bluuebunny/crossref_metadata_2025_split huggingface dataset:
FORMULATION AND EVALUATION OF EXTENDED RELEASE PELLETS OF PIOGLITAZONE HYDROCHLORIDE USING NATURAL AND SYNTHETIC POLYMERS BY FLUIDIZED BED COATING TECHNIQUE
Authors: B GOWTHAMI , S NIHITHA , NAGAM SANTHI PRIYA , NADENDLA RAMA RAO 
Published: October 2019

Objective: The objective of the current work was to develop Pioglitazone hydrochloride (HCl) pellets coated with natural polymer extracted from peas gum and also to compare the drug release profile with coatings containing semi-synthetic and synthetic polymers.
Methods: Fluidized bed coating technique was used to develop pellets. A 22 factorial design was employed to study the effect of independent variables (inlet air temperature and spray rate), on dependent variables (percentage entrapment efficiency, percentage friability, and average particle size). Optimization was done by fitting experimental data to the software program. Obtained pellets were subjected to different evaluation parameters which are critical in the development of the dosage form. An in vitro lag phase study was carried out for all batches in simulated gastric fluid (0.1N HCl) for 5 h and in vitro drug release study was carried out for optimized batch (E-2 and P-3) in simulated intestinal fluid (pH 7.4 phosphate buffer).
Results: The optimized batches E-2 and P-3 showed satisfactory percentage entrapment efficiency of 92.66±1.52, percentage friability of 0.57±0.03, and average particle size of 1424±16 μm. All batches maintained lag phase for 5 h in 0.1N HCl. An optimized batch of two different sizes exhibited a burst release within 30 min in a simulated intestinal fluid with no significant difference in release rate constant (*p>0.05) and followed first-order kinetics.
Conclusion: Thus, Pioglitazone HCl pulsatile pellets were successfully developed for treating diabetes mellitus by fluidized bed coating technique employing factorial design.
DESIGN, SYNTHESIS, MOLECULAR DOCKING, AND EVALUATION OF CHROMONE BASED TETRAZOLE DERIVATIVES
Authors: CHOPRA ANUJA , SINGH LAKHWINDER , VK KAPOOR , DHINGRA RICHA , DHINGRA NEELIMA 
Published: October 2019

Objectives: The objective of this research work was to design, synthesize, study the molecular docking, and evaluate the antimicrobial activity of some novel substituted 2-(Phenylamino)-3-(1H-tetrazol-5-yl)-4H-chromen-4-one derivatives (12a-h).
Methods: In the present work, 3-Formylchromones were transformed into pharmacologically active substituted 2-(Phenylamino)-3-(1H-tetrazol-5- yl)-4H-chromen-4-one derivatives (12a-h) through a multistep reaction. Initially, synthesis of the substituted 4-Oxo-2-(phenylamino)-4H-chromone-3- carbaldehydes (9a-h) was carried out using substituted acetophenones (6a-h) as starting material and by employing an earlier reported method (1,3-dipolar cycloaddition reaction). Then, these synthesized compounds were converted into respective oximes (10a-h).The obtained oximes (10a-h) were further converted into nitriles (11a-h) which were finally subjected to concerted cycloaddition through stepwise addition of neutral or anionic azide species to furnish final substituted 2-(Phenylamino)-3-(1H-tetrazol-5-yl)-4H-chromen-4-one derivatives (12a-h). All the newly synthesized compounds (12a-h) and a reference compound (ciprofloxacin) were docked into the active site of TyrRS (PDB: 1JIK) by means of the BioPredicta module of VLife MDS. The synthesized compounds (12a-h) were also evaluated in vitro for their antibacterial (against Staphylococcus aureus, Bacillus subtilis, Pseudomonas aeruginosa, and Escherichia coli bacterial stains) and antifungal activities (against Aspergillus niger and Candida albicans fungal strains) using Zone of Inhibition method.
Results: The formation of substituted 2-(Phenylamino)-3-(1H-tetrazol-5-yl)-4H-chromen-4-one derivatives (12a-h) was confirmed through their spectral analysis, that is, 1H-NMR, 13C-NMR, and Mass spectroscopy. During docking study, the recorded molecular binding interactions revealed that all the newly synthesized compounds (12a-h) interacted well with binding site of the enzyme. The synthesized compounds were also evaluated in vitro for their antibacterial (against S. aureus, B. subtilis, P. aeruginosa, and E. coli bacterial stains) and antifungal activities (against A. niger and C. albicans fungal strains). All the synthesized compounds exhibited moderate-to-potent antimicrobial activities.
Conclusions: All the synthesized compounds exhibited moderate-to-potent antimicrobial activity.
GAS CHROMATOGRAPHY-MASS SPECTROMETRIC ANALYSIS AND IDENTIFICATION OF BIOACTIVE CONSTITUENTS OF CATHARANTHUS ROSEUS AND ITS ANTIOXIDANT ACTIVITY
Authors: RANI JYOTI , KAPOOR MANISH 
Published: October 2019

