bluuebunny/crossref_metadata_2025 huggingface dataset:
DESIGN AND IN VITRO CHARACTERIZATION OF FLOATING TABLETS OF METRONIDAZOLE
Authors: ESWARAIAH M CHINNA , S JAYA
Published: October 2019

Objective: The objective of the present study was to formulate the effervescent floating matrix tablet of metronidazole and to evaluate the effect of varying concentrations of hydrophilic polymers on drug release.

Methods: Drug excipients interaction was studied by Fourier transform infrared spectrophotometer. The effervescent floating matrix tablets were prepared by direct compression technique using hydroxypropyl methylcellulose (HPMCK4) and xanthan gum alone and in combination as release retardants. Microcrystalline cellulose was used as diluent. Sodium bicarbonate was used as effervescent agent. The prepared matrix tablets were evaluated for their physicochemical parameters such as weight variation, hardness, friability, content uniformity, buoyancy time, and in vitro dissolution.

Results: Micromeritic properties and post-compression parameters were evaluated and all the parameters were found within the acceptable limit. The drug release data were subjected to different models to evaluate release kinetics and mechanism of drug release. The matrix tablets prepared with xanthan gum and a mixture of xanthan gum and HPMCK4 were retarded the drug release up to 12 h. The release mechanism of metronidazole was evaluated on the basis of release exponent n value in Peppas model. The n value of the formulations ranged from 0.46 to 0.89 which indicated Case II transport and zero-order release.

Conclusion: Floating matrix tablet is the simple, efficient, and economic method to sustain the release of metronidazole to eradicate Helicobacter pylori in peptic ulcer disease.
ELEMENTAL ANALYSIS OF AYURVEDIC DRUGS (BHASMAS) BY ATOMIC ABSORPTION SPECTROMETER
Authors: A ASHWINI , BR KERUR
Published: October 2019

Objective: Ayurvedic drugs/bhasmas are very potent and promising drugs for the treatment of various ailments. Bhasmas are the multielement samples, and the present work deals the analysis of the concentration of metallic elements in three ayurvedic bhasmas of four different brands, to compare and know the quality of commercial bhasma in market.

Methods: Commercially available abhraka bhasma (AB), mandoor bhasma (MB), and godanti bhasma (GB) in market from four different manufacturing companies were procured, and bhasma sample solution was prepared to analyze the elemental concentrations in bhasma; the solution is subjected to flame atomic absorption spectrometer (FAAS) technique and determined elemental concentration in bhasmas of four different commercial brands.

Results: FAAS analysis explores the presence of Mg, Al, K, Ca, Cr, Mn, Fe, Cu, Zn, Mo, and Cd elements’ concentration in three bhasmas/drugs by four manufacturers. AB is rich in Al and Fe following the other elements in low concentrations, MB is rich in Fe, Ca, Mn, Cu, K, and Al and other elements are present in less quantity, and GB is rich in Ca and all other elements were very less in quantity.

Conclusion: FAAS analysis showed that there is a difference in quantity/concentration of elements present in bhasma, aluminum (Al) is found high in Patanjali brand bhasmas compared to other three brands, and the toxic metal cadmium (Cd) is found in Dhootapapeshwar mandoor bhasma (DMB) (0.0458 mg/l), except DMB, all bhasmas found free from toxic metals, which reveal that there is a variation in quality of bhasmas from different manufacturers, and the elements present in bhasmas are found to be in permissible range for human intakes. As the mineral elements are essential in human diet, if the amount of any elements becomes too high in body, then it can affect the functioning of other important minerals in body causing the severe health problems, so it is must, to balance all nutrients in human diet, either through food or medicines. Hence, the present analysis work focuses on the variation of concentrations of elements present in bhasma of different manufacturers, which will help in practitioners to compare and refer good quality bhasmas or drugs in terms of their ingredients/elements, which plays a major role in functioning of human body normally. Further work is necessary to carry out on bhasmas and ayurvedic formulations in order to get good of diet supplementation.
NEPHROPROTECTIVE ROLE OF ZINC AGAINST THE AMMONIUM SULFATE TOXICITY IN MALE ALBINO RATS
Authors: TEKURI SIVA KUMAR , RANI AMURU SHOBHA , BASSAIAHGARI PURUSOTHAM , GALI YUVARANJANI , PABBARAJU NEERAJA
Published: October 2019

Objective: Intention of the present study is to investigate the protective role of zinc against ammonium sulfate (AS) toxicity in renal tissue by evaluating certain biochemical activities of albino rats.

Methods: Rats were divided into four groups, namely control, ammonia, zinc, and ammonia + zinc. Rats were exposed to AS (18.3 mg/kg body weight) or zinc chloride (4 mg/kg body weight) or both through intraperitoneally for 7-day experimentation with 24-h time interval.

Results: AS-administered rats showed significant increased levels of ammonia, urea, glutamine, glutamine synthetase, free amino acids, and lactate dehydrogenase and decreased levels of total proteins, pyruvate, succinate dehydrogenases, malate dehydrogenase, and biochemical activities when compared with control. Supplementation of zinc mitigated AS-induced oxidative stress and restored all the biochemical parameter activities. Zinc administered to normal rats did not exhibit any significant changes in any of the parameters studied.

