Search results for: poorly water soluble drugs

Authors: Geno Paul S. Cumla, Jan Mariel M. Gentiles, M. Brenda Gajelan-Samson

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Eutrophication is a process where in there is a surplus of nutrients present in a lake or river. Harmful cyanobacteria, hypoxia, and primarily algae, which contain toxins, grow because of the excess nutrients. Algal blooms can cause fish kills, limiting the light penetration which reduces growth of aquatic organisms, causing die-offs of plants and produce conditions that are dangerous to aquatic and human life. The main cause for eutrophication is the presence of excessive amounts of phosphorus (P) and nitrogen (N). Nitrogen is necessary for the production of the plant tissues and is usually used to synthesize proteins. Nitrate is a compound that contains nitrogen, and at elevated levels it can cause harmful effects. Excessive amounts of phosphorus, displaced through human activity, is the major cause of algae growth and as well as degraded water quality. To accomplish this study the Assessment of Soluble inorganic nitrogen (SIN), Assessment of Soluble reactive phosphate (SRP), Determination of Chlorophyll a (Chl-a) concentration, and Determination of Dominating Taxa were done. The study addresses the high probability of algal blooms in Maqueda Bay by assessing the biotic and abiotic factors of Antiao and Jiabong rivers. The data predicts the overgrowth of algae and to create awareness to prevent the event from taking place. The study assesses the adverse effects that could be prevented by understanding and controlling algae. This should predict future cases of algal blooms and allow government agencies which require data to create programs to prevent and assess these issues.

Keywords: eutrophication, chlorophyll a, nitrogen, phosphorus, red tide, Kjeldahl method, spectrophotometer, assessment of soluble inorganic nitrogen, SIN, assessment of soluble reactive phosphate, SRP

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Authors: K. Srujana, Vinay U. Rao, M. Sudhakar

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Isoniazide (INH) a freely water soluble and pyrazinamide (Z) a practically water insoluble first line anti tubercular (TB) drugs were identified as candidates for optimizing the Moisture Activated Dry Granulation (MADG) process. The work focuses on identifying the effect of binder type and concentration as well as the effect of magnesium stearate level on critical quality attributes of Disintegration time (DT) and in vitro dissolution test when the tablets are processed by the MADG process. Also, the level of the drug concentration, binder concentration and fluid addition during the agglomeration stage of the MADG process was evaluated and optimized. For INH, it was identified that for tablets with HPMC as binder at both 2% w/w and 5% w/w level and Magnesium stearate upto 1%w/w as lubrication the DT is within 1 minute and the dissolution rate is the fastest (> 80% in 15 minutes) as compared to when PVP or pregelatinized starch is used as binder. Regarding the process, fast disintegrating and rapidly dissolving tablets are obtained when the level of drug, binder and fluid uptake in agglomeration stage is 25% w/w 0% w/w binder and 0.033%. w/w. At the other 2 levels of these three ingredients, the DT is significantly impacted and dissolution is also slower. For pyrazinamide,it was identified that for the tablets with 2% w/w level of each of PVP as binder and Cross Caramellose Sodium disintegrant the DT is within 2 minutes and the dissolution rate is the fastest(>80 in 15 minutes)as compared to when HPMC or pregelatinized starch is used as binder. This may be attributed to the fact that PVP may be acting as a solubilizer for the practically insoluble Pyrazinamide. Regarding the process,fast dispersing and rapidly disintegrating tablets are obtained when the level of drug, binder and fluid uptake in agglomeration stage is 10% w/w,25% w/w binder and 1% w/w.At the other 2 levels of these three ingredients, the DT is significantly impacted and dissolution is comparatively slower and less complete.

Keywords: agglomeration stage, isoniazide, MADG, moisture distribution stage, pyrazinamide

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Authors: J. O. Idoko, C. N. Michael, T. O. Fasuan

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This study investigated the effects of cooking time, seed-to-water ratio and soaking time on proximate and functional properties of African walnut seed using Box-Behnken design and Response Surface Methodology (BBD-RSM) with a view to increase its utilization in the food industry. African walnut seeds were sorted washed, soaked, cooked, dehulled, sliced, dried and milled. Proximate analysis and functional properties of the samples were evaluated using standard procedures. Data obtained were analyzed using descriptive and inferential statistics. Quadratic models were obtained to predict the proximate and functional qualities as a function of cooking time, seed-to-water ratio and soaking time. The results showed that the crude protein ranged between 11.80% and 23.50%, moisture content ranged between 1.00% and 4.66%, ash content ranged between 3.35% and 5.25%, crude fibre ranged from 0.10% to 7.25% and carbohydrate ranged from 1.22% to 29.35%. The functional properties showed that soluble protein ranged from 16.26% to 42.96%, viscosity ranged from 23.43 mPas to 57 mPas, emulsifying capacity ranged from 17.14% to 39.43% and water absorption capacity ranged from 232% to 297%. An increase in the volume of water used during cooking resulted in loss of water soluble protein through leaching, the length of soaking time and the moisture content of the dried product are inversely related, ash content is inversely related to the cooking time and amount of water used, extraction of fat is enhanced by increase in soaking time while increase in cooking and soaking times result into decrease in fibre content. The results obtained indicated that African walnut could be used in several food formulations as protein supplement and binder.

