Search results for: Antibacterial drugs
Commenced in January 2007
Frequency: Monthly
Edition: International
Paper Count: 199

Search results for: Antibacterial drugs

139 The Effect of Substitution of CaO/MgO and CaO/SrO on in vitro Bioactivity of Sol-Gel Derived Bioactive Glass

Authors: Zeinab Hajifathali, Moghan Amirhosseinian

Abstract:

This study had two main aims: firstly, to determine how the individual substitution of CaO/MgO and CaO/SrO can affect the in vitro bioactivity of sol-gel derived substituted 58S bioactive glass (BG) and secondly to introduce a composition in the 60SiO2–(36-x)CaO–4P2O5–(x)MgO and 60SiO2–(36-x)CaO–4P2O5–(x)SrO quaternary systems (where x= 0, 5, 10 mol.%) with enhanced biocompatibility, alkaline phosphatase (ALP) activity, and more efficient antibacterial activity against MRSA bacteria. Results showed that both magnesium-substituted bioactive glasses (M-BGs) and strontium- substituted bioactive glasses (S-BGs) retarded the Hydroxyapatite (HA) formation. Meanwhile, magnesium had more pronounced effect. The 3-(4, 5dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) and ALP assays revealed that the presence of moderate amount (5 mol%) of Mg and Sr had a stimulating effect on increasing of both proliferation and differentiation of MC3T3-E1 cells. Live dead and Dapi/actin staining revealed both substitution of CaO/MgO and CaO/SrO resulted in more biocompatibility and stimulation potential of the MC3T3 cells compared with control. Taken together, among all of the synthesized magnesium substituted (MBGs) and strontium substituted (SBGs), the sample 58- BG with 5 mol% CaO/MgO substitution (BG-5M) was considered as a multifunctional biomaterial in bone tissue regeneration field with enhanced biocompatibility, ALP activity as well as the highest antibacterial efficiency against methicillin-resistant Staphylococcus aureus (MRSA) bacteria.

Keywords: Apatite, alkaline earth, bioactivity, biomedical applications, sol-gel.

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138 Influence of Natural Gum on Curcumin Supersaturation in Gastrointestinal Fluids

Authors: Patcharawalai Jaisamut, Kamonthip Wiwattanawongsa, Ruedeekorn Wiwattanapatapee

Abstract:

Supersaturation of drugs in the gastrointestinal tract is one approach to increase the absorption of poorly water-soluble drugs. The stabilization of a supersaturated state was achieved by adding precipitation inhibitors that may act through a variety of mechanisms. In this study, the effect of the natural gums, acacia, gelatin, pectin and tragacanth on curcumin supersaturation in simulated gastric fluid (SGF) (pH 1.2), fasted state simulated gastric fluid (FaSSGF) (pH 1.6), and simulated intestinal fluid (SIF) (pH 6.8) was investigated. The results indicated that all natural gums significantly increased the curcumin solubility (about 1.2-6-fold) when compared to the absence of gum, and assisted in maintaining the supersaturated drug solution. Among the tested gums, pectin at 3% w/w was the best precipitation inhibitor with a significant increase in the degree of supersaturation about 3-fold in SGF, 2.4-fold in FaSSGF and 2-fold in SIF.

Keywords: Curcumin, Solubility, Supersaturation, Precipitation inhibitor.

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137 Formulation and Technology of the Composition of Essential Oils as a Feed Additive in Poultry with Antibacterial Action

Authors: S. Barbaqadze, M. Goderdzishvili, E. Mosidze, L. Lomtadze, V. Mshvildadze, L. Bakuridze, D. Berashvili, A. Bakuridze

Abstract:

This paper focuses on the formulation of phytobiotic designated for further implantation in poultry farming. Composition was meant to be water-soluble powder containing antibacterial essential oils. The development process involved Thyme, Monarda and Clary sage essential oils. The antimicrobial activity of essential oils composite was meant to be tested against gram-negative and gram-positive bacterial strains. The results are processed using the statistical program Sigma STAT. To make essential oils composition water soluble surfactants were added to them. At the first stage of the study, nine options for the optimal composition of essential oils and surfactants were developed. The effect of the amount of surfactants on the essential oils composition solubility in water has been investigated. On the basis of biopharmaceutical studies, the formulation of phytobiotic has been determined: Thyme, monarda and clary sage essential oils 2:1:1 - 100 parts; Licorice extract 5.25 parts and inhalation lactose 300 parts. A technology for the preparation of phytobiotic has been developed and a technological scheme for the preparation of phytobiotic has been made up. The research was performed within the framework of the grant project CARYS-19-363 funded be the Shota Rustaveli National Science Foundation of Georgia.

Keywords: Clary, essential oils, monarda, phytobiotics, poultry, thyme.

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136 Effect of Different Model Drugs on the Properties of Model Membranes from Fishes

Authors: M. Kumpugdee-Vollrath, T. G. D. Phu, M. Helmis

Abstract:

A suitable model membrane to study the pharmacological effect of pharmaceutical products is human stratum corneum because this layer of human skin is the outermost layer and it is an important barrier to be passed through. Other model membranes which were also used are for example skins from pig, mouse, reptile or fish. We are interested in fish skins in this project. The advantages of the fish skins are, that they can be obtained from the supermarket or fish shop. However, the fish skins should be freshly prepared and used directly without storage. In order to understand the effect of different model drugs e.g. lidocaine HCl, resveratrol, paracetamol, ibuprofen, acetyl salicylic acid on the properties of the model membrane from various types of fishes e.g. trout, salmon, cod, plaice permeation tests were performed and differential scanning calorimetry was applied.