Conclusion: From the study, it concluded that zinc cotreatment with AS has effectively recovered the mitochondrial enzyme activities and ammonia metabolic biochemical parameters in renal tissue of rat treated with AS.
PROTECTIVE EFFECT OF ETHANOLIC ROOT EXTRACT OF COMMIPHORA CAUDATA AGAINST DIABETIC-INDUCED RATS IN HIGH-FAT DIET-STREPTOZOTOCIN MODEL
Authors: K ANITHA , LAKSHMI SABAPATHI MOHANA , SV SATYANARAYANA
Published: October 2019

Objective: The present study was to explore the phytochemical analysis and antidiabetic potential of the root of Commiphora caudata in high-fat diet (HFD) streptozotocin-induced diabetic rats.

Methods: The ethanolic root extract of C. caudata at a dose of 400 mg/kg and 200 mg/kg was administered to diabetic rats. Glibenclamide (5 mg/kg) was used as standard drug.

Results: The data were statistically assessed using one-way ANOVA followed by Dennett’s multiple comparison tests. To unfold the mechanism, we studied all the biochemical parameters glucose, total cholesterol, triglycerides (TG), high-density lipoproteins (HDL), low-density lipoproteins (LDL), and very LDL (VLDL) and histopathological examination of the pancreatic tissue section. The ethanolic extracts of root of C. caudata showed significant reduce of the level of cholesterol, TG, LDL, VLDL, and significant increase in the serum level of HDL at 400 mg/kg rather than 200 mg/kg.

Conclusion: Further studies should look into the characterization and isolation of the constituents to know the exact mechanism of hypoglycemic activity. Statistical analyses of this screening method confirm that the proposed method is appropriate and it can be expected to improve basic idea to the researcher who is working in area-like antidiabetic activity.
DEVELOPMENT AND VALIDATION OF HIGH-PERFORMANCE THIN-LAYER CHROMATOGRAPHY METHOD FOR SIMULTANEOUS ESTIMATION OF NEBIVOLOL HYDROCHLORIDE AND CILNIDIPINE
Authors: MINAL R. GHANTE  , ATASHA AKHADE  , PREETI GOTA  , ATUL NIKAM  , SUPRIYA JAGTAP  , VANDANA NIKAM
Published: October 2019

Objective: The proposed method describes method development and validation of nebivolol hydrochloride and cilnidipine in combined pharmaceutical tablet dosage form by high-performance thin-layer chromatography (HPTLC) having adequate specificity, sensitivity, and reproducibility.

Methods: Nebivolol hydrochloride and cilnidipine drug combination is used for the treatment of hypertension. Precoated aluminum plates with silica gel 60 F254 (E-Merck, Germany) were used for the chromatographic separation which was carried using chloroform:glacial acetic acid:methanol, in 8.5:1:0.5 (v/v/v) as a mobile phase. HPTLC separation of two drugs was carried by densitometric measurement at 270 nm.

Reults: The drugs were satisfactorily resolved with retardation factor values of 0.0.29±0.008 and 0.69±0.007 for nebivolol hydrochloride and cilnidipine, respectively. The method was found to be linear in the range of 100–1000 ng/spot and 50–500 ng/spot for nebivolol hydrochloride and cilnidipine, respectively. The correlation coefficient was found to be 0.989 and 0.996 for nebivolol hydrochloride and cilnidipine, respectively. Limit of detection and limit of quantitation values were 16.395 ng/band and 49.681 ng/band and 31.788ng/band and 96.328 ng/band, respectively. The mean recovery was found to be 100.570–101.936 and 100.269–101.333 for nebivolol hydrochloride and cilnidipine, respectively. The intra- and inter-day precision was found to be within the limit.

Conclusion: A simple, accurate, precise, and sensitive HPTLC method has been developed and validated in combined pharmaceutical tablet dosage form for simultaneous estimation of nebivolol hydrochloride and cilnidipine.
PHYTOCONSTITUENTS, PHARMACOLOGICAL ACTIVITY, AND MEDICINAL USE OF LEPIDIUM SATIVUM LINN.: A REVIEW
Authors: CHETNA BAREGAMA  , ANJU GOYAL
Published: October 2019

Herbal medicines are in nice demand within the developed additionally as developing countries for primary aid due to their wide biological and medicative activities, higher safety margins, and lesser prices. Lepidium sativum Linn. (Brassicaceae) is annual herb regionally referred to as halon in India, however, usually referred to as garden cress. L. sativum is a fast growing edible plant. Seeds, roots, and leaves of garden cress have economic importance; however, the crop is especially cultivated for seeds. It is a therapeutic vital herb in India. L. sativum has various pharmacological actions such as antibacterial activity, antifungal activity, antioxidant activity, cytotoxic activity, diuretic activity, hepatoprotective activity, hypoglycemic activity, antiosteoporotic activity, antiasthmatic activity, anti-carcinogenic effect, cardiotonic activity, smooth and skeletal muscles contraction activity, fracture healing property, chemoprotective effects, and hemagglutinating activity. It is used for menstrual cycle regulation, gastrointestinal problems such as diarrhea and constipation and to increase milk production. It is also reported to exhibit antirheumatic activity. It is also used as an immunity booster and brain intellect enhancer agent as traditional medicine. So that this review reveal that L. sativum is a source of medicinally active compounds and have a variety of pharmacological effects. These studies will be helpful to create focus toward L. sativum and may be useful in developing new formulations with more therapeutic and to provide a direction for advance research.
IN VITRO STUDY OF THE BRONCHORELAXATION EFFECT OF COPTOSAPELTA FLAVESCENS KORTH. ROOT’S EXTRACT AND FRACTIONS
Authors: KHEMASILI KOSALA  , MOCH. ARIS WIDODO  , SANARTO SANTOSO  , SETYAWATI SOEHARTO
Published: October 2019

