bluuebunny/crossref_metadata_2025_split huggingface dataset:
DEVELOPMENT OF ZOLMITRIPTAN MOUTH DISSOLVING FILMS: FORMULATION VARIABLES, MECHANICAL PROPERTIES, AND IN VITRO DRUG RELEASE STUDIES
Authors: SUDHIR MADDELA  , BUCHI N. NALLURI  
Published: October 2019

Objective: The objective of the present investigation is to prepare zolmitriptan (ZOL) mouth dissolving films (MDFs) and to investigate the influence of formulation variables on physicomechanical, chemical, and drug release properties of the prepared MDFs.
Methods: The MDFs were prepared by solvent casting technique using wet film applicator. The impact of hydroxypropyl methylcellulose of different viscosity grades (hydroxy propyl methyl cellulose [HPMC] E3, E5, and E15), plasticizers (glycerol and polyethylene glycol [PEG]-400), and solubilizing agents (polyvinyl pyrrolidone [PVP K30] and sodium lauryl sulfate [SLS]) on physicomechanical, chemical, and drug release properties were evaluated. The MDFs were also characterized by Fourier-transform infrared spectroscopy, differential scanning calorimetry, and X-ray diffractometry studies.
Results: The MDFs prepared were transparent and smooth and showed no recrystallization. The tensile strength of the MDFs increased significantly with an increase in polymer viscosities, and about a 2.63-fold increase in tensile strength was observed for HPMC E15 MDFs compared to E3, whereas an increase in film thickness resulted in brittle MDFs with low tensile strength. Similar results were observed with percent elongation and folding endurance of the MDFs. In vitro, drug release studies indicate that higher film thickness and polymer viscosities delayed the MDF disintegration and, in turn, the ZOL release. Addition of PVP K30 and SLS to HPMC E3 formulations resulted in 1.66- and 1.53-fold increase in ZOL release rates.
Conclusion: Overall, F7 formulation showed quicker disintegration (within 11 s) and ZOL release rates (within 180 s) along with good physicomechanical properties. These results indicated that the disintegration and drug release of ZOL can be enhanced to a greater extent by optimizing formulation variables in MDFs.
DEVELOPMENT AND VALIDATION OF A NOVEL METHOD FOR CAUSALITY ASSESSMENT USING SUSPECTED ADVERSE DRUG REACTIONS TO ANGIOTENSIN-CONVERTING ENZYME INHIBITORS
Authors: Sodhi Rupinder Kaur 
Published: October 2019

Objectives: The study has been designed to develop, test reliability, and construct validity of a novel versatile causality assessment tool (VCAT) method.
Methods: The study included 427 literature case reports of angiotensin-converting enzyme inhibitors with suspected adverse drug reactions from 1990 to February 25, 2016. The causality of these cases was assessed independently by 3 raters in 3 phases of the study. Kappa (k) and intra-class correlation Intraclass Correlation Coefficient (ICC) were used to test reliability and validity of the VCAT method.
Results: Intra-rater reliability was high between Phase I and Phase III (k=0.84–0.93; % agreement: 92.3–96.3%). Inter-rater agreement was good in Phase I (k=0.87–0.89, % agreement: 93.7–94.1%, ICC: 0.975) and Phase III (k=0.85–0.89, % agreement: 93–94.4%, ICC: 0.973). Validity was proved by the high agreement observed between Phase I and Phase II (k=0.78–0.94; % agreement: 89.7–97.2%; p<0.001); and between Phase II and Phase III (k=0.8–0.9; % agreement: 90.2–94.8%; p<0.001).
Conclusion: VCAT method is a standardized causal assessment tool that gives valid and reproducible results. It has shown good agreement with the expert judgment method. This method may overcome the limitations enthralled with existing methods of causality assessment.
SYNTHESIS AND EVALUATION OF ANTIMICROBIAL ACTIVITY OF PYRIMIDINE DERIVATIVES
Authors: BHAGCHAND JAT  , SWAPNA SANTRA  , PRASANTA KUMAR SANTRA  
Published: October 2019