Keywords: Fish skin, model membrane, permeation, DSC, lidocaine HCl, resveratrol, paracetamol, ibuprofen, acetyl salicylic acid.

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135 Biological Effects of a Carbohydrate-Binding Protein from an Annelid, Perinereis nuntia Against Human and Phytopathogenic Microorganisms

Authors: Sarkar M. A. Kawsar, Sarkar M. A. Mamun, Md S. Rahman, Hidetaro Yasumitsu, Yasuhiro Ozeki

Abstract:

Lectins have a good scope in current clinical microbiology research. In the present study evaluated the antimicrobial activities of a D-galactose binding lectin (PnL) was purified from the annelid, Perinereis nuntia (polychaeta) by affinity chromatography. The molecular mass of the lectin was determined to be 32 kDa as a single polypeptide by SDS-PAGE under both reducing and non-reducing conditions. The hemagglutinating activity of the PnL showed against trypsinized and glutaraldehyde-fixed human erythrocytes was specifically inhibited by D-Gal, GalNAc, Galβ1-4Glc and Galα1-6Glc. PnL was evaluated for in vitro antibacterial screening studies against 11 gram-positive and gram-negative microorganisms. From the screening results, it was revealed that PnL exhibited significant antibacterial activity against gram-positive bacteria. Bacillus megaterium showed the highest growth inhibition by the lectin (250 μg/disc). However, PnL did not inhibit the growth of gram-negative bacteria such as Vibrio cholerae and Pseudomonas sp. PnL was also examined for in vitro antifungal activity against six fungal phytopathogens. PnL (100 μg/mL) inhibited the mycelial growth of Alternaria alternata (24.4%). These results indicate that future findings of lectin applications obtained from annelids may be of importance to life sciences.

Keywords: Perinereis nuntia, Lectin, Inhibition zone, Mycelial growth.

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134 Anti-microbial Activity of Aristolochic Acid from Root of Aristolochia bracteata Retz

Authors: S. Angalaparameswari, T.S. Mohamed Saleem, M. Alagusundaram, S. Ramkanth, V.S. Thiruvengadarajan, K. Gnanaprakash, C. Madhusudhana Chetty, G. Pratheesh

Abstract:

The present research was designed to investigate the anti-microbial activity of aristolochic acid from the root of Aristolochia bracteata. From the methanolic & ethyl extract extracts of Aristolochia bracteata aristolochic acid I was isolated and conformed through IR, NMR & MS. The percentage purity of aristolochic acid I was determined by UV & HPLC method. Antibacterial activity of extracts of Aristolochia bracteata and the isolated compound was determined by disc diffusion method. The results reveled that the isolated aristolochic acid from methanolic extract was more pure than the compound from ethyl acetate extract. The various extracts (500μg/disc) of Aristolochia bracteata showed moderate antibacterial activity with the average zone of inhibition of 7-18 mm by disc diffusion method. Among the extracts, ethyl acetate & methanol extracts were shown good anti-microbial activity and the growth of E.coli (18 mm) was strongly inhibited. Microbial assay of isolated compound (Aristolochic acid I) from ethyl acetate & methanol extracts were shown good antimicrobial activity and the zone of inhibition of both at higher concentration 50 μg/ml was similar with the standard aristolochic acid. It may be concluded that the isolated compound of aristolochic acid I has good anti-bacterial activity.

Keywords: Aristolochic acid I, Anti-microbial activity, Aristolochia bracteata, Bacillus subtilis, E.coli

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133 In silico Studies on Selected Drug Targets for Combating Drug Resistance in Plasmodium falcifarum

Authors: D. Bhaskar, N. R. Wadehra, M. Gulati, A. Narula, R. Vishnu, G. Katyal

Abstract:

With drug resistance becoming widespread in Plasmodium falciparum infections, the development of the alternative drugs is the desired strategy for prevention and cure of malaria. Three drug targets were selected to screen promising drug molecules from the GSK library of 13469 molecules. Using an in silico structure-based drug designing approach, the differences in binding energies of the substrate and inhibitor were exploited between target sites of parasite and human to design a drug molecule against Plasmodium. The docking studies have shown several promising molecules from GSK library with more effective binding as compared to the already known inhibitors for the drug targets. Though stronger interaction has been shown by several molecules as compared to the reference, few molecules have shown the potential as drug candidates though in vitro studies are required to validate the results. In case of thymidylate synthase-dihydrofolatereductase (TS-DHFR), three compounds have shown promise for future studies as potential drugs.

Keywords: Drug resistance, Drug targets, In silico studies, Plasmodium falciparum.

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132 Packaging the Alkaloids of Cinchona Bark in Combination with Etoposide in Polymeric Micelles Nanoparticles

Authors: Diky Mudhakir, Satrialdi, Sukmadjaja Asyarie, Yeyet C. Sumirtapura

Abstract:

Today, cancer remains one of the major diseases that lead to death. The main obstacle in chemotherapy as a main cancer treatment is the toxicity to normal cells due to Multidrug Resistance (MDR) after the use of anticancer drugs. Proposed solution to overcome this problem is the use of MDR efflux inhibitor of cinchona alkaloids which is delivered together with anticancer drugs encapsulated in the form of polymeric nanoparticles. The particles were prepared by the hydration method. The characterization of nanoparticles was particle size, zeta potential, entrapment efficiency and in vitro drug release. Combination nanoparticle size ranged 29-45 nm with a neutral surface charge. Entrapment efficiency was above 87% for the use quinine, quinidine or cinchonidine in combination with etoposide. The release test results exhibited that the cinchona alkaloids release released faster than that of etoposide. Collectively, cinchona alkaloids can be packaged along with etoposide in nanomicelles for better cancer therapy.

