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Active Ingredient (active + ingredient)
Kinds of Active Ingredient Selected AbstractsPositive lymphocyte transformation test in a patient with allergic contact dermatitis of the scalp after short-term use of topical minoxidil solutionCONTACT DERMATITIS, Issue 1 2005Tobias Hagemann Topical 2,4-diamino-6-piperidinopyrimidine-3-oxide (minoxidil) solution has been widely used for the treatment of androgenetic alopecia for over 15 years now and the substance is currently approved for this indication in 2% and 5% formulation. Typical side effects of this topical treatment include irritative dermatitis going along with pruritus, erythema, scaling and dryness, which occur especially at the onset of the therapy. In some cases, allergic contact dermatitis or exacerbation of seborrhoic dermatitis has been reported. While most of the patients with allergic contact dermatitis described in the literature showed a positive sensitization to the vehicle substance propylene glycol evaluated by patch testing, reactions to the active ingredient minoxidil are rare. Here, we report a case of allergic sensitization to minoxidil, which we evaluated and differentiated from an irritative reaction by a combination of patch testing and lymphocyte transformation test. The differentiation of allergic and irritative adverse effects and the identification of the causative allergen are of major relevance for the proceeding and adjustment of the therapy. Patients with sensitizations against propylene glycol are candidates for preparations with alternative solvents but can proceed treatment with minoxidil. In contrast, patients with allergies to the active ingredient itself are no longer candidates for treatment with minoxidil and should undergo alternative therapeutic options. [source] The efficacy of a protective cream in a real-world apprentice hairdresser environmentCONTACT DERMATITIS, Issue 3 2001D. Perrenoud The object of this study was to compare the protective action of a new barrier cream (Excipial Protect®, Spirig Pharma AG, Egerkingen, Switzerland) to its vehicle in the context of hand irritation of apprentice hairdressers caused by repeated shampooing and exposure to hair-care products. This was a double-blind cross-over comparing Excipial Protect® (containing aluminium chlorohydrate 5% as active ingredient) against its vehicle alone. The efficacy of the creams was evaluated taking into account: (1) clinical scores by researchers, (2) biometric measurements, (3) subjective opinions of the subjects. An analysis of variance was performed considering order of application, degree of atopy, and reported number of shampoos. We observed very little difference in efficacy between the protective cream and its vehicle. The presence, however, of aluminium chlorhydrate in the protective cream was shown to have a positive effect against work-related irritation. The cosmetic qualities of the creams seemed, to the participants, to be as important as their real protective and hydrating properties, an important factor in compliance issues. [source] Botanical Extracts Used in the Treatment of CelluliteDERMATOLOGIC SURGERY, Issue 2005Doris Hexsel MD Background. Cellulite is defined as skin relief alterations that give the skin an orange peel or mattress appearance. The lesions tend to be asymptomatic and may be considered the anatomic expressions of the structures in the affected area, such as the fat and subcutaneous septa. Objective. The present article reviews the most important botanical extracts used as active ingredients in the treatment of cellulite, as well as the steps to obtain these botanicals as raw material and their standardization and quality control, which are important to guarantee their therapeutic action. Methods. The current literature was reviewed, and we also obtained information from the manufacturers of the prducts that contained botanicals because of the few publications about this subject. Conclusions. The reduction in fat deposits through the continuous use of anticellulite products depends on the availability of the active ingredient at the action site, the concentration of the ingredient in the formulation, and the physiochemical characteristics particular to each active ingredient. The botanicals used in topical products must have standardized extracts, which would permit each phytomedicine to have the same effect anywhere in the world. New scientific research is necessary to verify the efficacy and ideal concentrations of such substances. DORIS HEXSEL, MD, CECILIA ORLANDI, MD, AND DEBORA ZECHMEISTER DO PRADO, PHARM, HAVE INDICATED NO SIGNIFICANT INTEREST WITH COMMERCIAL SUPPORTERS. [source] The advantages and disadvantages of a ,herbal' medicine in a patient with diabetes mellitus: a case reportDIABETIC MEDICINE, Issue 6 2004D. M. Wood Abstract Background Patient-initiated alternative treatments in the management of chronic conditions are common and increasing in the United Kingdom. To date, there have been no reports of herbal medicine use alone in the management of diabetes mellitus. We report here the case of a man who attained excellent glycaemic control using a ,herbal' medicine and reveal how important it was to identify the products of active constituents. Case report A 48-year-old man attending our clinic in Tooting, South London with known Type 2 diabetes, with evidence of both micro- and