Objective: This study aimed to compare the bronchorelaxation effect of the methanol extract, hexane fraction, ethyl acetate fraction, and methanol fraction of Coptosapelta flavescens Korth. roots (CFRs) on the isolated bronchial rings of guinea pig.
Methods: Research design was experimental in which a 4-mm long bronchus of a male guinea pig was kept in an isolated organ bath containing Krebs-Henseleit solution at 37°C, pH 7.4, and flooded with carbogen gas. The bronchial ring was precontracted with methacholine and then given six doses of C. flavescens Korth. root’s methanol extract (MECFR) solution cumulatively. The extract’s solvent 10% dimethyl sulfoxide ethanol was used as negative control. This procedure was then repeated using CFRs hexane fraction (HFCFR) solution, CFRs ethyl acetate fraction (EAFCFR), and CFRs methanol fraction (MFCFR).
Results: The bronchorelaxation effect of MECFR, MFCFR, EAFCFR, and HFCFR is shown by their dose-response curves (DRCs) which are significantly different compared with the extracts solvent’s DRC. The maximal efficacy (Emax) of MFCFR was the same (p>0.05) as the MECFRs Emax, but the EAFCFRs and HFCFRs Emax were smaller (p<0.05) than the MECFRs Emax.
Conclusion: The bronchorelaxation effect of the MECFR on the guinea pig’s bronchial ring is similar to the CFRs methanol fraction, and is stronger than the CFRs ethyl acetate fraction and CFRs hexane fraction.
NEUROPROTECTIVE AND COGNITIVE ENHANCING EFFECT OF METHANOLIC MORUS ALBA LEAF FRACTION IN U87MG CELL LINES AND EXPERIMENTAL RAT MODEL
Authors: ANJALI RAJ  , SUMIT DEY  , SUBBA RAO VENKATA MADHUNAPANTULA  , MANJULA SN
Published: October 2019

Objective: The present study aims to investigate the protective effect of methanol fraction of Morus alba (MEMA) leaves against hydrogen peroxide (H2O2)-induced U87MG cell toxicity and aluminum fluoride (ALF)-induced rat toxicity.

Methods: The study was divided into in vitro and in vivo sections. U87MG cell lines were pre-treated with different fractions of MEMA for 20 h and further tested against 1000 ϻM of H2O2. The best fraction from in vitro studies was used to study the protective effects against ALF-induced neurotoxicity. Rats were divided i nto five different groups, and MEMA (200 and 400 mg/kg p.o) was administered for 14 days to the animals with α-tocopherol as the standard drug treatment. Behavioral studies were assessed using Barnes maze. The major biochemical measurements included catalase, superoxide dismutase and glutathione reductase, lipid peroxidation (LPO), and acetylcholinesterase (AchE) levels.

Results: In vitro studies indicated MEMA as a potential candidate followed by AQMA and ethyl acetate. The MEMA fraction was able to ameliorate ALF-induced neurotoxicity in the behavioral assessment. The higher antioxidant content in the fraction decreased the LPO levels from 250±4.07 to 115±3.22 as well as elevated the levels of most of the endogenous antioxidant enzyme levels. AchE levels were also decreased to 33.89±0.71 from 38.94±0.64.

Conclusion: Although the results obtained indicate that MEMA could significantly suppress oxidative stress-induced central neuronal damage both in vitro and in vivo, further mechanistic studies are required to delineate its neuroprotective pathway.
QUALITY BY DESIGN APPROACH TO STABILITY-INDICATING REVERSE-PHASE HIGH-PERFORMANCE LIQUID CHROMATOGRAPHY METHOD DEVELOPMENT, OPTIMIZATION, AND VALIDATION FOR THE ESTIMATION OF SIMEPREVIR IN BULK DRUG
Authors: VANITHA C  , SATYANARAYANA SV  , BHASKAR REDDY K
Published: October 2019

Objective: A simple, robust, precise, and selective stability-indicating liquid chromatography (LC) method (reverse-phase high-performance LC) was developed for the estimation of simeprevir through quality by design paradigm.

Methods: The chromatographic separation was performed on Water’s 2695(Alliance) equipped with a photodiode array detector at 300 nm. The method was developed on Discovery C18 column (250×4.6, 5 mm) using orthophosphoric acid and acetonitrile (55:45 % v/v) with the flow rate of 1 ml/min at 30°C. The degradation studies of simeprevir were carried out under the stress conditions of hydrolysis (acid, base, and neutral), oxidation, photolytic, and thermal as per the International Conference on Harmonization (ICH) guidelines. The peroxide hydrolysis shows more critical impurities which were well resolved from pure drug with the application of design of experiment and optimized the method.

Results: Independent variables (critical analytical attributes) selected for the method optimization were mobile phase ratio, flow rate, and temperature of the column based on the risk assessment. The retention time and resolution were selected as the method response. In response surface method, the central composite design and 23 factorial designs were employed for the optimization of the method. The polynomial equation was derived for the estimation of method response.