Objectives: Synthesis, characterization, and evaluation of antimicrobial activity of novel pyrimidine derivatives containing O, N, and S in the ring.
Methods: Pyrimidine derivatives were prepared in three steps. In the first step, chalcones containing -NO2 functional group were synthesized using Claisen-Schmidt condensation of aromatic aldehydes with 2-acetyl pyridine/3-acetylpyridine in methanol in the presence of aqueous NaOH. In the second step, -NO2 group was reduced to -NH2 group. Resulting compounds containing NH2 functional group were reacted with different dichlorothienopyrimidines and dichlorofuropyrimidines in the presence of N,N-diisopropylethylamine to obtain pyrimidine derivatives.Antibacterial and antifungal activity of pyrimidine derivatives were studied in vitro.
Results: Pyrimidine derivatives were synthesized and purified using flash column chromatography. Purity of synthesized pyrimidines was determined by high-performance liquid chromatography. Pyrimidines were characterized by elemental analysis, infrared, nuclear magnetic resonance, and mass spectral analysis. Analytical data of synthesized pyrimidines supported the proposed structures. Significant antibacterial and antifungal activity were observed in the synthesized pyrimidine derivatives.
Conclusion: Antibacterial and antifungal activity of the newly synthesized pyrimidine derivatives will definitely inspire future researchers for the preparation of new analogs.
DOUBLE-BLIND RANDOMIZED CLINICAL TRIAL OF KAEMPFERIA GALANGA L EXTRACT AS AN ANTI-INFLAMMATION (PROSTAGLANDIN E2 AND TUMOR NECROSIS FACTOR ALPHA) ON OSTEOARTHRITIS
Authors: NURPUDJI A TASLIM  , M NATSIR DJIDE  , YUSNITA RIFAI  , AKMAL NOVRIAN SYAHRUDDIN  , YOSEFA RIA RAMPO  , MURNI MUSTAMIN  , SIGIT ANGRIAWAN  
Published: October 2019

Objective: The purpose of this study was to compare the effectiveness of the rhizome extract against inflammatory markers such as tumor necrosis factor (TNF)-alpha and prostaglandin E2 (PGE2) with meloxicam in patients with osteoarthritis at knee.
Materials and Methods: This study designed two phases as follows: The preparation of rhizome extract in a capsule dosage form which was then followed by double-blind clinical trials, randomized controlled, pre- and post-test design (18 cases) using the WOMAC scores for pain, to markers of inflammation using an enzyme-linked immunosorbent assay method.
Results: The results did not reveal any significant differences in pain scores, stiffnesses, and physical function impairment between the intervention (the rhizome extract) and control groups (meloxicam), it either did not reveal any significant differences in the parameters of inflammatory marker TNF alpha and PGE2 among the groups.
Conclusion: The rhizome extract had the same effect on pain, stiffness, physical interference as meloxicam, and on PGE2 as well as on the inflammatory marker TNF-alpha. Therefore, this extract can be used as an alternative herbal medicine for osteoarthritis.
EFFECTS OF ETHANOL CINCAU (CYCLEA BARBATA MIERS) LEAVES EXTRACT ON MACROPHAGE MIGRATION ON BURN WOUND
Authors: DINA DEWI S L I  , WIBI RIAWAN  , IKA SETYO RINI  , TITIN ANDRI WIHASTUTI  , IKA FITRI APRILIANTI  , RETTY RATNAWATI  , HANDONO KALIM  , KARYONO MINTAREOM  , LOEKI ENGGAR FITRI  
Published: October 2019

Objective: Macrophages are essential cells in burn wound healing. The primary function of macrophages is phagocytosis of microbes and necrosis tissue. Migration of macrophages into the wound area is affected by interleukin-1 (IL-1). Ethanol extract of Cincau or green grass jelly leaves or Cyclea barbata Miers contains pectin, flavonoids, and alkaloids. These compounds influence the inflammatory process. The purpose of this study was to reveal the effect of ethanol Cincau leaves extract on the expression of IL-1 and the number of macrophages in second degree burn wounds tissue.
Methods: This study used 30 rats divided into six groups based on different treatments: NaCl 0.9% (K), silver sulfadiazine/(SSD) (P1), hydrogels (P2), Cincau extract 40% (P3), Cincau extract 50% (P4), and Cincau extract 60% (P5). Treatment was conducted over 4 days. On the 5th day, burn wounds tissues were taken, then immunohistochemistry staining was applied.
Results: One-way ANOVA test on the expression of IL-1 showed a difference among groups (p<0.05) and on the number of macrophages (p<0.05). Post hoc tests on the expression of IL-1 showed Cincau extracts 40% and 50% treated-groups significantly differ with the NaCl 0.9% group but not with hydrogel treated group. The similar result showed Cincau extracts 40% and 50% treated-groups significantly differ from the control group but not with SSD and hydrogel groups.
Conclusions: It can be concluded that ethanol extract of Cincau leaves can decrease IL-1 expression and increase the number of macrophages which have an important role in inflammation resolution of burn wounds.
EVALUATION OF ANTIDIABETIC AND ANTIHYPERLIPIDEMIC EFFECT OF VERNONIA DIVERGENS IN STREPTOZOTOCIN-INDUCED DIABETIC RATS
Authors: LAXMIDHAR MAHARANA  , MANOJ KUMAR SETHI  , RUDRA NARAYAN DASH  , SNIGDHA PATTNAIK  
Published: October 2019