macro-vascular diabetes-related complications, was poorly controlled despite a drug regimen consisting of oral metformin and twice daily insulin. He went to India for at least 1 year and on returning to the clinic had excellent glycaemic control off all diabetic medication. While away he had started himself on a regimen of three different ,herbal' balls. Samples of blood were found to contain chlorpropamide in a therapeutic concentration; chlorpropamide was also found in one of the balls. He has been counselled on the potential risks associated with chlorpropamide and his treatment reverted to a more conventional treatment regimen. Conclusions General practitioners and hospital physicians should be alert to those patients returning from abroad on effective ,herbal' medications that these may in fact contain an active ingredient. [source] Imaging studies of biodistribution and kinetics in drug developmentDRUG DEVELOPMENT RESEARCH, Issue 2 2003Marc S. Berridge Abstract Although the intravenous route of administration is rarely used for drugs, it is by far the most common route for PET and SPECT radiotracers. This article discusses the use of planar and tomographic nuclear medicine technologies to image and quantify the distribution of drugs after local administration. In principle, this would include topical dermatologic, otic, ophthalmic, rectal, and vaginal administration, as well as the intramuscular, oral, and inhalation routes, although precedents do not yet exist for all of these. The studies reviewed focus mainly on oral ingestion and oral and nasal inhalation. The use of nondrug tracers for formulations is discussed, principally with planar imaging or SPECT using radionuclides such as 99mTc, as well as PET imaging where the active ingredient of a formulation can be labeled with 11C or sometimes 18F. An example of the latter type is a study of the deposition and kinetics in the lungs and airways of triamcinolone acetonide, an antiinflammatory steroid used for topical treatment of allergic rhinitis and asthma, dispensed from an inhaler. PET has high potential for evaluation of different formulations and delivery devices in the development of topically applied drugs. Drug Dev. Res. 59:208,226, 2003. © 2003 Wiley-Liss, Inc. [source] Genotoxicity testing of the herbicide trifluralin and its commercial formulation Treflan using the piscine micronucleus testENVIRONMENTAL AND MOLECULAR MUTAGENESIS, Issue 6 2008Serpil Könen Abstract In this study, the genotoxic effects of a widely used herbicide, trifluralin, and its commercial formulation, Treflan, were evaluated using the micronucleus test in a commercially important fish species, Oreochromis niloticus (Nile Tilapia). Fish were exposed to 1, 5, and 10 ,g/L doses of trifluralin and Treflan for 3, 6, and 9 days under laboratory conditions. Ethylmethanesulfonate, at a single dose of 10 mg/L, was used as positive control. Micronuclei were evaluated on the peripheral erythrocytes. Both Treflan and trifluralin treatments significantly increased the micronucleus frequencies in peripheral erythrocytes of O. niloticus. Furthermore, the genotoxicity of the active ingredient, trifluralin, was observed to be higher than that of the commercial formulation Treflan. Our results indicate that herbicide trifluralin has genotoxic potential in fish. Environ. Mol. Mutagen., 2008. © 2008 Wiley-Liss, Inc. [source] Absorption of H2S in NaOCl caustic aqueous solutionENVIRONMENTAL PROGRESS & SUSTAINABLE ENERGY, Issue 3 2001Luke Chen Pilot plant experimental data were collected to study the feasibility of H2S removal from air streams utilizing aqueous solutions. Solutions of NaOCl/NaOH were tested in a packed bed scrubber and found to be effective. An efficiency of 99.2% H2S removal was achieved at a gas flow rate of 790 lb/f2 -hr and liquid-gas ratio of 5.06. Sodium hydroxide was found to be the active ingredient in the absorption process. A minimum alkalinity of pH 11 in the scrubbing solution was required for the H2S to be efficiently absorbed in the packed bed scrubber. For gas flow rates up to 2,100 lb/f2 hr, the height of a transfer unit (HTU) varied from 1.8 ft to 2 ft with different proportions of NaOCl and NaOH in the solution. [source] The Prospects of Carrying and Releasing Drugs Via Biodegradable Magnesium Foam,ADVANCED ENGINEERING MATERIALS, Issue 8 2010Eli Aghion Abstract Powder metallurgy technology was used to produce magnesium foams in order to evaluate their ability to perform as a solid biodegradable platform for drug delivery. The amount and delivery time of the released drug (gentamicin) was controlled by the level of space-holding particles (spacer) that was mixed with the magnesium powder prior to the sintering process. Metallurgical examination of the magnesium foams was carried out using optical and scanning electron microscopy (SEM) and X-ray diffraction analysis. Microtomography CT analysis was used to evaluate the structural characteristics of the magnesium foams and their internal interconnected porosity configuration. The corrosion behavior of the magnesium foams was evaluated by immersion test in a simulated physiological environment (PBS solution). The absorption of gentamicin was obtained by immersing magnesium foams in concentrated gentamicin solutions within a vacuum chamber, followed by water evaporation. The detection of gentamicin in PBS solution was carried out using