Keywords: African walnut, functional properties, proximate analysis, response surface methodology

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Authors: Do Su Park, Sang Jun Park, Cheon Soon Jeong

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This study was performed in order to investigate the optimum ripening conditions for the marketing of Squash. Research sample 'Bochang' was grown at Hongcheonin in Gangwon province in August 2014. Ripening the samples were stored under the conditions of 25℃, 30℃, and 35℃ with the humidity RH70 ± 5%. They were checked every 3 days for 21 days. The respiration rate, water loss, hardness, coloration, the contents of soluble solids, starch, total sugar were evaluated after storage. Respiration rate was reduced in all treatments with longer storage period. Water loss was increased in the higher temperature. The 13% water loss was found at 35℃ on 21st storage day. The store initially 25℃ and 30℃ Hardness 47N and the ripening 21 days decreased slightly. On the other hand, in the case of 35℃ showed a large reduction than 25℃ and 30℃. Soluble solid contents were increased with longer ripening period. 30℃ and 35℃ was highest ripening 15 days. In the case of 25℃, it was highest on 21th day. The higher the temperature, the higher the soluble solids content are. 25℃ and 30℃ Coloration was increased rapidly until the ripening 12 days. In case of 35℃, continued increase up to 21 days. 25℃ and 30℃ showed no differences. Meanwhile, in case of 35℃, appearance quality was reduced in Occurrence of yellowing phenomenon of pericarp occurs from after ripening for 9 days. The coloration of fruit flesh is increase until after ripening for 9 days and decrease from after ripening for 9 days. There was no significant difference depending on the conditions of temperature. The higher the temperature, the lower the content of the starch. In case of 30℃ and 35℃, was reduced with longer storage period. 25℃ was minimal content change. Total sugar was increased in all treatments with longer storage period. The higher the temperature, the higher the amount of total sugar content is. Therefore, at 25℃ for 18-21 days and at 30℃ for 12-15 days is suitable for ripening.

Keywords: marketing, ripening, temperature, winter squash

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Authors: Oranso T. Mahlangi, Bhekie B. Mamba

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The occurrence of trace organic compounds (TOrCs) in water has raised health concerns for living organisms. The majority of TorCs, including pharmaceuticals and volatile organic compounds, are poorly monitored, partly due to the high cost of analysis and less strict water quality guidelines in South Africa. Therefore, the removal of TorCs is important to guarantee safe potable water. In this study, ZnO nanoparticles were fabricated in situ in polyethersulfone (PES) polymer solutions. This was followed by membrane synthesis using the phase inversion technique. Techniques such as FTIR, Raman, SEM, AFM, EDS, and contact angle measurements were used to characterize the membranes for several physicochemical properties. The membranes were then evaluated for their efficiency in treating pharmaceutical wastewater and resistance to organic (sodium alginate) and protein (bovine serum albumin) fouling. EDS micrographs revealed uniform distribution of ZnO nanoparticles within the polymer matrix, while SEM images showed uniform fingerlike structures. The addition of ZnO increased membrane roughness as well as hydrophilicity (which in turn improved water fluxes). The membranes poorly rejected monovalent and divalent salts (< 10%), making them resistant to flux decline due to concentration polarization effects. However, the membranes effectively removed carbamazepine, caffeine, sulfamethoxazole, ibuprofen, and naproxen by over 50%. ZnO PES membranes were resistant to organic and protein fouling compared to the neat membrane. ZnO PES ultrafiltration membranes may provide a solution in the reclamation of wastewater.

Keywords: trace organic compounds, pharmaceuticals, membrane fouling, wastewater reclamation

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Authors: Li Liang

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Chinese titanium iron ore reserves with high calcium and magnesium accounted for more than 90% of the total reserves, and acid-soluble titanium slag which is produced by titanium iron ore always used to produce titanium dioxide through sulphate process. To broad the application range of acid-soluble titanium slag, the feasibility and thermodynamics of chlorinated reaction for preparation TiCl4 by titanium slag chlorination in molten slat were conducted in this paper. The analysis results show that TiCl4 can be obtained by chlorinate the acid-dissolved titanium slag with carbon. Component’s thermodynamics reaction trend is: CaO>MnO>FeO(FeCl2)>MgO>V2O5>Fe2O3>FeO(FeCl3)>TiO2>Al2O3>SiO2 in the standard state. Industrial experimental results are consistent with the thermodynamics analysis, the content of TiCl4 is more than 98% in the production. Fe, Si, V, Al, and other impurity content can satisfy the requirements of production.

Keywords: thermodynamics, acid-soluble titanium slag, preparation of TiCl4, chlorination

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

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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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Authors: Chaoran Liu

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Bioactive polysaccharides and polysaccharide-protein complex derived from mushrooms and fungi have a wide range of immunomodulatory activity with low side-effects and have therefore the potential to be developed as an adjuvant in cancer therapies. Mushrooms sclerotium is rich in polysaccharides and the polysaccharides isolated from the sclerotium of Polyporus rhinocerus have shown potent in vivo and in vitro immunomodulatory effects. Macrophages are considered to be an important component of the innate immune response against bacterial infection and cancer. To better understanding the immunomodulatory effects and its underlying mechanisms of sclerotial water-soluble polysaccharides extracted from P. rhinocerus on macrophages, the objectives of this study are to purify the water-soluble novel sclerotial polysaccharides and to characterize the structure and properties as well as to study the detailed molecular mechanisms of the in vitro immunomodulating effects in murine macrophages. The hot water-soluble fraction PRW from the sclerotium of P. rhinocerus was obtained using solvent extraction. PRW was further fractionated by membrane ultrafiltration to a give a fraction (PRW1) with molecular mass less than 50 kDa. PRW1 was characterized to be a polysaccharide-protein complex composed of 45.7% polysaccharide and 44.2% protein. The chemical structure of the carbohydrate moiety of PRW1 was elucidated by GC and FTIR to be mainly beta-D-glucan with trace amount of galactose and mannose. The immunomodulatory effects of PRW1 on murine RAW 264.7 macrophages were demonstrated in terms of the increase in nitric oxide production and cytokine production. Mechanistically, PRW1 initiates ERK phosphorylation to activate macrophages within 15 min and significantly improves the expression level of inducible NOS (iNOS) from 6 h after treatment. In summary, this study indicates that PRW1 is a potent immunomodulatory agent for macrophages and suggests that mushroom sclerotia from Polyporus rhinocerus requires for further investigation in cancer research.