Objective: The current investigation for antidiabetic activity of the plant Vernonia divergens (DC.) Edgew. has not been reported till date. However, to enlighten the folkloric claim of the plant, the study was carried out on various animal models such as albino mice, albino rabbits, Wistar rats, rabbits, hamsters, dogs, and monkeys.
Methods: The whole plant of V. divergens was studied on various animal models. Screening methods generally have been carried out on rodents and non-rodents, respectively. Various biochemical and hematological parameters such as serum glucose, plasma insulin, lipid profile and activities of liver enzymes, red blood cells, white blood cells, hemoglobin, and differential counts were measured to assess the antihyperglycemic and antihyperlipidemic activities as well as safety profile of the extract.
Results: Among all experimental extracts of V. divergens, it was found that the aqueous and methanolic extracts had maximum control of blood glucose in diabetic Wistar rats. While comparing with normoglycemic animals, it was observed that reduction of blood sugar level and increase in plasma insulin level are maximum with test extract. Among the study, the effects of the methanolic extract of V. divergens (MEVD) and aqueous extract of V. divergens (AEVD) were done through oral route in both the models, i.e., normoglycemic and hyperglycemic animal models. The safety profile was evaluated by toxicological evaluation and observed that, even at a higher dose level of 3000 mg/kg body weight, the MEVD and AEVD were safe and retain normal physiological and behavioral effect. The whole protein, whole cholesterol, aspartate aminotransferase, alanine aminotransferase, and alkaline phosphatase enzyme activity of streptozotocin-administered rats showed significantly higher than normal rats, and the test extract-treated rats significantly reduced the elevated levels.
Conclusion: It is concluded that the MEVD and AEVD (DC.) Edgew. might be beneficial in effectively reducing the blood glucose concentration and managing the various complications of diabetes. However, in comparison between both the extracts, the methanol extract was found to be significantly more potent than that of the A.E. in all aspects.
ANTI-INFLAMMATORY ACTIVITY OF METHANOL EXTRACT OF NIEBUHRIA APETALA (ROTH) DUNN – IN VITRO MODELS
Authors: RAJESH A  , DOSS A  , TRESINA PS  , MOHAN VR  
Published: October 2019

Objective: The objective of this study was to determine the anti-inflammatory activity of methanol extract of Niebuhria apetala and its possible mechanism of action.
Methods: Methanol extract of Niebuhria apetala leaf (NAL) was assessed for its anti-inflammatory activity by in vitro methods. Using albumin denaturation assay, proteinase inhibitory activity, membrane stabilization, and antilipoxygenase activity at different concentrations, in vitro anti-inflammatory activity was estimated. The standard drug used for this purpose was aspirin.
Results: Methanol extract NAL at a concentration range of 100–500 μg/ml significant (p<0.01) protects the heat-induced protein denaturation. At the concentration of 500 mg/ml, NAL showed significant (p<0.01) inhibition of protease inhibitory action. Heat-induced hemolysis of erythrocyte, hypotonicity-induced hemolysis, and lipooxygenase activity were significant (p<0.01) inhibited at the concentration of 500 μg/ml.
Conclusion: Finally, the present study indicates that methanol extract of Niebuhria apetala can be a potential source of anti-inflammatory agent.
IN VITRO-IN VIVO CORRELATIONSHIP APPROACH OF THE PREPARED MAGNETIC MICROSPHERES OF CYTARABINE
Authors: SATINDER KAKAR  , ANUREKHA JAIN  
Published: October 2019

Objective: The objective of this study was to study the in vitro-in vivo correlationship between the magnetic microspheres prepared by continuous solvent evaporation (CSE) method by 32 factorial designs.
Methods: CSE technique was used in the preparation of magnetic microspheres. Drug used was cytarabine and mice were the animal model used to check the correlationship.
Results: The profiles are nearly identical and reveal that drug absorption is rapid. The in vivo drug absorbed was found to be in concordance with the in vitro release as seen in the superimposable curves.
Conclusion: Cytarabine effectively reduces the amount of drug released and consequently absorbed in vivo in the initial phase.
A PRELIMINARY OBSERVATION ON AN EXPLICIT ANTIMICROBIAL ACTION OF MANGROVE PLANTS ON PSEUDOMONAS AERUGINOSA
Authors: TAMANNA SULTANA  , ARUP KUMAR MITRA  , SATADAL DAS  
Published: October 2019