a Fluorescence Polarimetry analyzer. The results show that the release profile of gentamicin from magnesium foam with 10 and 25% spacer in PBS solution was in accord with common dissolution kinetics of an active ingredient from polymeric drug delivery systems. [source] Effects of transgenic glufosinate-tolerant oilseed rape (Brassica napus) and the associated herbicide application on eubacterial and Pseudomonas communities in the rhizosphereFEMS MICROBIOLOGY ECOLOGY, Issue 3 2002Stephen Gyamfi Abstract A containment experiment was carried out in order to evaluate possible shifts in eubacterial and Pseudomonas rhizosphere community structures due to the release of genetically modified Basta-tolerant oilseed rape and the associated herbicide application. Treatments included cultivation of the transgenic plant as well as of the wild-type cultivar in combination with mechanical removal of weeds and the application of the herbicides Basta (active ingredient: glufosinate) and Butisan S (active ingredient: metazachlor). Rhizosphere soil was sampled from early and late flowering plants as well as from senescent plants. A culture-independent approach was chosen to characterize microbial communities based on denaturing gradient gel electrophoresis of 16S rRNA gene fragments amplified from rhizosphere DNA using eubacterial and Pseudomonas -specific PCR primers. Dominant pseudomonads in the rhizosphere were analyzed by sequence analysis. Whole community and Pseudomonas electrophoresis fingerprints revealed slightly altered microbial communities in the rhizosphere of transgenic plants; however, effects were minor as compared to the plant developmental stage-dependent shifts. Both herbicides caused transient changes in the eubacterial and Pseudomonas population structure, whereas differences due to the genetic modification were still detected at the senescent growth stage. The observed differences between transgenic and wild-type lines were most likely due to unintentionally modified plant characteristics such as altered root exudation. [source] Amphiregulin is a factor for resistance of glioma cells to cannabinoid-induced apoptosisGLIA, Issue 13 2009Mar Lorente Abstract Gliomas, one of the most malignant forms of cancer, exhibit high resistance to conventional therapies. Identification of the molecular mechanisms responsible for this resistance is therefore of great interest to improve the efficacy of the treatments against these tumors. ,9-Tetrahydrocannabinol (THC), the major active ingredient of marijuana, and other cannabinoids inhibit tumor growth in animal models of cancer, including glioma, an effect that relies, at least in part, on the ability of these compounds to induce apoptosis of tumor cells. By analyzing the gene expression profile of two sub-clones of C6 glioma cells with different sensitivity to cannabinoid-induced apoptosis, we found a subset of genes with a marked differential expression in the two sub-clones. Furthermore, we identified the epidermal growth factor receptor ligand amphiregulin as a candidate factor to mediate the resistance of glioma cells to cannabinoid treatment. Amphiregulin was highly overexpressed in the cannabinoid-resistant cell line, both in culture and in tumor xenografts. Moreover, in vivo silencing of amphiregulin rendered the resistant tumors xenografts sensitive to cannabinoid antitumoral action. Amphiregulin expression was associated with increased extracellular signal-regulated kinase (ERK) activation, which mediated the resistance to THC by blunting the expression of p8 and TRB3,two genes involved in cannabinoid-induced apoptosis of glioma cells. Our findings therefore identify Amphirregulin as a factor for resistance of glioma cells to THC-induced apoptosis and contribute to unraveling the molecular bases underlying the emerging notion that targeted inhibition of the EGFR pathway can improve the efficacy of antitumoral therapies. © 2009 Wiley-Liss, Inc. [source] Phytotoxicity assay for seed production using Brassica rapa L.INTEGRATED ENVIRONMENTAL ASSESSMENT AND MANAGEMENT, Issue 4 2010David Olszyk Abstract Although pesticide drift can affect crop yield adversely, current plant testing protocols emphasize only the potential impacts on vegetative plant growth. The present study was conducted to determine whether a plant species with a short life cycle, such as Brassica rapa L. Wisconsin Fast Plants®, can be used to indicate potential effects on seed production of herbicides applied at relatively low levels (e.g., low field application rates [FAR]). The effects of ,0.1,×,FAR of aminopyralid, cloransulam, glyphosate, primisulfuron, or sulfometuron applied 14 d after emergence (DAE), were evaluated for B. rapa grown in mineral soil in pots under greenhouse conditions. Effects were expressed as the effective concentration of the herbicide producing a 25% reduction in a response (EC25) based on nonlinear regression. Brassica rapa seed dry weight was reduced by sulfometuron at an EC25 of 0.00014,×,a field application rate (FAR) of 53,g active ingredient (a.i.) ha,1, primisulfuron at 0.008 (experiment 1) or 0.0050 (experiment 2),×,FAR of 40,g,a.i.,ha,1, cloransulam at 0.022,×,FAR of 18,g,a.i.,ha,1, glyphosate at 0.0399,×,FAR of 834,g,a.i.,ha,1, and by aminopyralid at 0.005,×,FAR of 123,g,a.i.,ha,1, but only for 1 of 2 experiments. Reduced seed production occurred at less than the FAR that reduced shoot