Keywords: Cinchona alkaloids, etoposide, MDR efflux inhitor, polymeric nanomicelles.

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131 Treatment of Mycotic Dermatitis in Domestic Animals with Poly Herbal Drug

Authors: U. Umadevi, T. Umakanthan

Abstract:

Globally, mycotic dermatitis is very common but there is no single proven specific allopathic treatment regimen. In this study, domestic animals with skin diseases of different age and breed from geographically varied regions of Tamil Nadu state, India were employed. Most of them have had previous treatment with native and allopathic medicines without success. Clinically, the skin lesions were found to be mild to severe. The trial animals were treated with poly herbal formulation (ointment) prepared using the indigenous medicinal plants – viz Andrographis paniculata, Lawsonia inermis and Madhuca longifolia. Allopathic antifungal drugs and ointments, povidone iodine and curabless (Terbinafine HCl, Ofloxacin, Ornidazole, Clobetasol propionate) were used in control. Comparatively, trial animals were found to have lesser course of treatment time and higher recovery rate than control. In Ethnoveterinary, this combination was tried for the first time. This herbal formulation is economical and an alternative for skin diseases.

Keywords: Allopathic drugs, dermatitis, domestic animals, poly herbal formulation.

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130 Molecular Dynamics and Circular Dichroism Studies on Aurein 1.2 and Retro Analog

Authors: Safyeh Soufian, Hoosein Naderi-Manesh, Abdoali Alizadeh, Mohammad Nabi Sarbolouki

Abstract:

Aurein 1.2 is a 13-residue amphipathic peptide with antibacterial and anticancer activity. Aurein1.2 and its retro analog were synthesized to study the activity of the peptides in relation to their structure. The antibacterial test result showed the retro-analog is inactive. The secondary structural analysis by CD spectra indicated that both of the peptides at TFE/Water adopt alpha-helical conformation. MD simulation was performed on aurein 1.2 and retro-analog in water and TFE in order to analyse the factors that are involved in the activity difference between retro and the native peptide. The simulation results are discussed and validated in the light of experimental data from the CD experiment. Both of the peptides showed a relatively similar pattern for their hydrophobicity, hydrophilicity, solvent accessible surfaces, and solvent accessible hydrophobic surfaces. However, they showed different in directions of dipole moment of peptides. Also, Our results further indicate that the reversion of the amino acid sequence affects flexibility .The data also showed that factors causing structural rigidity may decrease the activity. Consequently, our finding suggests that in the case of sequence-reversed peptide strategy, one has to pay attention to the role of amino acid sequence order in making flexibility and role of dipole moment direction in peptide activity. KeywordsAntimicrobial peptides, retro, molecular dynamic, circular dichroism.

Keywords: Antimicrobial peptides, retro, molecular dynamic, circular dichroism.

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129 Drug Combinations with Steroid Dispensing in Drugstores: A Study in the Center Area of Bangkok, Thailand

Authors: P. Thongmuang

Abstract:

The purposes of this research were 1) to survey the number of drugstores that unlawful dispense of asthma prescription drugs, in form of drug combinations in the Phaya Thai district of Bangkok, 2) to find the steroids contained in that drug combinations, 3) to find a means for informing general public about the dangers of drugs and for a campaign to stop dispensing them. Researcher collected drug combinations from 69 drugstores in Phaya Thai district from Feb 15, 2012 to Mar 15, 2012. The survey found 30.43%, 21, drug stores, sold asthma drug combinations to customers without a prescription. These collected samples were tested for steroid contamination by using Immunochromatography kits. Eleven samples, 52.38%, were found contaminated with steroids. In short, there should be control and inspection of drugstores in the distribution of steroid medications. To improve the knowledge of self health maintenance and drug usage among public, Thai Government and Department of Public Health should educate people about the side effects of using drug combinations and steroids.

Keywords: Dispensing, Drug Combinations, Steroids

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128 Biochemical Changes in the Liver of Mice after Exposure to Different Doses of Diclofenac Sodium

Authors: Deepak Mohan, Sushma Sharma

Abstract:

Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) are a group of widely used drugs for the treatment of rheumatoid diseases and to relieve pain and inflammation due to their analgesic anti-pyretic and anti-inflammatory properties. The therapeutic and many of the toxic effects of NSAIDs result from reversible inhibition of enzymes in the cyclooxygenase (COX) group. In the present investigation the effect of the drug on the concentration of lipids, and on the activity of the enzymes i.e. acid and alkaline phosphatase, GOT, GPT and lipid peroxidase were studied. There was a significant enhancement in the activities of both acid and alkaline phosphatase after 21 days of treatment. Proportionate increase in the MDA contents was observed after different days of diclofenac treatment. Cellular damage in the liver resulted in decrease in the activity of both GOT (Glutamate oxaloacetate transaminase) and GPT (Glutamate pyruvate transaminase) in both low and high dose groups. Significant decrease in the liver contents was also observed in both dose groups.

Keywords: Anti-inflammatory, cyclooxygenase, glutamate oxaloacetate transaminase, malondialdehyde.