Objective: The main objectives of this study were analysis of the phytochemicals produced by two different Catharanthus roseus morphotypes, i.e., pink and white flowered and evaluate it morphologically and phytochemically in terms of total phenolic content (TPC), total flavonoid content (TFC), antioxidant properties, and gas chromatography-mass spectrometry (GC-MS) analysis.
Methods: Methanolic extracts of both morphotypes were prepared by Soxhlet apparatus. After extraction, the extracts were filtered and solvent removed by rotatory evaporator. TPC was determined by Folin–Ciocalteu reagent method and TFC was estimated by aluminum chloride colorimetric method. Antioxidant and free radical scavenging activities were estimated by superoxide dismutase and 1,1-diphenyl-2-picrylhydrazyl assay. GC-MS analysis was performed at Central Instrumentation Laboratory/ SAIF, Panjab University, Chandigarh.
Results: Pink-flowered C. roseus showed highest activities in terms of TPC, TFC, and antioxidant activity as compared to white-flowered C. roseus. 42 different bioactive compounds were detected in the methanolic extract of pink, while only 7 compounds were identified in white-flowered C. roseus. The identification was performed by GS-MS analysis mainly based on retention time, peak area, molecular formula, and molecular weight.
Conclusion: The finding indicated that the pink-flowered C. roseus was phytochemically superior then the white one.
SYNTHESIS OF NEW BORON COMPOUNDS WITH AMOXICILLIN AND SOME OF ITS METAL COMPLEXES WITH USE THEM IN ANTIBACTERIAL, ASSESSMENT OF HEPATOPROTICTIVE AND KIDNEYACTIVITY, ANTICANCER AND ANTIOXIDANT APPLICATIONS
Authors: AL-JEBOURI GHANEM SH , NOORIKHALEEL ASMAA MOHAMMED 
Published: October 2019

Objective: New ligand ({7-[2-amino-2-(4-hydroxyphenyl)-acetamido-3,3-dimethyl-6-oxo-2-thia-5-aza bicyclo[3,2,0]heptane-4-carboxylic boric anhydride}) with its Co (II), Ni (II) and Cu (II) complexes. And new mixed ligand copper complex was synthesized.
Methods: The ligand was synthesized by the reaction of boric acid with amoxicillin (1:1) and the mixed ligand complex has been synthesized by the reaction of the ligand, 4-aminoantipyrine and Cu (II) ion (1:1:1).
Results: All studied compounds were characterized by the spectral method: Fourier transform infrared, ultraviolet-visible, thermal analysis (TG and DTG), flame atomic absorption and nuclear magnetic resonance. Also CHNS, melting point, magnetic susceptibility and molar conductivity.
Conclusion: According to the obtained data, all complexes were non electrolyte and the geometry was octahedral for all complexes. All synthesized compounds were tested as antibacterial agents against Escherichia Coli, Pseudomonas auroginosa as Gram-negative bacteria (G-) and Staphylococcus aureus epidermis as Gram-positive bacteria (G+). The results showed that copper complexes were more active in (10-2M) than the other compounds. The medicinal applications (hepatoprotective and kidney in serum of mice, histopathological of liver and kidney, anticancer and antioxidant in human cell were studied of the synthesized compounds and gave a good results in all tested.
ANTICANCER AND FREE RADICAL SCAVENGING POTENTIAL OF THE MARINE ALGICOLOUS ENDOPHYTIC FUNGUS CLADOSPORIUM UREDINICOLA
Authors: THIRUMALANADHUNI VASAVI , YERRAGURAVAGARI LAVANYA LATHA , MATHAKALA VANI , PALEMPALLI UMA MAHESWARI DEVI 
Published: October 2019