dry weight with sulfometuron and primisulfuron, whereas neither aminopyralid, cloransulam, nor glyphosate affected shoot dry weight. A short life cycle form of B. rapa could be used to indicate reduced seed production with plants grown only 1 week longer (,35,DAE) than as the current vegetative vigor test for nontarget herbicide effects on plants. Integr Environ Assess Manag 2010;6:725,734. © 2010 SETAC [source] Selecting and evaluating native plants for region-specific phytotoxicity testingINTEGRATED ENVIRONMENTAL ASSESSMENT AND MANAGEMENT, Issue 1 2008David Olszyke Abstract In this study, we evaluated methodology to determine risks to terrestrial native plant species from potential herbicide drift, focusing on 1) selection of native species for testing, 2) growth of these species, and 3) variability in herbicide response among native species and compared with crop plants. Native plant species were selected for initial testing on the basis of spatial analysis, which indicated that species from Illinois, USA, were at potential risk for off-target effects of herbicide drift. On the basis of preliminary seed germination tests, 5 native plant species (Andropogon gerardi, Polygonum lapathifolium, Solidago canadensis, Symphyotrichum lateriflorum, and Tridens flavus) were selected for comparison with crops grown in Illinois, normally used in the US Environmental Protection Agency's (USEPA's) Vegetative Vigor Test (Avena sativa, Daucus carota, Glycine max, Solanum lycopersicon, and Zea mays), or both. When treated with low concentrations of a test herbicide, sulfometuron methyl, 2 native species, P. lapathifolium and S. canadensis, were as sensitive as the 5 crop species. The effective herbicide concentrations producing a 25% reduction in shoot dry weight (EC25) for these species, ranged from 0.00015 to 0.0014 times a field application concentration of 52 g/ha active ingredient of sulfometuron methyl. S. lateriflorum and T. flavus were less sensitive than the other native species, whereas A. gerardi was tolerant to sulfometuron methyl with no growth reduction at any herbicide concentration tested. This study indicated that native species can be successfully selected and grown, used in the suite of species used in the USEPA's phytotoxicity test to assess risks of chemical herbicides to nontarget plants. It also showed (with a limited number of species) that native species varied more in sensitivity to simulated herbicide drift than crop species often used in phytotoxicity testing and that a Weibull function was useful to calculate EC25 values when low concentrations of herbicides was used. [source] A Hibiscus Abelmoschus seed extract as a protective active ingredient to favour FGF-2 activity in skinINTERNATIONAL JOURNAL OF COSMETIC SCIENCE, Issue 6 2009D. Rival Synopsis In the skin, heparin, heparan sulphate and heparan sulphate proteoglycans control the storage and release of growth factors and protect them from early degradation. We developed a cosmetic active ingredient containing Hibiscus Abelmoschus seed extract (trade name LinefactorÔ) that can maintain the FGF-2 content in the skin by mimicking the protective effect of heparan sulphate proteoglycans. By preventing the natural degradation of FGF-2, Hibiscus Abelmoschus seed extract maintains the bioavailability of this growth factor for its target cells, i.e. skin fibroblasts. Our in vitro evaluations showed that this ingredient exhibited heparan sulphate-like properties and dose-dependently protected FGF-2 from thermal degradation. We could also show that, in turn, the protected FGF-2 could stimulate the synthesis of sulphated GAGs, the natural protective molecules for FGF-2, thus providing a double protection. Finally, the in vitro results were confirmed in vivo thanks to a clinical study in which skin biomechanical properties and reduction in wrinkles were assessed. Résumé Dans la peau, l'héparane sulfate et les protéoglycanes à héparane sulfate contrôlent le stockage et la libération des facteurs de croissance et les protègent de la dégradation prématurée. Nous avons développé un actif cosmétique contenant un extrait de graines d'Hibiscus Abelmoschus capable de maintenir le contenu en FGF-2 de la peau en mimant l'effet protecteur des protéoglycanes à héparane sulfate. En prévenant la dégradation naturelle du FGF-2, l'extrait de graines d'Hibiscus Abelmoschus maintient la biodisponibilité de ce facteur de croissance pour ses cellules cibles que sont les fibroblastes de la peau. Les évaluations in vitro ont montré que cet ingrédient possédait des propriétés « héparane sulfate-like » et protégeait le FGF-2 de la dégradation thermique de façon dose-dépendante. Nous avons également pu montrer qu'en retour, le FGF-2 protégé pouvait stimuler la synthèse de GAGs sulfatés naturellement protecteurs du FGF-2, offrant ainsi une double protection. Enfin, les résultats in vitro ont été confirmés in vivo par une étude clinique au cours de laquelle les propriétés biomécaniques de la peau ainsi que la réduction des rides ont étéévaluées. [source] A very promising new glucolipidic surfactant: LipowheatTMINTERNATIONAL JOURNAL OF COSMETIC SCIENCE, Issue 6 2005A. Djedour Synopsis LipowheatTM is an entirely biodegradable 100% natural active ingredient, extracted from non-transgenic wheat. Thanks to its very interesting properties, it can integrate the composition of most cosmetic and pharmaceutical