Keywords: Polyporus rhinocerus, mushroom sclerotia, Polysaccharide-Protein Complex, macrophage activation

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Authors: Ben Salah Nahla

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The problem of water in Tunisia affects the quality and quantity. Tunisia is in a situation of water shortage. It was estimated that 4.6 Mm3/an. Moreover, the quality of water in Tunisia is also mediocre. In fact, 50% of the water has a high salinity (> 1.5g/l). There are several parameters which affect water quality such as sodium, fluoride. An excess of this parameter may induce some human health. Furthermore, the mining basin area has a problem of industrial waste. This problem may affect the water quality of the groundwater. Therefore, the purpose of this work is to assess the water quality in Basin Mining and the impact of fluorine. For this research, some water samples were done in the field and specific water analysis was implemented in the laboratory. Sampling is carried out on eight drilling in the area of the mining region. In the following, we will look at water view composition, physical and chemical quality. A physical-chemical analysis of water from a survey of the Mining area of Tunisia was performed and showed an excess for the following items: fluorine, sodium, sulfate. So many chemicals may be present in water. However, only a small number of them immediately concern in terms of health in all circumstances. Fluorine (F) is one particular chemical that is considered both necessary for the human body, but an excess of the rate of this chemical causes serious diseases. Sodium fluoride and sodium silicofluoride are more soluble and may spread in animals and plants where their toxicity largest organizations. The more complex particles such as cryolite and fluorite, almost insoluble, are more stable and less toxic. Thereafter, we will study the problem of excess fluorine in the water. The latter intended for human consumption must always comply with the limits for microbiological quality parameters and physical-chemical parameters defined by European standards (1.5 mg/l) and Tunisian (2 mg/l).

Keywords: water, minier basin, fluorine, silicofluoride

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Authors: E. Prema

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Biotechnology is a study relating to the practical application of living beings in different fields. Generally, it is a study with regard to living organisms in the industrial utilization. It is the technology, which uses living organisms or its parts for specific commercial use. Modification and application of living beings for different practical purposes is possible through biotechnology. Furthermore, today biotechnology is being used in different fields for better results. It is worthwhile to note here that biotechnology is one of the most innovative and intensive industries. It has used the genetically based characteristics in microorganisms, plants and animals to create drugs and to develop drug therapies, which may prevent, cure or alleviate disease and their symptoms. Drugs are basically chemicals and while patenting drugs, the conditions of patentability of chemicals and the types that can be patented are equally applicable to drugs also. Nowadays, the role of biotechnology for manufacturing drugs has assumed much importance because of intellectual property rights. By way using biotechnology, most of the pharmaceutical inventions are getting protection for the period of 20 years as per the Patents Act, 1970 as amended in 2005. There is no doubt that biotechnology is serving the public at large with regard manufacturing drugs and helping the needy people on time.

Keywords: biotechnology, drugs, intellectual property rights, patents

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Authors: A. Hilsana, Vinay U. Rao, M. Sudhakar

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Even though a number of non-steroidal anti-inflammatory drugs (NSAIDS) are available with different chemistries, they share a common solubility characteristic that is they are relatively more soluble in alkaline environment and practically insoluble in acidic environment. This work deals with developing a wax matrix drug delivery platform for controlled delivery of three model NSAIDS, Diclofenac sodium (DNa), Mefenamic acid (MA) and Naproxen (NPX) using the melt granulation technique. The aim of developing the platform was to have a general understanding on how an erodible matrix system modulates drug delivery rate and extent and how it can be optimized to give a delivery system which shall release the drug as per a common target product profile (TPP). Commonly used waxes like Cetostearyl alcohol and stearic acid were used singly an in combination to achieve a TPP of not 15 to 35% in 1 hour and not less than 80% Q in 24 hours. Full factorial design of experiments was followed for optimization of the formulation.

Keywords: NSAIDs, controlled delivery, target product profile, melt granulation

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Authors: Mewa Singh

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Nanomedicine, a fusion of nanotechnology and medicine, is an emerging technology ideally suited to the targeted therapies. Nanoparticles overcome the low selectivity of anti-cancer drugs toward the tumor as compared to normal tissue and hence result-in less severe side-effects. Our new technology, HYBRID-NANOENGINEERING™, uses a new molecule (MR007) in the creation of nanoparticles that not only helps in nanonizing the medicine but also provides synergy to the medicine. The simplified manufacturing process will result in reduced manufacturing costs. Treatment is made more convenient because hybrid nanomedicines can be produced in oral, injectable or transdermal formulations. The manufacturing process uses no protein, oil or detergents. The particle size is below 180 nm with a narrow distribution of size. Importantly, these properties confer great stability of the structure. The formulation does not aggregate in plasma and is stable over a wide range of pH. The final hybrid formulation is stable for at least 18 months as a powder. More than 97 drugs, including paclitaxel, docetaxel, tamoxifen, doxorubicinm prednisone, and artemisinin have been nanonized in water soluble formulations. Preclinical studies on cell cultures of tumors show promising results. Our HYBRID-NANOENGINEERING™ platform enables the design and development of hybrid nano-pharmaceuticals that combine efficacy with tolerability, giving patients hope for both extended overall survival and improved quality of life. This study would discuss or present this new discovery of HYBRID-NANOENGINEERING™ which targets drug delivery, synergistic, and potentiating effects, and barriers of drug delivery and advanced drug delivery systems.

Keywords: nano-medicine, nano-particles, drug delivery system, pharmaceuticals

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Authors: Muslim Khan, Kenneth B. Jensen, Kevin A. Francesconi

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Trace amounts (ca 1 µg/L, 13 nM) of arsenic are present in sea water mostly as the oxyanion arsenate. In contrast, arsenic is present in marine biota (animals and algae) at very high levels (up to100,000 µg/kg) a significant portion of which is present as lipid-soluble compounds collectively termed arsenolipids. The complex nature of sea water presents an analytical challenge to detect trace compounds and monitor their environmental path. We developed a simple method using liquid-liquid extraction combined with HPLC-High Resolution Mass Spectrometer capable of detecting trace of arsenolipids (99 % of the sample matrix while recovering > 80 % of the six target arsenolipids with limit of detection of 0.003 µg/L.)