Conclusion: The method was optimized for better resolution among the drug, and impurity peaks were then validated as per the ICH parameters.
THE THE MICROEMULSION AS A KEY PLAYER IN CONQUERING THE SKIN BARRIER FOR THE AIM OF TRANSDERMAL DELIVERY OF DRUGS: REVIEWING A SUCCESSFUL DECADE
Authors: RANIA YEHIA  , DALIA A ATTIA
Published: October 2019

Microemulsion (ME) systems are now considered of the most successful transdermal drug delivery systems. This is due to their nanodroplets size in the one hand and to their composition that enables the use of several mechanistically penetration enhancers in the same formulation on the other hand. This work summarizes the types, properties, and the merits of the use of MEs for transdermal delivery and reviews the successful studies that were performed to deliver several drugs through this important route during the past 10–12 years.
EVALUATION OF GRAPE SEED EXTRACT (VITIS VINIFERA) AS A CROSSLINKER ON THE STABILITY OF DENTINE COLLAGEN IN TOTAL-ETCH ADHESIVE SYSTEMS: AN IN VITRO STUDY
Authors: D DENNIS  , FENIKA MAITARI
Published: October 2019

Objective: The bond strength between resin and dentine is determined by the integrity of collagen, dentine, and resin monomers. The susceptibility of the dentine bond results from the instability of the bonding structure that adheres to the bonding material. This can be achieved using collagen cross-linker, synthetically and naturally in dentine substrates which are effective in protecting collagen fibrils from degradation, as proanthrocyanidin. The aim of this study was to see the effect of grape seed extract as a crosslinker on the stability of dentine collagen and see the differences between groups.

Methods: This study used 27 fresh premolars or third molars which were divided into three Groups, namely Group I giving grape seed extract 6.5%, Group II giving chlorhexidine 2%, and Group III only giving bonding ingredients. Samples were analyzed using scanning electron microscopy with ×1000 magnification.

Results: Data were analyzed using kappa statistic, Kruskal–Wallis, and Mann–Whitney. The result of the study significant differences between treatment groups (p<0.05) and the 2% chlorhexidine group showed the highest value compared to the grape seed extract group and without treatment.

Conclusion: Grape seed extract can be used as an alternative to chlorhexidine as a crosslinker to maintain bone strength of the composite restoration.
LOW-FLOW ANESTHESIA TECHNIQUE REDUCES EMERGENCE AGITATION IN PEDIATRIC PATIENTS UNDERWENT GENERAL ANESTHESIA
Authors: CHRISTOPHER RYALINO  , TJOKORDA GDE AGUNG SENAPATHI  , ADINDA PUTRA PRADHANA  , ANDRIAN YADIKUSUMO
Published: October 2019

Objectives: This study was designed to see the risk factors that contribute to emergence agitation (EA) and also to know the effectiveness of low-flow (LF) anesthesia technique in EA in pediatric patients.

Methods: A total of 200 pediatric patients aged 6 months–6 years underwent surgery with general anesthesia were divided into two groups. The high-flow (HF) group was maintained with 5 l fresh gas flow (FGF), and the LF group was maintained with 500 ml FGF. The outcome was measured after the surgery was completed on Face, Legs, Activity, Cry, and Consolability and pediatric anesthesia emergence delirium (PAED) scores. Agitation defined in PAED score ≥10, and no agitation defined in PAED score <10.

Results: EA incidence in the HF group was higher compared to the LF group (59.5 vs. 4.7%, p<0.001). HF anesthesia technique was a single risk factor for agitation event, whereas LF anesthesia may prevent EA incidence until up to 92.7%.

Conclusion: LF anesthesia reduced agitation incidences. The effectiveness of LF was 92.7% in reducing the incidence of agitation. HF anesthesia was the main risk factor for agitation incidences.
F FORMULATION DEVELOPMENT AND EVALUATION OF CARBOPOL-INCORPORATED THERMOREVERSIBLE GELS OF PSEUDOEPHEDRINE FOR RECTAL DRUG DELIVERY
Authors: FIROZ S  , PADMINI K  , PADMASREE K  , SRAVANI N  , HEMALATHA A  , VENNELARANI Y
Published: October 2019

Objectives: The present study describes the preparation and evaluation of a Poloxamer 188 (P188)-based thermoreversible gel using Carbopol 934P (C934P) as a mucoadhesive polymer of pseudoephedrine for enhancing the bioavailability and to avoid the first-pass metabolism.

Materials and Methods: Five formulations (F1-F5) were prepared using cold method. The prepared gels were characterized by pH, drug content, spreadability, mucoadhesive force, gelation temperature, and drug release profile. Thermoreversibility of P188/C934P gel was demonstrated by rheological studies. The drug-polymer compatibility was studied using Fourier transform infrared (FTIR).

Results: The incorporation of carbopol into P188 gel also reduced the amounts of drug released from the gel formulations. FT-IR studies revealed that there are no interactions between the drug and polymers. Drug content of gels was estimated and the results were found to be satisfactory. In vitro dissolution studies revealed a good drug release from the gels. The drug release was higher in formulations F4 and F5 and lower in F1, F2, and F3 formulations. The order of drug release was found to be F5>F4>F3>F2>F1.

Conclusion: These findings suggested that developed thermoreversible gels could be used as promising dosage forms to rectal drug delivery for prolonged periods in the management of hemorrhoids.
DESIGN, SYNTHESIS, MOLECULAR DOCKING, AND BIOLOGICAL EVALUATION OF PYRAZOLE 1-CARBOTHIAMIDE INCORPORATED ISOXAZOLE DERIVATIVES
Authors: RADHIKA TUMMA  , HARINADHA BABU VAMARAJU
Published: October 2019

Objectives: Novel isoxazole incorporated pyrazole carbothiamide 5 (a-r) was designed and synthesized, docked and evaluated for anticancer activity Michigan Cancer Foundation-7 (MCF-7), and breast cancer cell lines.