products. The aim of this work was first to realize a large range of stable simple or multiple emulsions, in order to determine and evaluate the ability of a new glucolipidic surfactant LipowheatTM to form and stabilize emulsions. The rheological properties of these emulsions were tested during a 30-day storage period at three different storage conditions (cold, room temperature and at 40°C). In addition to dynamic and static rheological tests, droplet size distribution of the cream was also determined. Furthermore, a stable simple emulsion was selected to realize percutaneous absorption and evaluate the properties of LipowheatTM. Résumé Ce travail a pour objectif de mettre à jour et d'évaluer les propriètés émulsionnantes d'un nouveau tensioactif de nature glucolipidique, connu jusqu'alors pour ses propriétés actives en cosmétologie: le LipowheatTM. Cette étude comporte plusieurs parties distinctes: 1) Formulation d'émulsions simples L/H et/ou H/L et multiples H/L/H stabilisèes par du LipowheatTM, avec des huiles variant par leur origine (naturelle ou synthétique) ainsi que par leur polarité. 2) Caractérisation rhéologique, granulométrique, et conductimétrique de ces émulsions après les avoir soumises pendant 30 jours à des conditions de vieillissement accéléré (conservation à température ambiante, à +4°C et +40°C) et ce, afin d'en retenir les plus stables pour la suite de l'étude. 3) Enfin, dans une dernière phase, les propriètés de ces crèmes dans le domaine de la libération dermopharmaceutique seront évaluées lors d'études in vitro. [source] 20-O-,-D-Glucopyranosyl-20 (S)-protopanaxadiol (compound K) induces expression of hyaluronan synthase 2 gene in transformed human keratinocytes and fibroblasts and increases hyaluronan in hairless mouse skinINTERNATIONAL JOURNAL OF COSMETIC SCIENCE, Issue 6 2004S. Kim Ginsenosides, the major active ingredient of ginseng, show a variety of biomedical efficacies such as anti-aging, anti-oxidation and anti-inflammatory activities. To understand the effects of 20-O-,-D-glucopyranosyl-20 (S)-protopanaxadiol (compound K), one of the major metabolites of ginsenosides on the skin, we assessed the expression level of approximately 100 transcripts in compound K-treated HaCaT cells using cDNA microarray analysis. Compound K treatment induced differential expression of 40 genes, which have been reported to be involved in the organization of the structure of the extracellular matrix as well as defense responses in human skin cells. One of the most interesting findings is a two-fold increase in hyaluronan synthase2 (HAS2) gene expression by compound K. We found that change in expression of HAS2 gene represents a specific response of HaCaT cells to compound K because hyaluronan synthase 1,3 was not changed by treatment with compound K. We also demonstrated that the compound K effectively induced hyaluronan synthesis in human skin cells and hairless mouse skin. A human clinical study indicated that topical application of compound K containing oil-in-water emulsion showed improvement of xerosis, wrinkle and fine lines in the aged skin. We concluded that compound K has anti-aging effects by the induction of HAS2 gene expression and following hyaluronan synthase. [source] A double-blind randomized vehicle-controlled clinical trial investigating the effect of ZnPTO dose on the scalp vs. antidandruff efficacy and antimycotic activityINTERNATIONAL JOURNAL OF COSMETIC SCIENCE, Issue 4 2003P. Bailey Synopsis Dandruff is a common problem in approximately 30% of the world's population. Reports in the literature regarding treatment of this condition with various antidandruff shampoos usually report the level of active ingredient within the formulation. However, we propose that a more important parameter relating to antidandruff efficacy is the amount of active ingredient delivered to the scalp from the shampoo. This report describes the results from two studies designed to investigate the relationship between the level of zinc pyrithione (ZnPTO) deposited onto the scalp and the resultant scalp condition. A double-blind randomized vehicle-controlled clinical study comparing three shampoos , a vehicle, a low-depositing ZnPTO shampoo and a high-depositing ZnPTO shampoo , was carried out in the U.K. with 53 panelists with dandruff or mild-to-moderate seborrheic dermatitis of the scalp. Both shampoos containing ZnPTO were significantly superior in antidandruff efficacy to the vehicle. Furthermore, the high-depositing ZnPTO shampoo was significantly superior compared with the low-depositing ZnPTO shampoo in terms of both antidandruff efficacy and antimycotic activity. Antidandruff performance and antimycotic activity of ZnPTO-containing shampoos is highly dependent on the amount of active ingredient delivered to the scalp. Furthermore, careful manipulation of the formulation parameters of an antidandruff shampoo can result in enhanced levels of delivery of the active ingredient without having to increase the level of active ingredient within the formulation. Résumé Les pellicules sont un problème courant rencontré par environ 30% de la population mondiale. Les rapports de la littérature relatifs à son traitement par des shampooings antipelliculaires mentionnent couramment le taux d'actif inclus dans la formule. Nous proposons cependant un paramètre plus important, vis à vis de l'activité antipelliculaire, c'est à dire le taux d'actif