Keywords: arsenolipids, sea water, HPLC-high resolution mass spectrometry

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Authors: Blessing A. Aderibigbe

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Combination therapy is a treatment approach that is used to prevent the emergence of drug resistance. This approach is used for the treatment of many chronic and infectious diseases. Potentiating agents are currently explored in combination therapy, resulting in excellent therapeutic outcomes. Breast cancer and malaria are two chronic conditions responsible globally for high death rates. In this research, a class of polymer-drug conjugates containing potentiating agents with either antimalarial or anticancer drugs were prepared by Michael Addition Polymerization reaction and ring-opening polymerization reaction. Conjugation of potentiating agents with bioactive compounds into the polymers resulted in conjugates with good water solubility, highly selective and non-toxic. In vitro cytotoxicity and in vitro antiplasmodial evaluation on the conjugates revealed that the conjugates were more effective when compared to the free drugs. The drug release studies further showed that the release profile of the drugs from the conjugates was sustained. The findings revealed the potential of polymer-drug conjugates to overcome drug toxicity and drug resistance, which is common with the currently used antimalarial and anticancer drugs.

Keywords: anticancer, antimalarials, combination therapy, polymer-drug conjugates

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Authors: Obinna Emmanuel Nkomadu

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The sea attracts many criminal activities including drug trafficking. The illicit traffic in narcotic drugs and psychotropic substances by sea poses a serious threat to maritime security globally. The seizure of drugs, particularly, on the African continent is on the raise. In terms of Southern Africa, South Africa is a major transit point for Latin American drugs and South Africa is the largest market for illicit drugs entering the Southern African region. Nigeria and South Africa have taken a number of steps to address this scourge, but, despite those steps, drugs trafficking at sea continues. For that reason and to combat a number of other threats to maritime security around the continent, a substantial number of AU members in 2016 adopted the African Charter on Maritime Security and Safety and Development in Africa (“the Charter”). However, the Charter is yet to come into force due to the number of States required to accede or ratify the Charter. This paper set out the pre-existing international instruments on drugs, to ascertain the domestic laws of Nigeria and South Africa relating to drugs with the relevant provisions of the Lomé Charter in order to establish whether any legal steps are required to ensure that Nigeria and South Africa comply with its obligations under the Charter. Indeed, should Nigeria and South Africa decide to ratify it and should it come into force, both States must cooperate with other relevant States in establishing policies, as well as a regional and continental institutions, and ensure the implementation of such policies. The paper urged the States to urgently ratify the Charter as it is a step in the right direction in the prevention and repression of drugs trafficking on the African maritime domain.

Keywords: cooperation against drugs trafficking at sea, Lomé Charter, maritime security, Nigerian and South Africa legislation on drugs

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Authors: Behcet Al, Şener Cindoruk, Suat Zengin, Mehmet Murat Oktay, Mehmet Mustafa Sunar, Hatice Eroglu, Cuma Yildirim

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Objective: In present study we aimed to investigate the chronic drug use due to chronic diseases in patients admitted to emergency department. Materials-Methods: 144 patients who applied to emergency department (ED) of medicine school of Gaziantep University between June 2013 and September 2013 with chronic diseases and use chronic drugs were included. Information about drugs used by patients were recorded. Results: Of patients, half were male, half were female, and the mean age was 58 years. The first three common diseases were diabetes mellitus, hypertension and coronary artery diseases. Of patients, %79.2 knew their illness. Fifty patients began to use drug within three months, 36 patient began to use within the last one year. While 42 patients brought all of their drugs with themselves, 17 patients brought along a portion of drugs. While three patients stopped their medication completely, 125 patients received medication on a regular basis. Fifty-two patient described the drugs with names, 13 patients described with their colors, 3 patients described by grammes, 45 patients described with the size of the tablet and 13 patients could not describe the drugs. Ninety-two patients explained which kind of drugs were used for each diseases, 17 patient explained partly, and 35 patients had no idea. Hundred patients received medication by themselves, 44 patients medications were giving by their relatives and med carers. Of medications, 140 were written by doctors directly, three medication were given by pharmacist; and one patient bought the drug by himself. For 11 patients the drugs were not harmonious to their diseases. Fifty-one patients admitted to the ED two times within last week, and 73 admitted two times within last month. Conclusion: The majority of patients with chronic diseases and use chronic drugs know their diseases and use the drugs in order, but do not have enough information about their medication.

Keywords: chronic disease, drug use, emergency department, medication

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Authors: Ahmed. Abdel Bary, Omneya. Khowessah, Mojahed. al-jamrah

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Introduction: The major challenge with the design of oral dosage forms lies with their poor bioavailability. The most frequent causes of low oral bioavailability are attributed to poor solubility and low permeability. The aim of this study was to develop solid nanodispersed tablet formulation of Glimepiride for the enhancement of the solubility and bioavailability. Methodology: Solid nanodispersions of Glimepiride (GMP) were prepared using two different ratios of 2 different carriers, namely; PEG6000, pluronic F127, and by adopting two different techniques, namely; solvent evaporation technique and fusion technique. A full factorial design of 2 3 was adopted to investigate the influence of formulation variables on the prepared nanodispersion properties. The best chosen formula of nanodispersed powder was formulated into tablets by direct compression. The Differential Scanning Calorimetry (DSC) analysis and Fourier Transform Infra-Red (FTIR) analysis were conducted for the thermal behavior and surface structure characterization, respectively. The zeta potential and particle size analysis of the prepared glimepiride nanodispersions was determined. The prepared solid nanodispersions and solid nanodispersed tablets of GMP were evaluated in terms of pre-compression and post-compression parameters, respectively. Results: The DSC and FTIR studies revealed that there was no interaction between GMP and all the excipients used. Based on the resulted values of different pre-compression parameters, the prepared solid nanodispersions powder blends showed poor to excellent flow properties. The resulted values of the other evaluated pre-compression parameters of the prepared solid nanodispersion were within the limits of pharmacopoeia. The drug content of the prepared nanodispersions ranged from 89.6 ± 0.3 % to 99.9± 0.5% with particle size ranged from 111.5 nm to 492.3 nm and the resulted zeta potential (ζ ) values of the prepared GMP-solid nanodispersion formulae (F1-F8) ranged from -8.28±3.62 mV to -78±11.4 mV. The in-vitro dissolution studies of the prepared solid nanodispersed tablets of GMP concluded that GMP- pluronic F127 combinations (F8), exhibited the best extent of drug release, compared to other formulations, and to the marketed product. One way ANOVA for the percent of drug released from the prepared GMP-nanodispersion formulae (F1- F8) after 20 and 60 minutes showed significant differences between the percent of drug released from different GMP-nanodispersed tablet formulae (F1- F8), (P<0.05). Conclusion: Preparation of glimepiride as nanodispersed particles proven to be a promising tool for enhancing the poor solubility of glimepiride.