Materials and Methods: Designed compounds were synthesized by the condensation of 1-(5-methyl-3-(4-nitrophenyl) isoxazole-4-yl) -3-(substitutedphenyl) prop-2-en-1-one (4) with thiosemicarbazides and substituted thiosemicarbazides to give the target molecules 5 (a-r). To predict the affinity and activity of the ligand molecule, the docking program Accelrys Discovery Studio 2.1 was employed to generate different bioactive binding poses of designing molecules at the active site of human Dihydrofolate Reductase (DHFR) (PDB ID: 1KMS). All the synthesized compounds were characterized based on the spectral and elemental analysis data. Antiproliferative activity was performed against MCF-7 breast cancer cell lines.

Results: All the synthesized compounds showed the characteristic peaks in Fourier-transform infrared,1H C13NMR, and mass spectral analysis. During docking, all the synthesized compounds 5 (a-r) exhibited higher fitness scores with minimum three bonding interaction with the active site human DHFR (PDB ID: 1KMS). In the MTT assay based on MCF-7 breast cancer cell lines, most of the compounds exhibited significant activity. In the antiproliferative assay against MCF-7 cell lines, most of the compounds exhibited potent activity with IC50 values in micromolar concentrations. Compounds 5a, 5b, 5f, 5h, and 5k have exhibited significant anticancer activity.

Conclusions: The derivatives were synthesized in quantitative yields. New derivatives possess the antiproliferative activity and antitubercular activity.
CHEMICAL ANALYSIS OF LITSEA CUBEBA ESSENTIAL OIL HARVESTED FROM ARUNACHAL PRADESH, INDIA AND ESTIMATION OF MOSQUITO REPELLENT ACTIVITY WITH REFERENCE TO NETWORK ANALYSIS
Authors: NAYANMONI BORUAH  , SUDARSHANA BORAH  , PRIYANKA SARKAR  , HEMANTA KUMAR SHARMA
Published: October 2019

Objective: Litsea cubeba is a medicinal plant indigenous to Southeastern Asia. The fruit of the plant is rich in essential oil. A study has been carried out to investigate on the chemical composition of essential oil of the plant harvested from Arunachal Pradesh and to find out its mosquito repellent activity.

Methods: The essential oil has been isolated from the fresh fruits by hydrodistillation and analyzed by gas chromatography–mass spectrometry. Compound-compound network analysis was carried out in SPSS software (IBM SPSS Statistics 20) followed by the construction of the network using Cytoscape 3.5.0. Mosquito repellent study was carried out using standard procedure.

Results: Citronellal (17.32%), citronellol (13.85%), nimbiol (9.35%), and myrcenol (7.40%) were the major constituents of the essential oil and the essential oil illustrated 3 h mosquito repellent activity against Aedes aegypti mosquitoes.

Conclusion: From this investigation, a significant difference could be observed in the essential oil composition from the previously reported data of other regional areas of Asia, and furthermore, the essential oil possesses significant mosquito repellent activity.
INVESTIGATION ON DISSOLUTION PATTERN AND MATHEMATICAL MODELING OF DRUG RELEASE OF QUERCETIN BY COMPLEXATION WITH CYCLODEXTRIN NANOSPONGES
Authors: SOBITHARANI P  , ANANDAM S  , MOHAN VARMA M  , VIJAYA RATNA J  , SHAILAJA P
Published: October 2019

Objective: The main objective of this study was to investigate the release pattern of a poorly water-soluble drug quercetin (QU) by fabricating its cyclodextrin nanosponges.

Methods: Characterization of the original QU powder and QU-loaded nanosponges was carried out by the Fourier-transformed infrared (FTIR) spectroscopy, transmission electron microscopy (TEM), and dissolution tester. The drug release pattern was subjected to various kinetic models.

Results: FTIR studies confirmed the formation of inclusion complex of drug. The particle size analysis revealed that the average particle size measured by laser light scattering method is around 400–420 nm with low polydispersity index. The particle size distribution is unimodal and having a narrow range. A sufficiently high zeta potential indicates that the complexes would be stable and the tendency to agglomerate would be miniscule. TEM image revealed the porous nature of nanosponges. The dissolution of the QU nanosponges was significantly higher compared with the pure drug.

Conclusion: From the kinetic study, it is apparent that the regression coefficient value closer to unity in case of Korsmeyer-Peppas model indicates that the drug release exponentially to the elapsed time. n value obtained from the Korsmeyer-Peppas plots, i.e., 0.9911 indicating non-Fickian (anomalous) transport ; thus, it projected that delivered its active ingredient by coupled diffusion and erosion.
SYNTHESIS, SPECTRAL CHARACTERIZATION, AND ANTIPROLIFERATIVE ACTIVITY OF DISPIROPYRROLIDINES CONTAINING 2-THIOXOTHIAZOLIDIN-4-ONE NUCLEUS
Authors: SIVAGNANAM JAYASURIYA  , THALIGAI SUBRAMANIAN MALAVIZHI  , STEPHENKUMAR CELESTINA  , KAVERI SUNDARAM
Published: October 2019

Objective: Spiro compounds are present in nature, endowed with deep biological activities. Heterocyclic compounds with a pyrrolidine scaffold are one of the paradigms of organic chemistry that exhibits a wide variety of properties and biological functions. Based on these, seven dispiropyrrolidines have been accomplished by [3+2] cycloaddition reaction from acenaphthenequinone and sarcosine with several dipolaro files such as substituted 5-benzylidene-2-thioxothiazolidin-4-ones.

Methods: Cycloadducts 4a-g were prepared by conventional method and the structures of the compounds 4a-g were completely characterized by infrared, 1H, 13C nuclear magnetic resonance spectral data, and elemental analysis. The cytotoxic activity of the synthesized compounds was carried out by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide assay.