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127 A Retrospective Drug Utilization Study of Antiplatelet Drugs in Patients with Ischemic Heart Disease

Authors: K. Jyothi, T. S. Mohamed Saleem, L. Vineela, C. Gopinath, K. B. Yadavender Reddy

Abstract:

Objective: Acute coronary syndrome is a clinical condition encompassing ST segments elevation myocardial infraction, Non ST segment is elevation myocardial infraction and un stable angina is characterized by ruptured coronary plaque, stress and myocardial injury. Angina pectoris is a pressure like pain in the chest that is induced by exertion or stress and relived with in the minute after cessation of effort or using sublingual nitroglycerin. The present research was undertaken to study the drug utilization pattern of antiplatelet drugs for the ischemic heart disease in a tertiary care hospital. Method: The present study is retrospective drug utilization study and study period is 6months. The data is collected from the discharge case sheet of general medicine department from medical department Rajiv Gandhi institute of medical sciences, Kadapa. The tentative sample size fixed was 250 patients. Out of 250 cases 19 cases was excluded because of unrelated data. Results: A total of 250 prescriptions were collected for the study according to the inclusion criteria 233 prescriptions were diagnosed with ischemic heart disease 17 prescriptions were excluded due to unrelated information. out of 233 prescriptions 128 are male (54.9%) and 105 patients are were female (45%). According to the gender distribution, the prevalence of ischemic heart disease in males are 90 (70.31%) and females are 39 (37.1%). In the same way the prevalence of ischemic heart disease along with cerebrovascular disease in males are 39 (29.6%) and females are 66 (62.6%). Conclusion: We found that 94.8% of drug utilization of antiplatelet drugs was achieved in the Rajiv Gandhi institute of medical sciences, Kadapa from 2011-2012.

Keywords: Angina pectoris, aspirin, clopidogrel, myocardial infarction.

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126 Carbamazepine Co-crystal Screening with Dicarboxylic Acids Co-Crystal Formers

Authors: Syarifah Abd Rahim, Fatinah Ab Rahman, Engku N. E. M. Nasir, Noor A. Ramle

Abstract:

Co-crystal is believed to improve the solubility and dissolution rates and thus, enhanced the bioavailability of poor water soluble drugs particularly during the oral route of administration. With the existing of poorly soluble drugs in pharmaceutical industry, the screening of co-crystal formation using carbamazepine (CBZ) as a model drug compound with dicarboxylic acids co-crystal formers (CCF) namely fumaric (FA) and succinic (SA) acids in ethanol has been studied. The co-crystal formations were studied by varying the mol ratio values of CCF to CBZ to access the effect of CCF concentration on the formation of the co-crystal. Solvent evaporation, slurry and cooling crystallization which representing the solution based method co-crystal screening were used. Based on the differential scanning calorimetry (DSC) analysis, the melting point of CBZ-SA in different ratio was in the range between 188oC-189oC. For CBZ-FA form A and CBZ-FA form B the melting point in different ratio were in the range of 174oC-175oC and 185oC-186oC respectively. The product crystal from the screening was also characterized using X-ray powder diffraction (XRPD). The XRPD pattern profile analysis has shown that the CBZ co-crystals with FA and SA were successfully formed for all ratios studied. The findings revealed that CBZ-FA co-crystal were formed in two different polymorphs. It was found that CBZ-FA form A and form B were formed from evaporation and slurry crystallization methods respectively. On the other hand, in cooling crystallization method, CBZ-FA form A was formed at lower mol ratio of CCF to CBZ and vice versa. This study disclosed that different methods and mol ratios during the co-crystal screening can affect the outcome of co-crystal produced such as polymorphic forms of co-crystal and thereof. Thus, it was suggested that careful attentions is needed during the screening since the co-crystal formation is currently one of the promising approach to be considered in research and development for pharmaceutical industry to improve the poorly soluble drugs.

Keywords: Carbamazepine, co-crystal, co-crystal former, dicarboxylic acid.

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125 Antimicrobial, Antiplasmid and Cytotoxicity Potentials of Marine Algae Halimeda opuntia and Sarconema filiforme Collected from Red Sea Coast

Authors: Samy A. Selim

Abstract:

The antimicrobial, antiplasmid and cytotoxic activities of marine algae Halimeda opuntia and Sarconema filiforme were investigated. Antimicrobial bioassay against some human pathogenic bacteria and yeast were conducted using disc diffusion method. Halimeda extract exhibited antibacterial activity against six species of microrganisms, with significant inhibition against Staphylococcus aureus. While Sarconema extract was better potent as antifungal against Candida albicans. Comparative antibacterial studies showed that Halimeda extract showed equivalent or better activity as compared with commercial antibiotic when tested against Staphylococcus aureus. Further tests conducted using dilution method showed both extracts as having bacteriostatic mode of action against the tested microorganisms. Methanol extract of two species showed significant cytotoxicity (LC50 <500μg) on brine shrimp. Halimeda opuntia showed highest cytotoxic activity (LC50 =192.3μg). Also, the present investigation was undertaken to investigate the ability of methanolic extract of the algal extracts to cure R-plasmids from certain clinical E. coli isolates. The active fraction of Halimeda and Sarconema could cure plasmids from E. coli at curing efficiencies of approximately 78%. The active fraction mediated plasmid curing resulted in the subsequent loss of antibiotic resistance encoded in the plasmids as revealed by antibiotic resistance profile of cured strains. The screening results confirm the possible use of marine algae Halimeda opuntia and Sarconema filiforme as a source of pharmacological benefits.

Keywords: Antimicrobial, antiplasmid Cytotoxicity, Marine Algae.