Objective: The objective was to study the antioxidant and anticancer potential of the endophytic fungus Cladosporium uredinicola, isolated from the marine brown alga Dictyota dichotoma.
Methods: Anticancer effect of the endophytic fungal extract was evaluated by 3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay using MDA-MB-231 human mammary adenocarcinoma cells as in vitro cancer models. 3T3-L1 pancreatic adipocytes were used as in vitro models for the evaluation of cytotoxic activity against normal cells using MTT assay. Free radical scavenging activity was assessed by 2, 2-diphenyl-1- picrylhydrazyl (DPPH) assay.
Results: The ethyl acetate extract of the endophytic fungus showed potent cytotoxic activity against MDA-MB-231 human breast adenocarcinoma cell lines with an inhibitory concentration (IC50) value of 373 μg/ml and a very mild cytotoxic effect on 3T3-L1 Cells with an IC50 value of 2403 μg/ml. DPPH free radical scavenging assay of the extract showed an IC50 value of 359 μg/ml indicating its potential free radical scavenging activity.
Conclusion: The results indicated that the endophytic fungus C. uredinicola, isolated from the marine brown alga D. dichotoma, acts as a potential source for anticancer and antioxidant metabolites. Moreover, these anticancer metabolites were observed to be less toxic to the normal cells, which make them prospective therapeutic agents.
EFFECTIVENESS OF GABAPENTIN USAGE TOWARD REDUCING PAIN INTENSITY LEVEL AND QUALITY OF LIFE OF POST-STROKE NEUROPATHIC PATIENTS IN REGIONAL GENERAL HOSPITAL, WEST NUSA TENGGARA PROVINCE YEAR 2018
Authors: QIYAAM NURUL , ADIKUSUMA WIRAWAN , NOPITASARI BAIQ LENY , ANDAYANI TRI MURTI , AMINI AULIA 
Published: October 2019

Objective: Stroke is defined as a sudden loss of brain function due to blockade/rupture of the brain’s blood vessels. Data collected by the Indonesian Stroke Foundation show that Indonesia ranks first in Asia as the country with the highest number of stroke sufferers. The purpose of this study was to determine the effectiveness of the use of gabapentin to reduce pain intensity and improve the quality of life of post-stroke neuropathic pain in NTB Province hospital patients.
Methods: This study was carried out in the period of June–July 2018. The targeted population was all post-stroke neuropathic patients who received gabapentin therapy in NTB provincial hospital. Affordable populations are post-stroke neuropathic pain patients who seek outpatient treatment at NTB provincial hospital that meets the inclusion and exclusion criteria. The results of the data will be analyzed using paired sample t-test. Obtained 15 patients were willing to participate in this study.
Results: The results of the study using questionnaire EQ-5D-3L after using gabapentin for 2 weeks. Patients experienced an improvement in the quality of life in each dimension items, namely the ability to walk/move from 6.7%, no problem to 60%, no self-care, 26.7% no problem to be 80% without problems, usual activities carried out from 13.3% had no problems to 46.7% had no problems, feeling of pain/discomfort from 60% having moderate problems to 60% had no problems, and anxiety/depression of 60% had no problem being 100% has no problem. While the measurement of the quality of life using the EQ-VAS questionnaire, there was a significant improvement in the quality of life between before and after using gabapentin at 32.66.
Conclusion: The use of gabapentin has effectiveness on reduction of pain intensity and the quality of life of post-stroke neuropathic patients in regional general hospital, West Nusa Tenggara Province year 2018.
ETHNOBOTANICAL AND ETHNOVETERINARY IMPORTANCE OF PLANTS OF SCRUB AREAS OF DACHIGAM NATIONAL PARK, JAMMU AND KASHMIR, INDIA
Authors: MALIK ARIF YAQOOB , SINGH D.P 
Published: October 2019