Keywords: glimepiride, solid Nanodispersion, nanodispersed tablets, poorly water soluble drugs

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Authors: Jun Sun, Tsz Tin Yu, Maryam Mirabediny, Matthew Lee, Adele Jones, Denis M. O’Carroll, Michael J. Manefield, Björn Åkermark, Biswanath Das, Naresh Kumar

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Reductive defluorination has emerged as a sustainable approach to clean water from Per and polyfluoroalkyl substances (PFASs), also known as forever organic containments. For last few decades, nano zero valent metals (nZVMs) have been intensively applied in the reductive remediation of groundwater contaminated with chlorinated organic compounds due to its low redox potential, easy application, and low production cost. However, there is inadequate information on the effective reductive defluorination of linear or branched PFAS using nZVMs as reductants because of the lack of suitable catalysts. CoII-5,10,15,20-Tetraphenyl-21H,23H-porphyrin (CoTPP) has been recently reported for effective catalyzing reductive defluorination of branched (br-) perfluorooctane sulfonate (PFOS) by using TiIII citrate as reductant. However, the low water solubility of CoTPP limited its applicability. Here, we explored a series of structurally related soluble cobalt porphyrin catalysts based on our previously reported best performing CoTPP. All soluble porphyrins [[meso-tetra(4-carboxyphenyl)porphyrinato]cobalt(III)]Cl·₇H₂O (CoTCPP), [[meso-tetra(4-sulfonatophenyl) porphyrinato]cobalt(III)]·9H2O (CoTPPS), and [[meso-tetra(4-N-methylpyridyl) porphyrinato]cobalt(II)](I)₄·₄H₂O (CoTMpyP) displayed better defluorination efficiencies than CoTPP. Especially, CoTMpyP presented the best defluorination efficiency for br-PFOS (94 %), branched perfluorooctanoic acid (PFOA) (89 %), and 3,7-Perfluorodecanoic acid (PFDA) (60 %) after 1 day at 70 0C. CoTMpyP-nZn0 system showed 88-164 times higher defluorination rate than VB12-nZn0 system in terms of all investigated br-PFASs. The CoTMpyP-nZn0 also performed effectively at room temperature, demonstrating the potential prospect for in-situ reductive systems. Based on the analysis of the intermediate products, the calculated bond dissociation energies (BDEs) and possible first interaction between CoTMpyP and PFAS, degradation pathways of 3,7-PFDA and 6-PFOS are proposed.

Keywords: cationic, soluble porphyrin, cobalt, vitamin b12, pfas, reductive defluorination

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Authors: Durata Haciu, Ozgur Birer

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Zinc acetate solution is sonicated at high power in water and in ethanol in the absence and presence of various peroxides. In the absence of peroxides, the products are zinc oxide and layered hydroxy zinc acetate in water and in ethanol, respectively. Layered basic zinc acetate are prepared for the first time using sonochemical methods. The addition of peroxides alters the reaction mechanisms. In water, insoluble peroxides produce zinc oxides while the water soluble peroxide, i.e.hydrogen peroxide, completely destroyed the structure and casted a doubt on the accepted peroxide initiated mechanism of reactions. In ethanol,peroxide addition caused the reaction mechanism to change and some oxide formation is observed. The reaction mechanism is sensitive to water/ethanol amounts as well as the peroxide to zinc ion mole ratio.Thin zinc oxide wafers (ca. 30 nm) with band gaps of 3.24 eV were obtained.

Keywords: ultrasound, zinc oxide, hydroxy zinc acetate, fenton, peroxide initiation

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Authors: Mohamed Bagues, Ikbel Souli, Feiza Boussora, Kamel Nagaz

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In southern Tunisia, two local barley accessions CV. Ardhaoui; 'Bengardeni' and 'Karkeni' were cultivated in the field under deficit drip irrigation with saline water. Three treatments were used: control or full irrigation T0 (100%ETc) and stressed T1 (75%ETc), T2 (50%ETc). Proline and soluble sugars contents increase significantly under drought between accessions compared to control and varies between growth stages. Moreover, the increasing of Ca2+ concentration enhances the absorption of Na+ ion, consequently K+/Na+ decrease significantly between accessions, these results suggest that a high tolerance of Bengardeni accession to drought stress. Therefore, drought tolerance indices (STI, SSI, MP, GMP, YSI and TOL) were used to identify high yielding and drought tolerant between accessions. MP explained the variation of GYi. GMP and STI explained the variation of GYs. The high values of MP, STI and GMP were associated with higher yielding accession. Higher TOL value is associated with significant grain yield reduction in stressed environment suggesting higher stress responses of accessions. Significant positive correlations between MP, STI and GMP and negative between YSI and SSI. MP, STI, GMP and YSI, TOL, SSI are not correlated with each other.