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124 Synthesis of Silver Nanoparticles by Chemical Reduction Method and Their Antibacterial Activity

Authors: Maribel G. Guzmán, Jean Dille, Stephan Godet

Abstract:

Silver nanoparticles were prepared by chemical reduction method. Silver nitrate was taken as the metal precursor and hydrazine hydrate as a reducing agent. The formation of the silver nanoparticles was monitored using UV-Vis absorption spectroscopy. The UV-Vis spectroscopy revealed the formation of silver nanopart├¡cles by exhibing the typical surface plasmon absorption maxima at 418-420 nm from the UV–Vis spectrum. Comparison of theoretical (Mie light scattering theory) and experimental results showed that diameter of silver nanoparticles in colloidal solution is about 60 nm. We have used energy-dispersive spectroscopy (EDX), X-ray diffraction (XRD), transmission electron microscopy (TEM) and, UV–Vis spectroscopy to characterize the nanoparticles obtained. The energy-dispersive spectroscopy (EDX) of the nanoparticles dispersion confirmed the presence of elemental silver signal no peaks of other impurity were detected. The average size and morphology of silver nanoparticles were determined by transmission electron microscopy (TEM). TEM photographs indicate that the nanopowders consist of well dispersed agglomerates of grains with a narrow size distribution (40 and 60 nm), whereas the radius of the individual particles are between 10 and 20 nm. The synthesized nanoparticles have been structurally characterized by X-ray diffraction and transmission high-energy electron diffraction (HEED). The peaks in the XRD pattern are in good agreement with the standard values of the face-centered-cubic form of metallic silver (ICCD-JCPDS card no. 4-0787) and no peaks of other impurity crystalline phases were detected. Additionally, the antibacterial activity of the nanopart├¡culas dispersion was measured by Kirby-Bauer method. The nanoparticles of silver showed high antimicrobial and bactericidal activity against gram positive bacteria such as Escherichia Coli, Pseudimonas aureginosa and staphylococcus aureus which is a highly methicillin resistant strain.

Keywords: Silver nanoparticles, surface plasmon, UV-Vis absorption spectrum, chemicals reduction.

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123 Cardiopulmonary Disease in Bipolar Disorder Patient with History of SJS: Evidence Based Case Report

Authors: Zuhrotun Ulya, Muchammad Syamsulhadi, Debree Septiawan

Abstract:

Patients with bipolar disorder are three times more likely to suffer cardiovascular disorders than the general population, which will influence their level of morbidity and rate of mortality. Bipolar disorder also affects the pulmonary system. The choice of long term-monotherapy and other combinative therapies have clinical impacts on patients. This study investigates the case of a woman who has been suffering from bipolar disorder for 16 years, and who has a history of Steven Johnson Syndrome. At present she is suffering also from cardiovascular and pulmonary disorder. An analysis of the results of this study suggests that there is a relationship between cardiovascular disorder, drug therapies, Steven Johnson Syndrome and mood stabilizer obtained from the PubMed, Cochrane, Medline, and ProQuest (publications between 2005 and 2015). Combination therapy with mood stabilizer is recommended for patients who do not have side effect histories from these drugs. The replacement drugs and combinations may be applied, especially for those with bipolar disorders, and the combination between atypical antipsychotic groups and mood stabilizers is often made. Clinicians, however, should be careful with the patients’ physical and metabolic changes, especially those who have experienced long-term therapy and who showed a history of Steven Johnson Syndrome (for which clinicians probably prescribed one type of medicine).

Keywords: Cardio-pulmonary disease, bipolar disorder, Steven Johnson Syndrome, therapy.

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122 Identification of the Antimicrobial Effect of Liquorice Extracts on Gram-Positive Bacteria: Determination of Minimum Inhibitory Concentration and Mechanism of Action Using a luxABCDE Reporter Strain

Authors: Madiha El Awamie, Catherine Rees

Abstract:

Natural preservatives have been used as alternatives to traditional chemical preservatives; however, a limited number have been commercially developed and many remain to be investigated as sources of safer and effective antimicrobials. In this study, we have been investigating the antimicrobial activity of an extract of Glycyrrhiza glabra (liquorice) that was provided as a waste material from the production of liquorice flavourings for the food industry, and to investigate if this retained the expected antimicrobial activity so it could be used as a natural preservative. Antibacterial activity of liquorice extract was screened for evidence of growth inhibition against eight species of Gram-negative and Gram-positive bacteria, including Listeria monocytogenes, Listeria innocua, Staphylococcus aureus, Enterococcus faecalis and Bacillus subtilis. The Gram-negative bacteria tested include Pseudomonas aeruginosa, Escherichia coli and Salmonella typhimurium but none of these were affected by the extract. In contrast, for all of the Gram-positive bacteria tested, growth was inhibited as monitored using optical density. However parallel studies using viable count indicated that the cells were not killed meaning that the extract was bacteriostatic rather than bacteriocidal. The Minimum Inhibitory Concentration [MIC] and Minimum Bactericidal Concentration [MBC] of the extract was also determined and a concentration of 50 µg ml-1 was found to have a strong bacteriostatic effect on Gram-positive bacteria. Microscopic analysis indicated that there were changes in cell shape suggesting the cell wall was affected. In addition, the use of a reporter strain of Listeria transformed with the bioluminescence genes luxABCDE indicated that cell energy levels were reduced when treated with either 12.5 or 50 µg ml-1 of the extract, with the reduction in light output being proportional to the concentration of the extract used. Together these results suggest that the extract is inhibiting the growth of Gram-positive bacteria only by damaging the cell wall and/or membrane.

Keywords: Antibacterial activity, bioluminescence, Glycyrrhiza glabra, natural preservative.