Objective: The rich plant diversity of mountains has been used by the indigenous people for thousands of years as health-care remedies. A study on the important plant communities of scrub ecosystems of Dachigam National Park was carried out with the special aim of enlisting the ethnobotanical, and ethnoveterinary uses of plants being used by the people of the area.
Methods: Data were collected by visual appraisal approach, rapid rural approach, and questionnaire methods coupled with group meetings and field discussions.
Results: Data collected from the present investigation indicate that 59 plants belonging to 33 families with Rosaceae, the dominant family, were exclusively used for ethnobotanical purposes and 10 plant species belonging to 8 families were having ethnoveterinary use. These species include 14 medicinal species, 10 vegetable species, 10 with edible species, 6 fodder species, 6 species used as tea substitutes, 3 species for menstrual problems, 3 species used for religious ceremonies, 2 species used for chutney, 2 art and craft species, and 1 species used for ornamental, fuelwood, and agricultural tools each.
Conclusion: The people of the area are exclusively dependent on medicinal plants using traditional knowledge that provides them with the best therapeutic and economic benefits. Such traditional knowledge could be valuable for developing local and regional conservation strategies for these fragile ecosystems. There is an urgent need to thoroughly analyze the secondary metabolite properties of such plants to validate their authenticity in the local health-care systems.
ANTIOXIDANT EFFECT OF VITAMINS COMBINED A, C, AND E DOSE ON TYPE 2 DIABETIC PATIENTS
Authors: GOZIF MOHAMMED N OMAR  , FADEL YOUSIF AL-ARABI  , MANSOUR ABDULNABI H MEHDI  , MADHUKAR M FAWADE  
Published: October 2019

Objectives: This study is to investigate the effect of oral Vitamins combined (A, C, and E) with metformin on the levels of fasting blood sugar (FBS), postprandial blood sugar (PPBS), hemoglobin (HbA1c), total cholesterol (TC), triglycerides (TG), high-density lipoprotein (HDL), and low-density lipoprotein (LDL) in Type 2 diabetic patients.
Methods: A total of 32 patients with Type 2 diabetes were divided randomly into A and B groups, i.e., 16 per each group. Group A received metformin only twice a day while Group B received one tablet of Antox and metformin twice a day for 3 months. FBS, PPBS, HbA1c, TC, TG, LDL, and HDL were measured before and after the dose, and the results were analyzed statistically.
Results: A significant decreases in FBS, PPBS, HbA1c, TC, TG, and LDL whereas results showed increasing significance in HDL level that seen in the patients of Group B which received Antox and metformin compared to the group which received metformin only. In conclusion, the results indicate that daily consumption of supplementary vitamins with metformin leads to improving blood glucose and lipids in patients with Type 2 diabetes and reducing the risk of complications. Hence, the dose can be used combined Vitamins A, C, and E with metformin in the treatment of Type 2 diabetes by maintaining good glycemic control.
IN VITRO STUDIES ON THE SYNERGISTIC EFFECT OF MORINDA CITRIFOLIA L. (NONI) AND METHOTREXATE ON CYTOTOXICITY OF HELA CELL LINES
Authors: MHATRE BHAKTI  , MARAR THANKAMANI  
Published: October 2019