Objectives: Due to emerging drug-resistant microorganisms throughout the world, newer antimicrobial agents should be looked for. Plants are enriched with different bioactive chemicals. In this study, we searched antibacterial activities of some mangrove plant extracts against Pseudomonas aeruginosa, Staphylococcus aureus, and Escherichia coli.
Methods: In the present study, the antimicrobial activity of the leaves of Bruguiera gymnorhiza, Excoecaria agallocha, Avicennia alba, and Aegialitis rotundifolia was evaluated against a few reference pathogenic bacterial strains, namely, P. aeruginosa ATCC 27853, E. coli ATCC 25922, S. aureus ATCC 29213, and multidrug-resistant bacterial strains E. coli extended-spectrum beta-lactamases strain. Aqueous, ethanolic, methanolic, and dimethyl sulfoxide (DMSO) extracts were studied. The antimicrobial activities of the organic solvent extracts on the various test microorganisms were investigated using agar well diffusion technique followed by determination of minimum inhibitory concentration values by serial dilution in a microtiter plate.
Results: Ethanol and DMSO extracts of B. gymnorhiza exhibited promising antimicrobial activity followed by extracts of A. alba and E. agallocha. Among all microorganisms studied, P. aeruginosa ATCC 27853 showed significant growth inhibition with ethanol and DMSO extracts.
Conclusion: Extracts of some mangrove plants, particularly, B. gymnorhiza showed very good antimicrobial activities against common microbial agents causing human infections and in general mangrove plants appear to act better on P. aeruginosa.
AN EXPERIMENTAL STUDY EVALUATING THE INFLUENCE OF QUERCETIN ON MONOSODIUM GLUTAMATE-INDUCED DEPRESSION IN SWISS ALBINO MALE MICE
Authors: SRIRAM BS  , RAVICHANDRA V  
Published: October 2019

Objective: The objective of the study was to evaluate the antidepressant activity of quercetin in monosodium glutamate (MSG) model of depressed male mice.
Methods: MSG was administered (500 mg/kg) to different groups of albino male mice daily for 21 days to induce depression. The interventions (Quercetin and imipramine) were started on day 9th and continued till 21st day. On 23rd day, mice are sacrificed, hippocampus and amygdala supernatant are subjected for analysis. p<0.05 was considered as statistically significant.
Results: There was a statistically significant reduction in interleukin (IL)-6 levels in animals treated with quercetin and imipramine compared to control group (p<0.001). There was also a statistically significant increase in brain-derived neurotrophic factor (BDNF) levels in quercetin with MSG groups (p<0.05) and imipramine with MSG groups (p<0.01). There was no statistically significant difference in IL-6 and BDNF levels between the groups of animals treated with quercetin (100 mg/kg) and imipramine (10 mg/kg) alone.
Conclusion: Quercetin appeared to have an antidepressant activity. More extensive research is required to substantiate and elucidate the role of quercetin in behavioral disorders such as depression.
DEVELOPMENT, EVALUATION AND TARGETING OF STAVUDINE LOADED SERUM ALBUMIN POLYMER BASED NANOCARRIERS TO HIV RESERVOIRS
Authors: JENITA J JOSEPHINE LENO 
Published: October 2019

Objective: Stavudine is an antiretroviral drug that is part of the nucleoside reverse transcriptase inhibitor (NRTIs) family, which is used to delay the progression of HIV infection. The present investigation involves the development and evaluates stavudine loaded nanocarriers using natural polymer bovine serum albumin (BSA).
Methods: The desolvation technique was used to prepare nanoparticles and coated with 1% v/v polysorbate 80 to improve the targeting of drugs to the organs (HIV reservoirs). Biodistribution studies were also investigated for the best formulation to determine the targeting efficiency of nanocarriers loaded stavudine and compared with pure compound.
Results: The formulated nanocarriers have shown mean particle size below 300 nm, zeta potential in the range of -16.5 Mv, encapsulation efficiency in the range of 50.10 to 73.7%, drug loading in the range of 14.73 to73.84%. Cumulative % drug release was in the range of 24.72 to 71.20% and release kinetics studies showed that the mechanism of drug release was controlled simultaneously by diffusion and erosion of the matrix type formulations. The stability studies over a period of three months confirmed the stability of BSA nanoparticles. Biodistribution studies demonstrated that nanoparticles coated with 1% v/v polysorbate 80 were able to reach the HIV reservoirs in an amount higher than that of uncoated stavudine nanoparticles or pure drug itself.
Conclusion: The method adopted is simple and the biodistribution studies demonstrated that nanoparticles coated with 1% polysorbate 80 were able to reach the selected organs in an amount higher than that of uncoated stavudine nanoparticles or pure drug itself.
GENETIC SUSCEPTIBILITY OF TRANSCRIPTION FACTOR 7-LIKE 2 GENE VARIANT AND RISK OF TYPE 2 DIABETES IN ASIAN INDIANS
Authors: NAVNEET KAUR  , GURJIT KAUR BHATTI  , SANJAY KUMAR BHADADA  , SAMER SINGH  , JASVINDER SINGH BHATTI  
Published: October 2019

