengaturan dan penerapan standardisasi produk di Indonesia di tinjau dari ketentuan Technical Barriers to Trade (TBT) Agreement serta bagaimana perumusan Standar Nasional Indonesia dan penetapan standar nasional secara wajib. Kajian ini menggunakan metode penelitian hukum normatif pendekatan Perundang-undangan (statue approach). Untuk bahan hukum, penelitian ini menggunakan bahan hukum dan bahan non hukum yang diperoleh dalam penelitian ini akan dianalisis secara preskriptif dengan metode deduktif. Hasil penelitian menunjukkan bahwa pengaturan akan TBT Agreement di Indonesia dituangkan melalui Undang-Undang Nomor 20 Tahun 2014 tentang Standarisasi dan Penilaian Kesesuaian. Penerapan akan standarisasi produk di Indonesia dapat dilakukan secara sukarela maupun wajib. Penerapan Standarisasi secara wajib dapat dilakukan jika menyangkut keperluan melindungi kepentingan umum, keamanan negara, perkembangan ekonomi nasional dan pelestarian fungsi lingkungan hidup. Upaya pengurangan hambatan perdagangan tersebut akan berjalan dengan baik apabila masing-masing negara memberlakukan standar wajib menerapkan Good Regulatory Practices dan melaksanakan notifikasi standarisasi ke WTO sesuai dengan ketentuan TBT Agreement.