224 research outputs found

    Modeling Diachrony in Dictionaries

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    we want to show in this paper that it is possible to apply coherent modeling principles to deal with this variety of structures while providing a precise account of complex sub-components such as diachronic information as they appear in dictionaries with wide lexical coverage. Besides, we want to show that such modeling principles can guide the possible evolution of the TEI towards a more flexible data for the concrete representation of dictionaries

    FORMULATION AND EVALUATION OF RAMIPRIL MOUTH DISSOLVING FILMS

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    Objective: The present investigation was aimed at preparation and evaluation of mouth dissolving films (MDFs) of Ramipril to enhance patient convenience, compliance and to improve bioavailability. Methods: MDFs with 0.5% w/w Ramipril were prepared by a solvent casting method using a wet film applicator. The effects of film formers, wetting/solubilizing, saliva stimulating agents and film modifiers on the physicomechanical and in vitro Ramipril release from MDFs were evaluated. Results: The MDFs prepared were transparent, smooth and showed no re-crystallization upon storage. MDFs casted with hydroxypropyl methylcellulose (HPMC) E3 as film former and polyethylene glycol (PEG-400) as plasticizer showed superior Ramipril release rates and good physicomechanical properties when compared to MDFs with E5 and E15 as film formers. HPMC E3 MDFs with polyvinyl pyrrolidone K30 (PVP K30) and sodium lauryl sulphate (SLS) gave superior drug release properties than MDFs without PVP K30 and SLS. The HPMC E3 MDFs with citric acid (CA) as saliva stimulating and xylitol as soothing agent gave significantly superior in vitro drug release than the MDFs without CA and xylitol. Release kinetics data reveals diffusion as a drug release mechanism. Conclusion: From the obtained results, it can be concluded that the administration of Ramipril as MDF may provide a quick onset of action with enhanced oral bioavailability and therapeutic efficacy

    Formulation and Evaluation of Chlorpheniramine Maleate Mouth Dissolving Films

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    The present investigation was aimed at preparation and evaluation of mouth dissolving films (MDFs) of an anti-histamine drug, Chlorpheniramine Maleate (CPM) to enhance convenience and compliance to the elderly and paediatric patients. The MDFs were prepared using wet film applicator and evaluated for physicochemical and physicomechanical properties. MDFs were prepared with 0.6% and 0.8% w/w CPM. The MDFs with 0.8% w/w drug load showed re-crystallisation within 10 days, while the MDFs with 0.6% w/w CPM load were transparent with no re-crystallization. The effect of film formers, film thickness, film modifiers, saliva stimulating and soothing agents on the physicomechanical properties and CPM release from MDFs were evaluated. MDFs casted at 30mil thickness containing poly ethylene glycol (PEG-400) as plasticizer showed superior CPM release rates along with good physicomechanical properties. MDFs with hydroxy propyl methyl cellulose (HPMC) E3 as film former gave superior CPM release rate when compared to E5 and E15 formulations. MDFs with poly vinyl pyrrolidone K30 (PVPK30) gave superior drug release properties when compared to MDFs without PVP K30. The MDFs with citric acid (CA) and xylitol gave superior CPM release than the other MDFs. Release kinetics data reveals diffusion as drug release mechanism

    Enantioselective Synthesis of Antiepileptic Drug: (-)-Levetiracetam-Synthetic Applications of the Versatile New Chiral N-Sulïżœnimine

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    We report an asymmetric synthesis of (-)-Levetiracetam (1) in six steps starting from versatile new chiral N-sulïżœnimine (3). e key step, stereoselective 1,2-addition of ethylmagnesium bromide (EtMgBr) to chiral N-sulïżœnimine derived from (R)-glyceraldehyde acetonide and (S)-t-BSA, gave the corresponding sulfonamide (2) in high diastereoselectivity. Simultaneous deprotection and deacetylation followed by NaIO 4 cleavage and reduction gave -amino alcohol (6). Subsequent reactions yielded the targeted compound levetiracetam (1)

    Developments on drug discovery and on new therapeutics: highly diluted tinctures act as biological response modifiers