Results: The dispiropyrrolidines 4a-g were showed a moderate-to-good cytotoxic activity against human cervical cancer lines. Among all the synthesized compounds, 4d was found to be more potent with human cervical cancer line with an half maximal inhibitory concentration (IC50) value of 5.5 μM.

Conclusion: The synthesized compound 4d found to be an excellent activity which is nearly closed to reference drug gemcitabine with an IC50 value of 4.6 μM.
PROTECTIVE ROLE OF PTEROSTILBENE ON PLASMA AND TISSUE GLYCOPROTEIN COMPONENTS IN HIGH-FAT DIET-FED AND STREPTOZOTOCIN-INDUCED TYPE 2 DIABETIC MICE
Authors: GUNASEELAN THANGASAMY  , LEELAVINOTHAN PARI
Published: October 2019

Objective: The aim of the current study is to evaluate the effect of pterostilbene (PTS), on deranged plasma and tissue glycoprotein components in high-fat-diet (HFD) and streptozotocin (STZ)-induced type 2 diabetic mice.

Methods: The experimental duration was 16 weeks. The C57BL6/J mice were fed a normal diet, normal diet with PTS, HFD, and STZ injection (10th week only), and diabetic mice with PTS for the past 6 weeks.

Results: A significant increase in glycoprotein components such as hexose, hexosamine, fucose, and sialic acid (SA) in plasma was observed in diabetic mice. In hepatic and renal tissues, a significant decrease in SA with an increase in other glycoprotein components was detected in diabetic mice when compared with control mice. Oral administration of PTS significantly improved the glycoprotein levels in plasma and tissues of diabetic mice to near normal level.

Conclusion: In this study, we resolved that PTS improves disturbed glycoprotein metabolism in HFD and STZ-induced type 2 diabetic mice.
Settlement and bearingcapacity of long pile
Authors: Ter-Martirosyan Armen Zavenovich , Ter-Martirosyan Zaven Grigor’evich , Trinh Tuan Viet , Luzin Ivan Nikolaevich
Published: October 2019

When a long pile is interacting with the soil, the combined force applied to the pile head is distributed among the side face and the pile toe inhomogeneously. The toe gets not more than 30 % from the general force, which doesn’t let using the reserves of the bearing capacity of relatively firm soil under the fifth pile. Account for the depth of the pile toe and the dead load of the soil allows increasing the bearing capacity of the soil under the pile toe and decrease the pile settlement in general. For the quantitative estimation of these factors it is necessary to solve the task on the interaction of the rigid long pile with the surrounding soil, which includes under the pile toe, which is absolutely rigid round stamp.The article presents the formulation and analytical solution to a quantification of the settlement of a circular foundation with the due account for its depth, basing on the development of P. Mindlin’s studies as well as the interactions between a long rigid pile and surrounding soils, including under pile toe.It is proposed to compare the estimated value of stresses under the heel of pile with the initial critical load for the round foundation to check the condition that the estinated value is less than the intial critical one.
SOME APPLICATION OF THE FOKKER-PLANCK EQUATION
Authors: Pirozhkov Victor Grigorevich , Roshka Olga Olegovna , Aleroev Temirkhan Sultanovich
Published: October 2019

In this paper, we study the foreign exchange rates of a pair Russian ruble/US dollar on the subject of fractality. It has been shown that the time series studied quotes has the basic fractal properties. With the help of the Hurst exponent was calculated by the Hausdorff dimension, which was a fractional number that supports the hypothesis of fractality. Volatility charts were compared with charts of known solutions of the fractional differential equation wandering point particle in a self-similar fractal set. The solution of this equation is a function of Mittag-Leffler. It is shown that graphs of the Mittag-Leffler function repeat exactly the structure of graphs volatilities for different periods of time. The solution of such an equation is written out using the Mittag-Leffler functions. The graphs of these decisions are compared with the volatility charts for different time periods. It also clearly confirms that the Russian currency market is a fractal. Thus, these results will help in predicting market behavior in advance a preset time in the future, which is almost a valuable tool for working with Russian currency market.
Organization and implementation of risk-management in building enterprise
Authors: Barkhi Reza , Borkovskaya Victoria G.
Published: October 2019

Introduction. Consider the system of organization and implementation of risk management in the building enterprise. The introduction and management of risks in an industrial enterprise is an actual problem due to the occurrence of the following list of factors: incomplete information, elements of randomness, unpredictability of actions of a partner or competitor, among others. Risk management is a process that must begin at the development stage of a industrial company’s strategy, and necessarily with the participation of its owners, since it is the owners who, when developing a strategy, should determine the maximum level of total risk that the industry company will be ready to accept in the course of its activities. Risk management in industrial enterprises should be implemented within the framework of the system and process approaches, taking into account the specifics of the industry using modern effective management methods and production organizations, as well as using risk management tools. Materials and methods. The methodology of the continuous risk management process was used to study the industry organization and implementation of risk management, and systems analysis, modeling and synthesis methods were used. Results. It was determined that the creation of a risk management department is appropriate for effective risk management at the industry enterprise. The main responsibilities of this unit, including for staff and other users (including employees, consultants and contractors), in order to successfully implement the management strategy, require unconditional implementation to minimize risks and eliminate costs in implementing risk management. It was revealed that as a result of introducing risk management in industry enterprises of various industries, a set of measures should be developed to evaluate the operational risks of an enterprise, integral risk, quantitative assessment of which is based on a comprehensive analysis of financial and accounting reports, and conducting an integrated risk assessment based on all levels of responsibility within the industrial enterprise. Conclusions. Risk management at industrial enterprises should be carried out within the framework of the system and process approaches, taking into account the specifics of the industry using modern effective management methods and production industrial organizations, as well as using risk management tools.
Autocontrol de la agresividad de las usuarias de crack
Authors: Limberger Jéssica , Staevie dos Santos Bruna , Ribeiro Beneton Emanueli , Andretta Ilana
Published: October 2019