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121 Using Data Mining Techniques for Finding Cardiac Outlier Patients

Authors: Farhan Ismaeel Dakheel, Raoof Smko, K. Negrat, Abdelsalam Almarimi

Abstract:

In this paper we used data mining techniques to identify outlier patients who are using large amount of drugs over a long period of time. Any healthcare or health insurance system should deal with the quantities of drugs utilized by chronic diseases patients. In Kingdom of Bahrain, about 20% of health budget is spent on medications. For the managers of healthcare systems, there is no enough information about the ways of drug utilization by chronic diseases patients, is there any misuse or is there outliers patients. In this work, which has been done in cooperation with information department in the Bahrain Defence Force hospital; we select the data for Cardiac patients in the period starting from 1/1/2008 to December 31/12/2008 to be the data for the model in this paper. We used three techniques for finding the drug utilization for cardiac patients. First we applied a clustering technique, followed by measuring of clustering validity, and finally we applied a decision tree as classification algorithm. The clustering results is divided into three clusters according to the drug utilization, for 1603 patients, who received 15,806 prescriptions during this period can be partitioned into three groups, where 23 patients (2.59%) who received 1316 prescriptions (8.32%) are classified to be outliers. The classification algorithm shows that the use of average drug utilization and the age, and the gender of the patient can be considered to be the main predictive factors in the induced model.

Keywords: Data Mining, Clustering, Classification, Drug Utilization..

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120 Design and Development of Graphene Oxide Modified by Chitosan Nanosheets Showing pH-Sensitive Surface as a Smart Drug Delivery System for Controlled Release of Doxorubicin

Authors: Parisa Shirzadeh

Abstract:

Drug delivery systems in which drugs are traditionally used, multi-stage and at specified intervals by patients, do not meet the needs of the world's up-to-date drug delivery. In today's world, we are dealing with a huge number of recombinant peptide and protean drugs and analogues of hormones in the body, most of which are made with genetic engineering techniques. Most of these drugs are used to treat critical diseases such as cancer. Due to the limitations of the traditional method, researchers sought to find ways to solve the problems of the traditional method to a large extent. Following these efforts, controlled drug release systems were introduced, which have many advantages. Using controlled release of the drug in the body, the concentration of the drug is kept at a certain level, and in a short time, it is done at a higher rate. Graphene is a natural material that is biodegradable, non-toxic, natural and wide surfaces of graphene plates makes it more effective to modify graphene than carbon nanotubes. Graphene oxide is often synthesized using concentrated oxidizers such as sulfuric acid, nitric acid, and potassium permanganate based on Hummer method. graphene oxide is very hydrophilic and easily dissolves in water and creates a stable solution. Graphene oxide (GO) has been modified by chitosan (CS) covalently, developed for control release of doxorubicin (DOX). In this study, GO is produced by the hummer method under acidic conditions. Then, it is chlorinated by oxalyl chloride to increase its reactivity against amine. After that, in the presence of CS, the amino reaction was performed to form amide transplantation, and the DOX was connected to the carrier surface by π-π interaction in buffer phosphate. GO, GO-CS, and GO-CS-DOX were characterized by FT-IR and TGA to recognize new functional groups which show the new bonding of CS to GO, RAMA and SEM to recognize size of layers that show changing in size and number of layers. The ability to load and release is determined by UV-Visible spectroscopy. The loading result showed a high capacity of DOX absorption (99%) and pH dependence identified as a result of DOX release from GO-CS nanosheet at pH 5.3 and 7.4, which show a fast release rate in acidic conditions.

Keywords: Graphene oxide, chitosan, nanosheet, controlled drug release, doxorubicin.

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119 Quantitative Assessment of Different Formulations of Antimalarials in Sentinel Sites of India

Authors: Taruna Katyal Arora, Geeta Kumari, Hari Shankar, Neelima Mishra

Abstract:

Substandard and counterfeit antimalarials is a major problem in malaria endemic areas. The availability of counterfeit/ substandard medicines is not only decreasing the efficacy in patients, but it is also one of the contributing factors for developing antimalarial drug resistance. Owing to this, a pilot study was conducted to survey quality of drugs collected from different malaria endemic areas of India. Artesunate+Sulphadoxine-Pyrimethamine (AS+SP), Artemether-Lumefantrine (AL), Chloroquine (CQ) tablets were randomly picked from public health facilities in selected states of India. The quality of antimalarial drugs from these areas was assessed by using Global Pharma Health Fund Minilab test kit. This includes physical/visual inspection and disintegration test. Thin-layer chromatography (TLC) was carried out for semi-quantitative assessment of active pharmaceutical ingredients. A total of 45 brands, out of which 21 were for CQ, 14 for AL and 10 for AS+SP were tested from Uttar Pradesh (U.P.), Mizoram, Meghalaya and Gujrat states. One out of 45 samples showed variable disintegration and retension factor. The variable disintegration and retention factor which would have been due to substandard quality or other factors including storage. However, HPLC analysis confirms standard active pharmaceutical ingredient, but may be due to humid temperature and moisture in storage may account for the observed result.

Keywords: Antimalarial medicines, counterfeit, substandard, thin layer chromatography.