délivré par le shampooing sur le cuir chevelu. Cet article décrit les résultats de deux études conçues pour déterminer les types de relation entre le taux de Zn PTO déposé sur le cuir chevelu et l'état de celui ci qui en résulte. Une étude randomisée, contrôlée par véhicule, a comparé 3 shampooings (la base véhicule non traitante, un shampooing à faible déposition de Zn PTO et un shampooing à fort taux de dépôt de Zn PTO), a été conduite au Royaume Uni sur 53 volontaires sujets pelliculaires ou à faible ou modérée Dermite Séborrhéique. Les deux shampooings contenant le Zn PTO ont été trouvés significativement supérieurs dans leur activité anti pelliculaire au véhicule. De plus, le shampooing à fort dépôt était significativement plus efficace que celui à faible dépôt, tant dans l'activité anti pellicualire qu'anti mycotique. En conclusion, la performance anti pelliculaire et anti mycotique de shampooings à base de Zn PTO semble hautement dépendante du taux d'actif délivré sur le cuir chevelu. De plus, un choix judicieux des paramètres de formulation du shampooing anti pelliculaire peut amener à accroître les taux de délivrance de l'actif sans avoir à augmenter celui ci au sein de la formule. [source] Efficacy of chemical and botanical over-the-counter pediculicides available in Brazil, and off-label treatments, against head lice ex vivoINTERNATIONAL JOURNAL OF DERMATOLOGY, Issue 3 2010André Asenov MD Background, There is a lack of reliable data on the efficacy of over-the-counter (OTC) pediculicides in Brazil. Methods, We performed ex vivo assays of eight marketed pediculicides: 1% permethrin (Kwell®, Clean Hair®, Keltrina®, Nedax®), 0.02% deltamethrin (Deltacid®, Pediderm®), and two "natural" products (Piolho e Lêndea®, Pilogenio®). We also tested 5% permethrin (Keltrina Plus®), traditional home remedies and an ivermectin-based product used in veterinary medicine. Head lice (49,52 per group) were immersed in the compound for 3 min and washed after 20 min to simulate the typical in vivo treatment protocol. Lice were examined for activity up to 24 h using stringent criteria for survival. Results, Of the permethrin containing products, highest mortality was observed with Kwell® and Clean Hair® (97.9 and 90.2% after 4 h). Keltrina®, Nedax®, Keltrina Plus®, and the two deltamethrin-based products showed only a low efficacy of <60% after 4 h. With exception of pure coconut oil (80% mortality after 4 h), home remedies showed a very low efficacy, and both marketed products killed few lice. The ivermectin-based product caused a mortality of 100% after 4 h. Conclusions, Most Brazilian OTC products did not show a satisfactory efficacy against head lice. Resistance may be present. Ivermectin and coconut oil are promising compounds for topical treatment. Laboratory-based tests should be used to assess resistance patterns and to identify formulations of the active ingredient that increase the efficacy. Standardized testing should be performed before a product is licensed for head lice treatment. [source] Evidence of pesticide resistance in medium-sized mammalian pests: a case study with 1080 poison and Australian rabbitsJOURNAL OF APPLIED ECOLOGY, Issue 4 2002Laurie E. Twigg Summary 1Toxicant-resistance is a potential, or very real, problem with many pest-control programmes world-wide. However, apart from rodents, pesticide-resistance has not been well documented in vertebrates. We assessed the potential impact of developing resistance to 1080 in rabbit populations with differing levels of historical exposure to 1080-baiting programmes in south-western Australia. 2The sensitivity to 1080 of three out of the four populations of rabbits Oryctolagus cuniculus examined had decreased significantly since Australian rabbits were last tested over 25 years ago. The lethal dose50 (LD50) values for these populations, as determined from formal toxicity trials, ranged from 0·744 to 1·019 mg pure 1080 kg,1, and were significantly greater (P < 0·05) than the previously reported values for Australian rabbits (LD50 range 0·34,0·46 mg pure 1080 kg,1). The LD50 value for the fourth population (0·584 mg pure 1080 kg,1), which has had the least exposure to 1080, did not differ from that reported previously (P > 0·05). 3The lethal dose99 (LD99) values for the four rabbit populations tested ranged from 1·181 to 1·666 mg pure 1080 kg,1, and suggested that, theoretically, all rabbits should be killed during routine baiting campaigns provided that there is no loss of active ingredient from the bait. In reality, the efficacy of 1080 poison bait laid in trails for controlling free-ranging rabbits was reduced in those populations where rabbits had decreased sensitivity to 1080. Mean reductions in rabbit numbers 7,9 days after trail baiting of resistant and sensitive populations ranged from 51·2% to 65·2%, and from 76·4% to 76·5%, respectively. 