A literatura aponta dificuldades no autocontrole da agressividade de mulheres usuárias de crack. No entanto, carecem estudos que expliquem tais dificuldades. Este estudo tem como objetivo identificar o valor preditivo de comorbidades psiquiátricas, contextos de interação e situações relacionadas ao uso de drogas no autocontrole da agressividade de usuárias de crack. Trata-se de uma pesquisa quantitativa, transversal e explicativa. Um total de 62 usuários de crack foram avaliadas através dos instrumentos: Questionário sobre Uso de Drogas, Mini International Neuropsychiatric Interview, Screening Cognitivo do WAIS-III, IHS-Del-Prettee Structured Clinical Interview for DSM Disorder. O envolvimento com o tráfico de drogas e o Episódio Depressivo Maior foram preditores de baixos escores no autocontrole da agressividade. Ações conjuntas como Treinamento de Habilidades Sociais, Tratamento de Episódios Depressivos Maiores e prevenção da exposição a comportamentos de risco, como o tráfico de drogas, são necessárias, pois essas variáveis ​​apresentaram valor explicativo no autocontrole da agressividade.
Factores asociados a los accidentes de motocicleta en Barcelona, España
Authors: Hidalgo-Fuentes Sergio , Sospedra-Baeza María
Published: October 2019

Este estudio analizó los accidentes de motocicleta y ciclomotor en Barcelona (España). 53.190 informes de conductores de motocicleta y ciclomotor involucrados en accidentes entre los años 2006 y 2011 fueron extraídos de la base de datos de accidentes con víctimas de la Dirección General de Tráfico. Estos datos fueron analizados en términos de sexo, grupos de edad, motivo del desplazamiento, día de la semana, infracciones de velocidad, uso del casco y lesividad, con el objetivo de estudiar las características de los accidentes de motocicleta y ciclomotor en Barcelona y evaluar las diferencias entre conductores varones y mujeres en estos accidentes. La gravedad de los accidentes sufridos por conductores varones es superior a la de las mujeres. Se encontraron diferencias significativas en todas las variables consideradas en el estudio, lo que implica diferencias en el perfil del conductor de accidentado.
Evaluación del engagement en trabajadores de la salud en Uruguay a través de la escala Utrecht de engagement en el trabajo (UWES)
Authors: Gómez Garbero Lucía , Labarthe Javier , Ferreira-Umpiérrez Augusto , Chiminelli-Tomás Virginia
Published: October 2019

El objetivo principal de este estudio fue examinar las propiedades psicométricas de la versión en español de la escala Utrecht de engagementen el trabajo (UWES) en su versión de 17 ítems para la evaluación de trabajadores de la salud en Uruguay. La muestra se compuso de 1324 trabajadores de ambos sexos (63.7% de mujeres) de diferentes instituciones de salud, públicas (45.7%) y privadas (54.3%), de Montevideo y del interior del país (64.4% y 35.6% respectivamente). Los análisis de consistencia interna, mediante coeficiente alfa de Cronbach, revelan niveles satisfactorios de consistencia interna de la escala total y los tres factores, y refuerzan la evidencia de debilidad de dos ítems de la escala. Los análisis de estructura factorial a partir de un análisis factorial confirmatorio, muestran el ajuste medianamente aceptable del modelo trifactorial a los datos, aunque los elevados índices de correlación entre los factores latentes indican que un modelo unifactorial también podría ser aceptable. La evidencia de este estudio sugiere que la versión en español del UWES-17 puede ser un instrumento válido y confiable para la medición del compromiso y sus tres factores en los trabajadores de salud en Uruguay.
Neoconstitucionalismo Utópico en Ecuador
Authors: Celi Toledo Israel
Published: October 2019

En esta ponencia ensayamos un análisis histórico conceptual del paradigma neoconstitucional en América Latina y Ecuador, en aras de identificar las ideas que inspiran proyectos transnacionales de política jurídica. Luego, hablaremos de los actores e ideas que tuvieron expresión en el proceso constituyente de Montecristi (Ecuador), con objeto de evidenciar la agencia de intelectuales del derecho que influyeron en el diseño constitucional basado en el paradigma neoconstitucional ecuatoriano. Finalmente, a partir de lo anterior, y de desarrollos conceptuales atribuibles al institucionalismo histórico ecuatoriano, se argumenta que el neoconstitucionalismo en Montecristi es una utopía desarmada, no solo por los problemas inherentes a un lenguaje normativista y periférico, sino también, debido a las condiciones políticas y sociales de la polis que busca transformar.
De esta manera, nuestro trabajo también pretende plantear interrogantes al pensamiento jurídico ecuatoriano y latinoamericano, desde la crítica al neoconstitucionalismo, un paradigma que transforma la realidad en apéndice de la norma, y conlleva fuertes límites como “tipo ideal”, en un contexto institucional en el que la política no está dispuesta a trasladar al campo jurídico los conflictos más relevantes del proceso democrático.
Conciencia obrera y conciencia histórica como referentes sociohistóricos de autogestión en territorios del Cauca
Authors: Arboleda Suarez Edgar
Published: October 2019