Background: The variants of transcription factor 7-like 2 (TCF7L2) gene have been shown to be associated with type 2 diabetes mellitus (T2DM) and its related complications.
Objectives: We aimed to explore the possible association of rs7903146 (C/T) variant in TCF7L2 with the risk of T2DM in the North Indian population.
Methods: The present case–control study included a total of 638 human subjects (318 T2DM subjects and 320 healthy controls). Various anthropometric, biochemical, and genetic parameters were studies in all the subjects. Genotyping of TCF7L2 gene was carried out using allele-specific polymerase chain reaction method.
Results: The results of this study indicate significantly higher values of body mass index, waist circumference, waist-to-hip ratio, and body fat (%) in T2DM subjects than controls (p≤0.001). Dyslipidemia represented by higher levels of triglycerides and reduced values of high-density lipoprotein was more predominant in diabetic subjects compared to healthy subjects. The frequency of risk genotype (TT) frequency was significantly higher in T2DM subjects (16.4%) compared to controls (11.6%). The “T” allele was more dominant in diabetic subjects than controls. Logistic regression analysis of the data revealed a significant association of TT genotype with 2-fold (odds ratio with 95% of confidence interval; 2.09 [1.29–3.42] p=0.003) and CT genotype with 1.7-fold (1.73 [1.23–2.44] p=0.002) increased risk of developing T2DM.
Conclusions: The present study demonstrated a significant association of rs7903146 (C/T) variant in TCF7L2 with the augmented risk of T2DM in North Indian population.
“La Educación Ambiental”, un desafio en la construcción del currículo pertinente para los territorios en Posacuerdo
Authors: Castro Juan Jose , Gómez Hernández Mercy Yomaira 
Published: October 2019

Los habitantes de los territorios afectados por la violencia en Colombia, han vivido el drama de la desaparición de familiares, la pérdida de vecinos, el maltrato, las violaciones, la perdida de sus tierras, deterioro del medio ambiente y el desplazamiento. Factores que desestabilizaron y marcaron la vida de quienes la padecieron y que luego del proceso de paz logran vivir con un poco de más tranquilidad, requiriendo de una educación pertinente que contribuya a dar repuesta a sus necesidades.
Dentro de la investigación denominada “Pertinencia de la Educación Ambiental en el Posacuerdo”, adelantada por los autores, arroja como resultados la poca pertinencia de los procesos curriculares en los establecimientos educativos, siendo escasa la generación de alternativas apropiadas para la articulación de la Educación Ambiental, requiriendo la vinculación de la comunidad educativa en la construcción del Proyecto Ambiental Escolar, empleando como ejes del aprendizaje y de práctica pedagógica la mitigación de los impactos ambientales provocados por el conflicto armado.
MODERN APPROACHES TO EARLY RADIOLOGICAL DIAGNOSIS OF BONE AND CEREBRAL METASTASES OF PERIPHERAL NON-SMALL CELL LUNG CANCER
Authors: Laryukov A. V. , Laryukova E. K. , Mikhailov M. K. 
Published: October 2019

Objective:сonstructive principles development of early diagnosis of bone and cerebral metastases of peripheral non-small cell lung cancer (PNSCLC), is based on the targeted preventive and personalized application of radiological and nuclear diagnostic methods.Materials and methods.There was performed the retrospective analysis of medical cards of 1473 patients with peripheral non-small cell lung cancer for the evaluation of the characteristics and frequency of bones and brain metastases. The frequency and features of bone and brain metastases depending on clinical and morphological features of the primary lung tumor were studied. 118 patients with PNSCLC with bone and brain metastases, regardless of clinical symptoms, were examined using a wide range of modern radiological and nuclear methods.Conclusion:the original algorithm has been developed on the study of the diagnostic significance of medical imaging methods. The application of this algorithm will significantly improve the early diagnosis of bone and cerebral metastases and improve the staging of PNSCLC.