4These findings suggest that genetic resistance to 1080 is developing in at least some populations of Australian rabbits. This has world-wide implications for agricultural protection and wildlife conservation programmes that rely on a 1080-baiting strategy for reducing the impact of vertebrate pests. [source] Season-long mating disruption of citrus leafminer, Phyllocnistis citrella Stainton, with an emulsified wax formulation of pheromoneJOURNAL OF APPLIED ENTOMOLOGY, Issue 6 2010L. L. Stelinski Abstract The citrus leafminer, Phyllocnistis citrella Stainton (Lepidoptera: Gracillariidae), is a major worldwide pest of citrus. Larval feeding by this insect facilitates proliferation of citrus bacterial canker, Xanthomonas axonopodis pv. citri. Herein, we describe a season-long disruption trial of P. citrella with a newly developed, emulsified wax dispenser of pheromone (SPLAT-CLMTM). A formulation containing a 3 : 1 blend of (Z,Z,E)-7,11,13-hexadecatrienal:(Z,Z)-7,11-hexadecadienal at a 0.2% loading rate of active ingredient by weight and deployed twice per season (24 weeks total) at 490 g of formulation/ha caused season-long disruption of male moth catch in pheromone traps as well as reduced leaf infestation. Analysis of pheromone release from dispensers by gas chromatography revealed that effective disruption of P. citrella occurred at a deployment rate of 126 ,g of (Z,Z,E)-7,11,13-hexadecatrienal/ha/h. Direct observation of moth behaviour in the field suggested that disruption by this formulation occurred by a non-competitive mechanism. A formulation of the 3 : 1 attractive blend at a 0.02% pheromone loading rate caused only 2,6 weeks of disruption per deployment and did not reduce leaf infestation during mid and end of the season evaluations. A formulation containing 0.2% of (Z,Z)-7,11-hexadecadienal alone and deployed at 490 g/ha caused 6,7 weeks of moth disruption to pheromone traps and did not prevent leaf infestation, while an identical formulation loaded with 0.02% (w/w) of (Z,Z)-7,11-hexadecadienal alone had no effect on P. citrella orientation to pheromone traps. The SPLAT formulation evaluated herein appears to be an excellent release device for (Z,Z,E)-7,11,13-hexadecatrienal given that approximately 100 days of steady release occurred following an initial brief (ca. 7 days) burst of higher release. The advantages of SPLAT as a formulation for P. citrella disruption include low cost of manufacturing, biodegradable and weather resistant characteristics, and flowability allowing machine application. Mating disruption should be an effective alternative to insecticides for management of P. citrella and may reduce the incidence of citrus canker. [source] Short-term assessment of dung beetle response to carbosulfan treatment against desert locust in SudanJOURNAL OF APPLIED ENTOMOLOGY, Issue 8 2009H. Eriksson Abstract The beneficial role of dung beetles (Coleoptera: Scarabaeidae) is well known. Potential risks to these beetles from the widespread use of insecticides against the desert locust, a significant plant pest in Africa, the Near East and South West Asia, have not been studied previously. Short-term responses of dung beetles to carbamate carbosulfan (Marshal®, ultra low-volume formulation, 100 g active ingredient ha,1) were assessed during desert locust control operations at five sites within two major biotopes: Acacia tortilis shrubland and cultivated wetland; on the Red Sea Coast of Sudan. The study took place during January,February 2004. At each site, fresh dung from Zebu cows was placed in areas targeted for desert locust control. Dung pats were placed in plots in two areas and left for 24 h, before and after insecticide application. Beetles were extracted by floatation. There was a significant decrease in abundance between the pre- and post-spray period in treated areas for the Scarabaeinae species Onthophagus margaritifer (a dark colour morph). In contrast, it was found that Aphodius lucidus and beetles at the subfamily level of Aphodiinae increased in numbers after insecticide treatment. Mortality and sublethal impacts as well as a repellent effect of the insecticide may explain the decrease in Onthophagus margaritifer, while the increase in Aphodiinae beetles could be an indirect response to lower numbers of Scarabaeinae beetles in competing for the same resource. These organisms and the applied methodology may be useful for environmental monitoring of desert locust control, thus further studies are suggested. The assessment also revealed a marked difference between the two biotopes with high abundance and species richness of dung beetles in A. tortilis shrubland, while these measures were low in the cultivated wetland. Five new species of dung beetles for Sudan were found in this study. [source] Effects of intentional gaps in spray coverage on the efficacy of gypsy moth mating disruptionJOURNAL OF APPLIED ENTOMOLOGY, Issue 9-10 2005K. Tcheslavskaia Abstract:, The study was conducted during 2001 and 2002 in forested areas in Virginia, US to examine the effects of gaps in coverage of pheromone on gypsy moth, Lymantria dispar (L.) (Lep., Lymantriidae), mating disruption. Gypsy moth male moth catches in pheromone-baited traps were significantly reduced in plots treated with the gypsy moth sex pheromone, disparlure, at an overall application rate of 37.5 g of active ingredient (AI)/ha but with untreated gaps of 30 or 90 m between 30-m wide treated swaths. In one of the two plots with 90 m gaps, significantly more males were captured in traps in the untreated areas compared with the treated areas within the plot. However, in another plot, significant differences in trap catches between treated and untreated areas were not observed. No difference in male moth catches in the pheromone-baited traps was observed between treated and untreated areas within the plots treated with 30 m gaps. Female mating success did not differ significantly between treated