Objective: Cancer remains to be one of the leading causes of death around the world. Modern targeted therapies have undeniably improved cancer patients’ survival, but search still continues for safer and more effective drugs. This work is an attempt to assess the effectiveness of cotreatment of aqueous fruit extract of Morinda citrifolia L. (Noni) on methotrexate (MTX)-induced cytotoxicity on HeLa cancer cell line.
Methods: HeLa cells were treated with different concentrations of MTX and Noni alone and in combination for 24 and 48 h and studied for the cytotoxic effects by various approaches.
Results: There was a dose-dependent inhibition of growth when treated with MTX in a dose range of 0.045–45.4 μg/ml and Noni for a dose range of 0.3–30 mg/ml for 48 h. The IC50 for MTX was 4.45 μg/ml (1 μM/ml), and for Noni, it was 8 mg/ml while the combination exhibited a more intensive growth inhibitory effect. Our results were confirmed with phase-contrast microscopy, whereby the number of viable cells decreased with an increase in the concentration of Noni. Cells were found to have rounded up and detached from the flask indicating apoptosis. Apoptosis in HeLa cell lines was further confirmed by DNA fragmentation and flow cytometry.
Conclusion: It can be concluded that Noni may enhance MTX cytotoxicity by inducing apoptosis and cell cycle arrest. Hence, cotreatment with Noni may reduce the dosage of MTX necessary for inhibiting proliferation of malignant cells and hence decrease the toxic effects of MTX on the system.
OPTIMIZATION OF COMPONENT VARIABLES BY STATISTICAL APPROACH FOR DESIGN OF CHRONOTHERAPEUTIC DOSAGE FORM FOR HYPERTENSION
Authors: SHAILESH SHARMA  , NIMRATA SETH  
Published: October 2019

Objective: Blood pressure (BP) pursues circadian rhythms projecting its highest values during early morning and lowest during night. The aim of the present investigation was to design a newer programmable chronotherapy based capsule system containing delayed release microspheres of losartan potassium for effective management of hypertension.
Methods: First, the microspheres were prepared with Eudragit RS100 by optimization technique through the application of Design Expert® software. The optimized microsphere formulation was filled in a capsule shell, and these shells were coated with 10% w/v Eudragit L100:Eudragit S100 (in ratio 1:2), in isopropyl alcohol: water as solvent system, to provide the necessary delay in emptying of capsule content. The whole capsular system was evaluated by various characteristic formulation parameters. Validation of optimization model and statistical interpretation of results was done using analysis of variance.
Results: The results indicated that the optimized triple coated capsule shells showed an extended release of drug from microspheres after a lag time of 4 h.
Conclusion: Conclusively, the chronotherapeutic system of losartan potassium was successfully developed to be dosed at bedtime that could benefit from the known circadian rhythms of the disease to control the BP for once a day therapy
STABILITY-INDICATING REVERSE-PHASE HIGH-PERFORMANCE LIQUID CHROMATOGRAPHY METHOD FOR THE SIMULTANEOUS QUANTIFICATION OF APIGENIN AND LUTEOLIN FROM ACHILLEA MILLEFOLIUM LINN
Authors: GOMATHY SUBRAMANIAN  , S.N.MEYYANATHAN  , GOWRAMMA BYRAN  
Published: October 2019

Objective: A stability-indicating reverse-phase high-performance liquid chromatographic method was developed and validated for the analysis of apigenin and luteolin. The degradation behavior of apigenin and luteolin was investigated under different stress conditions as recommended by the International Conference on Harmonization (ICH).
Methods: In the present study, a reversed-phase high-performance liquid chromatography method was developed and the resolution of the plant constituents was successfully achieved using Hibar Lichrospher C8 column with ultraviolet detector at a wavelength of 269 nm. The mobile phase consisted of methanol and 0.5% trifluoroacetic acid (80:20 v/v) at a flow rate of 1.0 ml/min. Both apigenin and luteolin were subjected to various stress degradation studies such as oxidation, acid and alkaline hydrolysis, and photolytic degradation.
Results: The proposed method was found to be linear (1–5 μg/ml) with the linear correlation coefficient of R2=0.99. Although the degradation products of stressed conditions were not identified, the methods were able to detect the changes due to stress condition.
Conclusion: The method provides good sensitivity and excellent precision and reproducibility. Forced degradation studies on apigenin and luteolin give information about their storage and intrinsic stability conditions considering the advanced pharmaceutical aspects of formulations.
BIOAVAILABILITY AND DISSOLUTION ENHANCEMENT OF GLYBURIDE NANOSUSPENSION
Authors: PRADEEP KUMAR M  
Published: October 2019