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118 Synthesis and Antimicrobial Profile of Newer Schiff Bases and Thiazolidinone Derivatives

Authors: N. K. Fuloria, S. Fuloria, R. Gupta

Abstract:

Esterification of p-bromo-m-cresol led to formation of 2-(4-bromo-3-methylphenoxy)acetate (1). 2-(4-Bromo-3-methyl phenoxy)acetohydrazide (2) is derived from Compound (1) by hydrazination. Compound (2) was reacted with different aromatic aldehydes to yield N-(substituted benzylidiene)-2-(4-bromo-3-methyl phenoxy)acetamide(3a-c). Cyclization of compound (3a-c) with thioglycolic acid yielded 2-(4-bromo-3-methylphenoxy)-N-(4-oxo-2- arylthiazolidin-3-yl) acetamide (4a-c). The newly synthesized compounds were characterized on the basis of spectral studies and evaluated for antibacterial and antifungal activities.

Keywords: Imines, Thiazolidinone, Schiff base, Antimicrobial.

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117 Evaluation of Gingival Hyperplasia Caused by Medications

Authors: Ilma Robo, Saimir Heta, Greta Plaka, Vera Ostreni

Abstract:

Purpose: Drug gingival hyperplasia is an uncommon pathology encountered during routine work in dental units. The purpose of this paper is to present the clinical appearance of gingival hyperplasia caused by medications. There are already three classes of medications that cause hyperplasia and based on data from the literature, the clinical cases encountered and included in this study have been compared. Materials and Methods: The study was conducted in a total of 311 patients, out of which 182 patients were included in our study, meeting the inclusion criteria. After each patient's history was recorded and it was found that patients were in their knowledge of chronic illness, undergoing treatment of gingivitis hypertrophic drugs was performed with a clinical examination of oral cavity and assessment by vertical and horizontal evaluation according to the periodontal indexes. Results: Of the data collected during the study, it was observed that 97% of patients with gingival hyperplasia are treated with nifedipine. 84% of patients treated with selected medicines and gingival hyperplasia in the oral cavity has been exposed at time period for more than 1 year and 1 month. According to the GOI, in the first rank of this index are about 21% of patients, in the second rank are 52%, in the third rank are 24% and in the fourth grade are 3%. According to the horizontal growth index of gingival hyperplasia, grade 1 included about 61% of patients and grade 2 included about 39% of patients with gingival hyperplasia. Bacterial index divides patients by degrees: grading 0 - 8.2%, grading 1 - 32.4%, grading 2 - 14% and grading 3 - 45.1%. Conclusions: The highest percentage of gingival hyperplasia caused by drugs is due to dosing of nifedipine for a duration of dosing and application for systemic healing for more than 1 year.

Keywords: Drug gingival hyperplasia, horizontal growth index, vertical growth index.

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116 Improvement of Reaction Technology of Decalin Halogenation

Authors: Dmitriy Yu. Korulkin, Ravshan M. Nuraliev, Raissa A. Muzychkina

Abstract:

In this research paper were investigated the main regularities of a radical bromination reaction of decalin. There had been studied the temperature effect, durations of reaction, frequency rate of process, a ratio of initial components, type and number of the initiator on decalin bromination degree. There were specified optimum conditions of synthesis of a perbromodecalin by the method of a decalin bromination. There are developed the technological flowchart of receiving a perbromodecalin and the mass balance of process on the first and the subsequent loadings of components. The results of research of antibacterial and antifungal activity of synthesized bromoderivatives have been represented.

Keywords: Decalin, optimum technology, perbromodecalin, radical bromination.

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115 New Ways for Designing External Fixators Applied in Treatment of Open and Unstable Fractures

Authors: Karel Frydrýšek, Pavel Koštial, Karla Barabaszová, Jana Kukutschová

Abstract:

This paper deals with a new way for designing external fixators applied in traumatology and orthopaedics. These fixators can be applied in the treatment of open and unstable fractures or for lengthening human or animal bones etc. The new design is based on the development of Ilizarov and other techniques (i.e. shape and weight optimalization based on composite materials, application of smart materials, nanotechnology, low x-ray absorption, antibacterial protection, patient's comfort, reduction in the duration of the surgical treatment, and cost).

Keywords: biomechanics, design, external fixators, newmaterials, traumatology

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114 Development and Validation of a UPLC Method for the Determination of Albendazole Residues on Pharmaceutical Manufacturing Equipment Surfaces

Authors: R. S. Chandan, M. Vasudevan, Deecaraman, B. M. Gurupadayya

Abstract:

In Pharmaceutical industries, it is very important to remove drug residues from the equipment and areas used. The cleaning procedure must be validated, so special attention must be devoted to the methods used for analysis of trace amounts of drugs. A rapid, sensitive and specific reverse phase ultra performance liquid chromatographic (UPLC) method was developed for the quantitative determination of Albendazole in cleaning validation swab samples. The method was validated using an ACQUITY HSS C18, 50 x 2.1mm, 1.8μ column with a isocratic mobile phase containing a mixture of 1.36g of Potassium dihydrogenphosphate in 1000mL MilliQ water, 2mL of triethylamine and pH adjusted to 2.3 ± 0.05 with ortho-phosphoric acid, Acetonitrile and Methanol (50:40:10 v/v). The flow rate of the mobile phase was 0.5 mL min-1 with a column temperature of 350C and detection wavelength at 254nm using PDA detector. The injection volume was 2µl. Cotton swabs, moisten with acetonitrile were used to remove any residue of drug from stainless steel, teflon, rubber and silicon plates which mimic the production equipment surface and the mean extraction-recovery was found to be 91.8. The selected chromatographic condition was found to effectively elute Albendazole with retention time of 0.67min. The proposed method was found to be linear over the range of 0.2 to 150µg/mL and correlation coefficient obtained is 0.9992. The proposed method was found to be accurate, precise, reproducible and specific and it can also be used for routine quality control analysis of these drugs in biological samples either alone or in combined pharmaceutical dosage forms.