Keywords: drought, proline, soluble sugars, minerals, yield, drought tolerance indices, barley

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Authors: N. Rajendra Prasad

Abstract:

Resveratrol (RSV), a grape phytochemical, has drawn greater attention because of its beneficial ef-fects against cancer. However, RSV has some draw-backs such as unstabilization, poor water solubility and short biological half time, which limit the utili-zation of RSV in medicine, food and pharmaceutical industries. In this study, we have encapsulated RSV in gelatin nanoparticles (GNPs) and studied its anti-cancer efficacy in NCI-H460 lung cancer cells. SEM and DLS studies have revealed that the prepared RSV-GNPs possess spherical shape with a mean diameter of 294 nm. The successful encapsulation of RSV in GNPs has been achieved by the cross-linker glutaraldehyde probably through Schiff base reaction and hydrogen bond interaction. Spectrophotometric analysis revealed that the max-imum of 93.6% of RSV has been entrapped in GNPs. In vitro drug release kinetics indicated that there was an initial burst release followed by a slow and sustained release of RSV from GNPs. The prepared RSV-GNPs exhibited very rapid and more efficient cellular uptake than free RSV. Further, RSV-GNPs treatment showed greater antiproliferative efficacy than free RSV treatment in NCI-H460 cells. It has been found that greater ROS generation, DNA damage and apoptotic incidence in RSV-GNPs treated cells than free RSV treatment. Erythrocyte aggregation assay showed that the prepared RSV-GNPs formulation elicit no toxic response. HPLC analysis revealed that RSV-GNPs was more bioavailable and had a longer half-life than free RSV. Hence, GNPs carrier system might be a promising mode for controlled delivery and for improved therapeutic index of poorly water soluble RSV.

Keywords: resveratrol, coacervation, anticancer gelatin nanoparticles, lung cancer, controlled release

Procedia PDF Downloads 425

Authors: Anoff Anim, Lila Mahmoud, Maria Katsikogianni, Sanjit Nayak

Abstract:

Sustained and controlled delivery of antimicrobial drugs have been largely studied recently using metal organic frameworks (MOFs)and different polymers. However, much attention has not been given to combining both MOFs and biodegradable polymers, which would be a good strategy in providing a sustained gradual release of the drugs. Herein, we report a comparative study of the sustained and controlled release of widely used antibacterial drugs, cephalexin and metronidazole, from zinc-based MOF-5 incorporated in biodegradable polycaprolactone (PCL) and poly-lactic glycolic acid (PLGA) membranes. Cephalexin and metronidazole were separately incorporated in MOF-5 post-synthetically, followed by their integration into biodegradable PLGA and PCL membranes. The pristine MOF-5 and the loaded MOFs were thoroughly characterized by FT-IR, SEM, TGA and PXRD. Drug release studies were carried out to assess the release rate of the drugs in PBS and distilled water for up to 48 hours using UV-Vis Spectroscopy. Four bacterial strains from both the Gram-positive and Gram-negative types, Staphylococus aureus, Staphylococuss epidermidis, Escherichia coli, Acinetobacter baumanii, were tested against the pristine MOF, pure drugs, loaded MOFs and the drug-loaded MOF-polymer composites. Metronidazole-loaded MOF-5 composite of PLGA (PLGA-Met@MOF-5) was found to show highest efficiency to inhibit the growth of S. epidermidis compared to the other bacteria strains while maintaining a sustained minimum inhibitory concentration (MIC). This study demonstrates that the combination of biodegradable MOF-polymer composites can provide an efficient platform for sustained and controlled release of antimicrobial drugs and can be a potential strategy to integrate them in biomedical devices.

Keywords: antimicrobial resistance, biodegradable polymers, cephalexin, drug release metronidazole, MOF-5, PCL, PLGA

Procedia PDF Downloads 103

Authors: J. W. Ahn, I. Y. Choi, T. V. Dinh, J. C. Kim

Abstract:

A cooler has been widely employed in the extractive system of the continuous emission monitoring system (CEMS) to remove water vapor in the gas stream. The effect of the cooler on analytical target gases was investigated in this research. A commercial cooler for the CEMS operated at 4 C was used. Several gases emitted from a coal power plant (i.e. CO2, SO2, NO, NO2 and CO) were mixed with humid air, and then introduced into the cooler to observe its effect. Concentrations of SO2, NO, NO2 and CO were made as 200 ppm. The CO2 concentration was 8%. The inlet absolute humidity was produced as 12.5% at 100 C using a bubbling method. It was found that the reduction rate of SO2 was the highest (~21%), followed by NO2 (~17%), CO2 (~11%) and CO (~10%). In contrast, the cooler was not affected by NO gas. The result indicated that the cooler caused a significant effect on the water soluble gases due to condensate water in the cooler. To overcome this problem, a correction factor may be applied. However, water vapor might be different, and emissions of target gases are also various. Therefore, the correction factor is not only a solution, but also a better available method should be employed.

Keywords: cooler, CEMS, monitoring, reproductive, sampling

Procedia PDF Downloads 336

Authors: Chayonnat Thanamun, Kreangkrai Maneeintr

Abstract:

For petroleum industry, polymer flooding is the one of the main methods in enhanced oil recovery (EOR) that is used water-soluble polymer such as partially hydrolyzed polyacrylamide (HPAM) to increase oil production. It is added to the flooding water to improve the mobility ratio in the flooding process. During the polymer flooding process, water is produced as a by-product along with oil and gas production. This produced water is a mixture of inorganic and organic compound. Moreover, produced water is more difficult to treat than that from water flooding. In this work, the effect of HPAM residue on the wastewater treatment from polymer flooding is studied. Polyaluminium chloride (PAC) is selected to use as a flocculant. Therefore, the objective of this study is to evaluate the effect of polymer residues in produced water on the wastewater treatment by using PAC. The operating parameters of this study are flocculant dosage ranging from 300,400 and 500 mg/L temperature from 30-50 Celsius degree and HPAM concentrations from 500, 1000 and 2000 mg/L. Furthermore, the turbidity, as well as total suspended solids (TSS), are also studied. The results indicated that with an increase in HPAM concentration, the TSS and turbidity increase gradually with the increasing of coagulant dosage under the same temperature. Also, the coagulation-flocculation performance is improved with the increasing temperature. This can be applied to use in the wastewater treatment from oil production before this water can be injected back to the reservoir.