El documento presenta el escenario de crisis empresarial experimentado por Industrias Puracé SA en la década de los noventa; una antigua empresa dedicada a la explotación de azufre natural en la región Puracé en el Departamento del Cauca, Colombia; la cual es rescatada (o recuperada) por sus trabajadores a través de una nueva nominación simbólica denominada Empresa Minera Indígena del Cauca –EMICAUCA SA-. Se resalta el acervo sociohistórico de los trabajadores en cuanto obreros, aspecto que se expresa en la conciencia de clase obrera y, de otra parte, la conciencia histórica de su condición indígena, como recursos que permiten la emergencia de esta experiencia de autogestión.
OBJECTIFICATION OF MENTAL DISORDERS USING SPECIAL MAGNETIC RESONANCE IMAGING TECHNIQUES IN THE SYSTEM OF MONITORING THE MENTAL HEALTH OF SERVICEMEN
Authors: Tarumov D. A. , Marchenko A. A. , Trufanov A. G. , Romanov G. G. , Lobachev A. V. , Mavrenkov E. M. , Iskhakov D. N. , Zheleznyak I. S. , Shamrey V. K. , Trufanov G. E. , Fisun A. Ya.
Published: October 2019

Introduction. Alcoholism and opioid addiction are the leading problems of modern narcology and together with adaptation disorders create a significant contribution to dismission from the ranks of the Armed Forces. Identifying the latent forms of mental disorders is of particular importance for making expert decisions at invoking. Special MRI techniques allow to evaluate the functional and microstructural connectivity of distant parts of the brain.

Materials and methods. With the application of functional MRI and tractography, 405 patients were examined from the potential conscription pool: 76 patients with alcohol dependence syndrome, 170 with opioid dependence syndrome, and 9 with adaptation disorders. In patients suffering from adaptation disorders, opioid dependence and alcoholism, an analysis of the neural network of the passive mode of the brain was performed.

Results. There was established, comparing to the control group, all the patients suffering from addiction demonstrated a weakening of the functional connections of all brain structures. Compared with the control group, the patients with drug addiction and alcoholism had microstructural deformation between the cortical and subcortical structures, especially between the amygdala and the hippocampus. The weakening of functional and microstructural links in the network of the passive mode of the brain in groups of drug addicts indicates that they have violated the processes of control, thinking and the correct decision making. In case of adaptation disorders, integral bilateral differences in terms of global and local node efficiency between groups of patients with adaptation disorder and healthy individuals showed a higher significance of the network of passive mode of the brain in the system of mutual functional connectivity of the posterior cingulate cortex and preclinical. The data obtained create the basis for the creation of biomarkers for patients suffering from mental disorders, which can be used to examine, guide and evaluate the treatment of this pathology.
USING QCT TO DETECT DRUG-INDUCED OSTEOPOROSIS IN PATIENTS WITH MENTAL DISORDERS
Authors: Ananyeva N. I. , Likhonosova S. E. , Neznanov N. G. , Mazo G. E. , Nasyrova R. F. , Shnayder N. F. , Lipatova L. V. , Rybakova K. V. , Malyshko L. V. , Gadgieva F. Sh. , Kocyubinskaya Yu. V. , Andreev E. V.
Published: October 2019

In clinical practice, the assessment of the cumulative risk of drug-induced osteoporosis in patients with mental disorders is difficult because there are no algorithms to reveal patients with a high risk of antipsychotic-induced osteoporosis and BMD is not evaluated in patients with mental disorders. 95 patients aged from 21 to 60 years with a mental illness duration of at least 12 months on antipsychotics and anticonvulsants therapy were examined. 23 patients (24%) had shown a violation of BMD. There is a significant correlation between the number of risk factors and a decrease in BMD. However, additional study of pharmacogenetic and laboratory data on the risk of osteoporosis is required, which will make it possible to plan therapy more precisely, additionally prescribe drugs that regulate BMD in these categories of patients.
DYNAMIC BRAIN MAGNETIC RESONANCE IMAGING OF DROWNING VICTIUM WITH HYPOXIC DAMAGE
Authors: Andropova P. L. , Popov P. A. , Gavrilov P. V.
Published: October 2019

In most countries, drowning is one of the three leading causes of children’s death from 5 and 14 years of age, and the most common cause with children under the age of 4 [1–3]. Drowning makes 7% of all fatal accidents involving similar types of brain damage among all age groups worldwide.

The aim. To show the importance of brain magnetic resonance studies of a patient with hypoxic-ischemic lesion during the acute period. An attempt to predict the outcome after global brain hypoxia in a little boy.

Materials and methods. A 2-year-old boy was examined with a dynamic brain MRI after drowning.

Results. Brain MRI made 30 minutes later after drowning showed bilateral matter hyperintensity from the parietal lobes, posterior frontal lobes, hippocampus, right lenticular nucleus, ventral tegmentum of the brainstem on the diffusion-weighted imaging (DWI). A lower diffusion coefficient on Apparent diffusion coefficient (ADC) maps reveals intracellular (cytotoxic) edema caused by acute hypoxic damage. At follow-up after 15 days — T2-weighted image shows white matter hyperintensity. The expansion of the ventricular system, the subarachnoid space of the large hemispheres reflects diffuse cerebral atrophy.

Conclusion. Physicians need revealing the vastness of hypoxic brain damage and reliable criteria to predict the outcome of the disease. Diffusion-weighted magnetic resonance imaging provides a sensitive measure of cerebral hypoxia and provides a reliable prediction of the outcome of drowning.