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    <p>Abstract</p> <p>Background</p> <p>In the search for new therapies novel drugs and medications are being discovered, developed and tested in laboratories. Highly diluted substances are intended to enhance immune system responses resulting in reduced frequency of various diseases, and often present no risk of serious side-effects due to its low toxicity. Over the past years our research group has been investigating the action of highly diluted substances and tinctures on cells from the immune system.</p> <p>Methods</p> <p>We have developed and tested several highly diluted tinctures and here we describe the biological activity of M1, M2, and M8 both <it>in vitro </it>in immune cells from mice and human, and <it>in vivo </it>in mice. Cytotoxicity, cytokines released and NF-ÎșB activation were determined after <it>in vitro </it>treatment. Cell viability, oxidative response, lipid peroxidation, bone marrow and lymph node cells immunophenotyping were accessed after mice <it>in vivo </it>treatment.</p> <p>Results</p> <p>None of the highly diluted tinctures tested were cytotoxic to macrophages or K562. Lipopolysaccharide (LPS)-stimulated macrophages treated with all highly diluted tinctures decreased tumour necrosis factor alpha (TNF-α) release and M1, and M8 decreased IFN-<it>Îł </it>production. M1 has decreased NF-ÎșB activity on TNF-α stimulated reporter cell line. <it>In vivo </it>treatment lead to a decrease in reactive oxygen species (ROS), nitric oxide (NO) production was increased by M1, and M8, and lipid peroxidation was induced by M1, and M2. All compounds enhanced the innate immunity, but M1 also augmented acquired immunity and M2 diminished B lymphocytes, responsible to acquired immunity.</p> <p>Conclusions</p> <p>Based on the results presented here, these highly diluted tinctures were shown to modulate immune responses. Even though further investigation is needed there is an indication that these highly diluted tinctures could be used as therapeutic interventions in disorders where the immune system is compromised.</p

    The long-term prediction of return to work following serious accidental injuries: A follow up study

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    Background Considerable indirect costs are incurred by time taken off work following accidental injuries. The aim of this study was to predict return to work following serious accidental injuries. Method 121 severely injured patients were included in the study. Complete follow-up data were available for 85 patients. Two weeks post trauma (T1), patients rated their appraisal of the injury severity and their ability to cope with the injury and its job-related consequences. Time off work was assessed at one (T2) and three years (T3) post accident. The main outcome was the number of days of sick leave taken due to the accidental injury. Results The patients' appraisals a) of the injury severity and b) of their coping abilities regarding the accidental injury and its job-related consequences were significant predictors of the number of sick-leave days taken. Injury severity (ISS), type of accident, age and gender did not contribute significantly to the prediction. Conclusions Return to work in the long term is best predicted by the patients' own appraisal of both their injury severity and the ability to cope with the accidental injury

    In vitro and in vivo anticancer properties of a Calcarea carbonica derivative complex (M8) treatment in a murine melanoma model

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    <p>Abstract</p> <p>Background</p> <p>Melanoma is the most aggressive form of skin cancer and the most rapidly expanding cancer in terms of worldwide incidence. Chemotherapeutic approaches to treat melanoma have had only marginal success. Previous studies in mice demonstrated that a high diluted complex derived from <it>Calcarea carbonica </it>(M8) stimulated the tumoricidal response of activated lymphocytes against B16F10 melanoma cells <it>in vitro</it>.</p> <p>Methods</p> <p>Here we describe the <it>in vitro </it>inhibition of invasion and the <it>in vivo </it>anti-metastatic potential after M8 treatment by inhalation in the B16F10 lung metastasis model.</p> <p>Results</p> <p>We found that M8 has at least two functions, acting as both an inhibitor of cancer cell adhesion and invasion and as a perlecan expression antagonist, which are strongly correlated with several metastatic, angiogenic and invasive factors in melanoma tumors.</p> <p>Conclusion</p> <p>The findings suggest that this medication is a promising non-toxic therapy candidate by improving the immune response against tumor cells or even induce direct dormancy in malignancies.</p

    Controlling Groundwater Exploitation Through Economic Instruments: Current Practices, Challenges and Innovative Approaches

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    Groundwater can be considered as a common-pool resource, is often overexploited and, as a result, there are growing management pressures. This chapter starts with a broad presentation of the range of economic instruments that can be used for groundwater management, considering current practices and innovative approaches inspired from the literature on Common Pool Resources management. It then goes on with a detailed presentation of groundwater allocation policies implemented in France, the High Plains aquifer in the USA, and Chile. The chapter concludes with a discussion of social and political difficulties associated with implementing economic instruments for groundwater management
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