Keywords: wastewater treatment, petroleum production, polyaluminium chloride, polyacrylamide

Procedia PDF Downloads 116

Authors: Anoff Anim, Lila A. M. Mahmoud, Maria Katsikogianni, Sanjit Nayak

Abstract:

Sustained and controlled delivery of antimicrobial drugs have been largely studied recently using metal organic frameworks (MOFs)and different polymers. However, much attention has not been given to combining both MOFs and biodegradable polymers, which would be a good strategy in providing a sustained gradual release of the drugs. Herein, we report a comparative study of the sustained and controlled release of widely used antibacterial drugs, cephalexin and metronidazole, from zinc-based MOF-5 incorporated in biodegradable polycaprolactone (PCL) and poly-lactic glycolic acid (PLGA) membranes. Cephalexin and metronidazole were separately incorporated in MOF-5 post-synthetically, followed by their integration into biodegradable PLGA and PCL membranes. The pristine MOF-5 and the loaded MOFs were thoroughly characterized by FT-IR, SEM, TGA and PXRD. Drug release studies were carried out to assess the release rate of the drugs in PBS and distilled water for up to 48 hours using UV-Vis Spectroscopy. Four bacterial strains from both the Gram-positive and Gram-negative types, Staphylococus aureus, Staphylococuss epidermidis, Escherichia coli, Acinetobacter baumanii, were tested against the pristine MOF, pure drugs, loaded MOFs and the drug-loaded MOF-polymer composites. Metronidazole-loaded MOF-5 composite of PLGA (PLGA-Met@MOF-5) was found to show highest efficiency to inhibit the growth of S. epidermidis compared to the other bacteria strains while maintaining a sustained minimum inhibitory concentration (MIC). This study demonstrates that the combination of biodegradable MOF-polymer composites can provide an efficient platform for sustained and controlled release of antimicrobial drugs and can be a potential strategy to integrate them in biomedical devices.

Keywords: antimicrobial resistance, biodegradable polymers, cephalexin, drug release metronidazole, MOF-5, PCL, PLGA

Procedia PDF Downloads 99

Authors: Rouighi Mustapha, Bouzid Laghaa Souad, Rouighi Tahar

Abstract:

Due to rain Shortage and the increase of population in the last years, wells excavation and groundwater use for different purposes had been increased without any planning. This is a great challenge for our country. Moreover, this scarcity of water resources in this region is unfortunately combined with rapid fresh water resources quality deterioration, due to salinity and contamination processes. Therefore, it is necessary to conduct the studies about groundwater quality in Algeria. In this work consists in the identification of the factors which influence the water quality parameters in Laghouat region by using statistical analysis Principal Component Analysis (PCA), Hierarchical Cluster Analysis (HCA) and geographic information system (GIS) in an attempt to discriminate the sources of the variation of water quality variations. The results of PCA technique indicate that variables responsible for water quality composition are mainly related to soluble salts variables; natural processes and the nature of the rock which modifies significantly the water chemistry. Inferred from the positive correlation between K+ and NO3-, NO3- is believed to be human induced rather than naturally originated. In this study, the multivariate statistical analysis and GIS allows the hydrogeologist to have supplementary tools in the characterization and evaluating of aquifers.

Keywords: cluster, analysis, GIS, groundwater, laghouat, quality

Procedia PDF Downloads 294

Authors: M. S. Deshpande, Snehal D. Bomble

Abstract:

Tuberculosis (TB) is a deadly contagious disease that is caused by a bacterium called Mycobacterium tuberculosis. More than sixty years ago, the introduction of the first anti-TB drugs for the treatment of TB (streptomycin (STR), p-aminosalcylic acid (PAS), isoniazid (INH), and then later ethambutol (EMB) and rifampicin (RIF)) gave optimism to the medical community, and it was believed that the disease would be completely eradicated soon. Worldwide, the number of TB cases has continued to increase, but the incidence rate has decreased since 2003. Recently, highly drug-resistant forms of TB have emerged worldwide. The prolonged use of classical drugs developed a growing resistance and these drugs have gradually become less effective and incapable to meet the challenges, especially those of multi drug resistant (MDR)-TB, extensively drug resistant (XDR)-TB, and HIV-TB co-infections. There is an unmet medical need to discover newer synthetic molecules and new generation of potent drugs for the treatment of tuberculosis which will shorten the time of treatment, be potent and safe while effective facing resistant strains and non-replicative, latent forms, reduce adverse side effect and not interfere in the antiretroviral therapy. This paper attempts to bring out the review of anti-TB drugs, and presents a novel method of synthesizing new anti-tuberculosis drugs and potential compounds to overcome the bacterial resistance and combat the re-emergence of tuberculosis.

Keywords: tuberculosis, mycobacterium, multi-drug resistant (MDR)-TB, extensively drug resistant (XDR)-TB

Procedia PDF Downloads 351

Authors: Lacramioara Ochiuz, Manuela Hortolomei, Aurelia Vasile, Iulian Stoleriu, Marcel Popa, Cristian Peptu

Abstract:

Local antibiotherapy is one of the most effective acne therapies. Erythromycin (ER) is a macrolide antibiotic topically administered for over 30 years in the form of gel, ointment or hydroalcoholic solution for the acne therapy. The use of ER as a base for topical dosage forms raises some technological challenges due to the physicochemical properties of this substance. The main disadvantage of ER is the poor water solubility (2 mg/mL) that limits both formulation using hydrophilic bases and skin permeability. Cyclodextrins (CDs) are biocompatible cyclic oligomers of glucose, with hydrophobic core and hydrophilic exterior. CDs are used to improve the bioavailability of drugs by increasing their solubility and/or their rate of dissolution after including the poorly water soluble substances (such as ER) in the hydrophobic cavity of CDs. Adding CDs leads to the increase of solubility and improved stability of the drug substance, increased permeability of substances of low water solubility, decreased toxicity and even to active dose reduction as a result of increased bioavailability. CDs increase skin tolerability by reducing the irritant effect of certain substances. We have included ER to lactide modified β-cyclodextrin, in order to improve the therapeutic effect of topically administered ER. The aims of the present study were to synthesise and describe a new complex with prolonged release of ER with lactide modified β-cyclodextrin (CD-LA_E), to investigate the CD-LA_E complex by scanning electron microscopy (SEM) and Fourier transform infrared spectroscopy (FTIR), to analyse the effect of semisolid base on the in vitro and ex vivo release characteristics of ER in the CD-LA_E complex by assessing the permeability coefficient and the release kinetics by fitting on mathematical models. SEM showed that, by complexation, ER changes its crystal structure and enters the amorphous phase. FTIR analysis has shown that certain specific bands of some groups in the ER structure move during the incapsulation process. The structure of the CD-LA_E complex has a molar ratio of 2.12 to 1 between lactide modified β-cyclodextrin and ER. The three semisolid bases (2% Carbopol, 13% Lutrol 127 and organogel based on Lutrol and isopropyl myristate) show a good capacity for incorporating the CD-LA_E complex, having a content of active ingredient ranging from 98.3% to 101.5% as compared to the declared value of 2% ER. The results of the in vitro dissolution test showed that the ER solubility was significantly increased by CDs incapsulation. The amount of ER released from the CD-LA_E gels was in the range of 76.23% to 89.01%, whereas gels based on ER released a maximum percentage of 26.01% ER. The ex vivo dissolution test confirms the increased ER solubility achieved by complexation, and supports the assumption that the use of this process might increase ER permeability. The highest permeability coefficient was obtained in ER released from gel based on 2% Carbopol: in vitro 33.33 μg/cm2/h, and ex vivo 26.82 μg/cm2/h, respectively. The release kinetics of complexed ER is performed by Fickian diffusion, according to the results obtained by fitting the data in the Korsmeyer-Peppas model.

Keywords: erythromycin, acne, lactide, cyclodextrin

Procedia PDF Downloads 233

Authors: Anoff Anim, Lila Mahmound, Maria Katsikogianni, Sanjit Nayak

Abstract:

Sustained and controlled delivery of antimicrobial drugs have been largely studied recently using metal organic frameworks (MOFs)and different polymers. However, much attention has not been given to combining both MOFs and biodegradable polymers which would be a good strategy in providing a sustained gradual release of the drugs. Herein, we report a comparative study of the sustained and controlled release of widely used antibacterial drugs, cephalexin and metronidazole, from zinc-based MOF-5 incorporated in biodegradable polycaprolactone (PCL) and poly-lactic glycolic acid (PLGA) membranes. Cephalexin and metronidazole were separately incorporated in MOF-5 post-synthetically, followed by their integration into biodegradable PLGA and PCL membranes. The pristine MOF-5 and the loaded MOFs were thoroughly characterized by FT-IR, SEM, TGA and PXRD. Drug release studies were carried out to assess the release rate of the drugs in PBS and distilled water for up to 48 hours using UV-Vis Spectroscopy. Four bacterial strains from both the Gram-positive and Gram-negative types, Staphylococus aureus, Staphylococuss epidermidis, Escherichia coli, Acinetobacter baumanii, were tested against the pristine MOF, pure drugs, loaded MOFs and the drug-loaded MOF-polymer composites. Metronidazole-loaded MOF-5 composite of PLGA (PLGA-Met@MOF-5) was found to show highest efficiency to inhibit the growth of S. epidermidis compared to the other bacteria strains while maintaining a sustained minimum inhibitory concentration (MIC). This study demonstrates that the combination of biodegradable MOF-polymer composites can provide an efficient platform for sustained and controlled release of antimicrobial drugs, and can be a potential strategy to integrate them in biomedical devices.

Keywords: antimicrobial resistance, biodegradable polymers, cephalexin, drug release metronidazole, MOF-5, PCL, PLGA

Procedia PDF Downloads 50

Authors: M. P. Raju, P. D. Safai, P. S. P. Rao, P. C. S. Devara, C. V. Naidu

Abstract:

In order to study the Physical and chemical characteristics of aerosols, samples of Total Suspended Particulates (TSP) were collected using a high volume sampler at Pune, a semi-urban location in SW India during March 2009 to February 2010. TSP samples were analyzed for water soluble components like F, Cl, NO3, SO4, NH4, Na, K, Ca, and Mg and acid soluble components like Al, Zn, Fe and Cu using Ion-Chromatograph and Atomic Absorption Spectrometer. Analysis of the data revealed that the monthly mean TSP concentrations varied between 471.3 µg/m3 and 30.5 µg/m3 with an annual mean value of 159.8 µg/m3. TSP concentrations were found to be less during post-monsoon and winter (October through February), compared to those in summer and monsoon (March through September). Anthropogenic activities like vehicular emissions and dust particles originated from urban activities were the major sources for TSP. TSP showed good correlation with all the major ionic components, especially with SO4 (R= 0.62) and NO3 (R= 0.67) indicating the impact of anthropogenic sources over the aerosols at Pune. However, the overall aerosol nature was alkaline (Ave pH = 6.17) mainly due to the neutralizing effects of Ca and NH4. SO4 contributed more (58.8%) to the total acidity as compared to NO3 (41.1%) where as, Ca contributed more (66.5%) to the total alkalinity than NH4 (33.5%). Seasonality of acid soluble component Al, Fe and Cu showed remarkable increase, indicating the dominance of soil source over the man-made activities. Overall study on TSP indicated that aerosols at Pune were mainly affected by the local sources.

Keywords: chemical composition, acidic and neutralization potential, radiative forcing, urban station

Procedia PDF Downloads 222