Objective: The main objective was to develop nanosuspension of glyburide (GLY) by quasi emulsification solvent diffusion method and to enhance dissolution and bioavailability characteristics of the drug GLY, an antidiabetic drug which belongs to Biopharmaceutical Classification System-II category.
Materials and Methods: In this work, nanoparticles were prepared using polyvinyl alcohol, hydroxypropyl methyl cellulose, and Eudragit RL100. Twelve formulations of GLY (GLY-1–GLY-12) were formulated using the excipients at various compositions. Drug and excipient compatibility studies were conducted using Fourier transform infrared and differential scanning calorimeter. The prepared nanosuspension was analyzed using scanning electron microscopy for surface of the particle analysis, melting point, solubility, particle charge zeta (mv), percentage drug entrapment efficiency (%), and in vitro drug release. The optimized formulations of nanosuspension were further studied for in vivo pharmacokinetic evaluation. Reverse-phase high-performance liquid chromatography method was developed, validated, and used for the study of these formulations in rat plasma.
Results: From these studies, it was confirmed that drugs and excipients chosen were compatible with each other. GLY-8 was the best formulation with a particle size of 85–96 nm with 168.7°C melting point, freely soluble in phosphate buffer pH 7.4, 93.53% drug entrapment, and 90.26±1 mV of zeta potential. This formulation shows percentage drug release of 99.85% in 24 h. In vivo pharmacokinetic study for optimized formulation (GLY -8) suggested that there was no reaction with the rat plasma. From the results, it was shown that Cmax and Tmax were found to be 0.604±0.03 μg/ml and 2±1.01 h, respectively. The values of t1/2 (h), area under the curve (AUC) (0-t), and AUC (0-∞) were found to be 10.04 h, 2.562±0.41 μg.h/ml, and 2.147±0.45 μg.h/ml, respectively.
Conclusion: Based on the results obtained, oral administration of nanosuspension could not only provide the better absorption of poorly water soluble drugs but may also reduce toxicity and provide a new tool in drug delivery system.
BLOOD PRESSURE LOWERING EFFECT OF POLYHERBAL PREPARATION CONTAINING ALLIUM SATIVUM, BELERICAE FRUCTUS, CURCUMA AERUGINOSA, AND AMOMI FRUCTUS ON RAT MODEL OF HYPERTENSION
Authors: DWI ARIS AGUNG NUGRAHANINGSIH  , SHOLIKHAH EN  , MUSTOFA M  , YULIANI FS  , PURWONO S  , NGATIDJAN N  
Published: October 2019

Objective: The study aimed to investigate the blood pressure lowering effect of the polyherbal preparation contains Allium sativum, Belericae fructus, Curcuma aeruginosa, and Amomi fructus in the animal model of hypertension.
Methods: Deoxycorticosterone acetate uninephrectomy salt rat model was used to develop hypertension model. Hypertensive rats were divided into five groups that were no treatment (negative control group [NEG]), hydrochlorothiazide treatment, polyherbal preparation 63 mg/kg treatment (DOSE 1), polyherbal preparation 126 mg/kg treatment (DOSE 2), and polyherbal preparation 252 mg/kg treatment (DOSE 3). The treatment was started after hypertension developed and given for 3 weeks.
Results: The result showed that the mean of systolic blood pressure in DOSE 2 group was significantly lower compared with those on NEG group (145.86 mmHg vs. 174.71 mmHg, p<0.05).
Conclusion: Our study provides evidence to support the use of the polyherbal preparation containing A. sativum, B. fructus, C. aeruginosa, and A. fructus for lowering blood pressure.