Keywords: Cleaning validation, Albendazole, residues, swab analysis, UPLC.

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113 Learners’ Violent Behaviour and Drug Abuse as Major Causes of Tobephobia in Schools

Authors: Prakash Singh

Abstract:

Many schools throughout the world are facing constant pressure to cope with the violence and drug abuse of learners who show little or no respect for acceptable and desirable social norms. These delinquent learners tend to harbour feelings of being beyond reproach because they strongly believe that it is well within their rights to engage in violent and destructive behaviour. Knives, guns, and other weapons appear to be more readily used by them on the school premises than before. It is known that learners smoke, drink alcohol, and use drugs during school hours, hence, their ability to concentrate, work, and learn, is affected. They become violent and display disruptive behaviour in their classrooms as well as on the school premises, and this atrocious behaviour makes it possible for drug dealers and gangsters to gain access onto the school premises. The primary purpose of this exploratory quantitative study was therefore to establish how tobephobia (TBP), caused by school violence and drug abuse, affects teaching and learning in schools. The findings of this study affirmed that poor discipline resulted in producing poor quality education. Most of the teachers in this study agreed that educating learners who consumed alcohol and other drugs on the school premises resulted in them suffering from TBP. These learners are frequently abusive and disrespectful, and resort to violence to seek attention. As a result, teachers feel extremely demotivated and suffer from high levels of anxiety and stress. The word TBP will surely be regarded as a blessing by many teachers throughout the world because finally, there is a word that will make people sit up and listen to their problems that cause real fear and anxiety in schools.

Keywords: Aims and objectives of quality education, Debilitating effects of tobephobia, Fear of failure associated with education, learners’ violent behaviour and drug abuse.

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112 Ni-B Coating Production on Magnesium Alloy by Electroless Deposition

Authors: Ferhat Bülbül

Abstract:

The use of magnesium alloys is limited due to their susceptibility to corrosion although they have many attractive physical and mechanical properties. To increase mechanical and corrosion properties of these alloys, many deposition method and coating types are used. Electroless Ni–B coatings have received considerable interest recently due to its unique properties such as cost-effectiveness, thickness uniformity, good wear resistance, lubricity, good ductility and corrosion resistance, excellent solderability and electrical properties and antibacterial property. In this study, electroless Ni-B coating could been deposited on AZ91 magnesium alloy. The obtained coating exhibited a harder and rougher structure than the substrate.

Keywords: Amorphous, electroless Ni–B, magnesium, X-ray diffraction.

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111 Wound Healing Dressing and Some Composites Such as Zeolite, TiO2, Chitosan and PLGA: A Review

Authors: L. B. Naves, L. Almeida

Abstract:

The development of Drugs Delivery System (DDS) has been widely investigated in the last decades. In this paper, first a general overview of traditional and modern wound dressing is presented. This is followed by a review of what scientists have done in the medical environment, focusing on the possibility to develop a new alternative for DDS through transdermal pathway, aiming to treat melanoma skin cancer.

Keywords: Cancer Therapy, Dressing Polymers, Melanoma, wound healing.

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110 Determination of in Vitro Susceptibility of the Typhoid Pathogens to Synergistic Action of Euphorbia Hirta, Euphorbia Heterophylla and Phyllanthus Niruri for Possible Development of Effective Anti-Typhoid Drugs

Authors: Abalaka, M. E., Daniyan, S. Y., Adeyemo, S. O.

Abstract:

Studies were carried out to determine the in vitro susceptibility of the typhoid pathogens to combined action of Euphorbia hirta, Euphorbia heterophylla and Phyllanthus niruri. Clinical isolates of the typhoid bacilli were subjected to susceptibility testing using agar diffusion technique and the minimum inhibitory concentration (MIC) determined with tube dilution technique. These isolates, when challenged with doses of the extracts from the three medicinal plants showed zones of inhibition as wide as 26±0.2mm, 22±0.1mm and 18±0.0mm respectively. The minimum inhibitory concentration (MIC) revealed organisms inhibited at varying concentrations of extracts: E. hirta (S. typhi 0.250mg/ml, S. paratyphi A 0.125mg/ml, S. paratyphi B 0.185mg/ml and S. paratyphi C 0.225mg/ml), E. heterophylla (S. typhi 0.280mg/ml, S. paratyphi A 0.150mg/ml, S. paratyphi B 0.200mg/ml and S. paratyphi C 0.250mg/ml) and P. niruri (S. typhi 0.150mg/ml, S. paratyphi A 0.100mg/ml, S. paratyphi B 0.115mg/ml and S. paratyphi C 0.125mg/ml). The results of the synergy between the three plants in the ration of 1:1:1 showed very low MICs for the test pathogens as follows S. typhi 0.025mg/ml, S. paratyphi A 0.080mg/ml, S. paratyphi B 0.015mg/ml and S. paratyphi C 0.10mg/ml with the diameter zone of inhibition (DZI) ranging from 35±0.2mm, 28±0.4mm, 20±0.1mm and 32±0.3mm respectively. The secondary metabolites were identified using simple methods and HPLC. Organic components such as anthroquinones, different alkaloids, tannins, 6-ethoxy-1,2,3,4-tetrahydro-2,2,4-trimethyl and steroids were identified. The prevalence of Salmonellae, a deadly infectious disease, is still very high in parts of Nigeria. The synergistic action of these three plants is very high. It is concluded that pharmaceutical companies should take advantage of these findings to develop new anti-typhoid drugs from these plants.

Keywords: A Prevalence, Susceptibility, Synergistic, Typhoid pathogens.

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