and untreated areas within the one plot in which it was measured. These results suggest that it may be possible to lower costs associated with gypsy moth mating disruption applications by alternating treated and untreated swaths, which would reduce flight time and fuel costs, without a reduction in efficacy. [source] Orientational disruption of codling moth, Cydia pomonella (L.) (Lep., Tortricidae), by concentrated formulations of microencapsulated pheromone in flight tunnel assaysJOURNAL OF APPLIED ENTOMOLOGY, Issue 9-10 2005L. L. Stelinski Abstract:, The effects of two formulations of microencapsulated pheromone (CheckMate CM-F), containing 14.3% (E,E)-8,10-dodecadien-1-ol (codlemone), on the behaviour of the male codling moth, Cydia pomonella (L.), were evaluated in a flight tunnel after several periods of formulation ageing. The two treatments of CheckMate CM-F evaluated consisted of the label-recommended field rate of 50 g active ingredient (a.i.)/ha diluted in: (1) a standard 1000 l of water (low concentration 0.05 g/l), and (2) a low volume of 100 l of water (high concentration 0.5 g/l). The low-concentration treatment was formulated by diluting 0.071 ml of CheckMate CM-F in 500 ml of water and the high-concentration treatment contained 0.71 ml of CheckMate CM-F in 500 ml of water. Wax-paper strips (2.1 × 20 cm) were treated at 0.06 ml of solution/cm2. The mean (±SE) number of CheckMate CM-F microcapsules adhering to treated wax-paper strips in the high-concentration treatment (398 ± 38) was sevenfold greater than that (57 ± 5) counted on wax-paper strips treated with the low concentration. Both low- and high-concentration treatments prevented anemotactic orientation of male codling to an adjacent 0.1 mg codlemone lure for up to 24 h after application. These moths flew out of the release cages, but exhibited erratic and short flights not restricted to any plume and ending at the tunnel walls or the floor. This occurred with approximately 60 and 400 microcapsules per wax-paper strip in the low- and high-concentration treatments, releasing codlemone at approximately 0.15 and 1.5 ,g/h respectively. After 2 days of ageing, the low-concentration treatment no longer interfered with the ability of males to find the codlemone lure. However, the number of males contacting the lure was significantly reduced for up to 6 days with the high-concentration treatment relative to the control and low-concentration treatments. The high-concentration treatment no longer impeded normal orientational flight after 2,6 days of ageing; but, it diverted males from the codlemone lure by causing them to land on the adjacent treated wax-paper strips. This occurred at a release rate of approximately 0.7 ,g codlemone/h from approximately 400 microcapsules per wax-paper strip distributed as clumps of approximately 30 microcapsules per 14 mm2. We suggest that an initial but short-lived disruption mechanism like camouflage is followed by a longer period of false-plume following to clumps of microcapsules. The low-volume, concentrated application method for disseminating pheromone microcapsules warrants further investigation for moth codling, as well as other pests because this approach may improve the efficacy without the need for increasing the field application rate. [source] Effect of triflumuron on brood development and colony survival of free-flying honeybee, Apis mellifera L.JOURNAL OF APPLIED ENTOMOLOGY, Issue 4 2004O. G. Amir Abstract:, The effect of the insect growth regulator (IGR) triflumuron (Alsystin® 25 WP) on honeybee, Apis mellifera L. (Hym., Apidae), was studied in a semi-field test. Free-living colonies were fed one litre per hive of sucrose syrup containing 0, 0.025, 0.25 or 2.5 g of triflumuron. A significant reduction in flight activity was noted 6,10 weeks post-treatment at the two higher doses. These colonies reared less brood than before treatment. While the comb area occupied by uncapped brood was as high as [0.025 and 0.25 g active ingredient (a.i.)] or higher (2.5 g a.i.) than before treatment, there was a significant decline in capped brood at the two higher doses, indicating enhanced larval mortality. No capped brood was reared in the hive treated at the highest dose from 3,9 weeks post-treatment. Yet there was a significant accumulation of pollen and honey in the brood compartment at all doses. All colonies except the one treated at the highest dose survived the following winter. However, at 43 weeks post-treatment, hives treated at intermediate and low doses showed a significant increase in uncapped brood and a significant decrease in capped brood. This study revealed a strong residual toxicity of triflumuron to brood and substantiated its classification as hazardous to honeybee. [source] Do bacteria need to be regulated?JOURNAL OF APPLIED MICROBIOLOGY, Issue 3 2006P. Silley Abstract Additives for use in animal nutrition are regulated under Regulation (EC) No. 1831/2003. The scope of this paper addresses the specific microbiological issues relevant to a microbial feed additive, containing a Bacillus spp. and uses as an example a product with the trade name, Calsporin®. Bacillus subtilis C-3102 is the active ingredient in Calsporin® and is added to animal feed to favourably affect animal production and performance (growth and feed efficiency), by modulating the gastrointestinal flora. It is not the purpose of this review to present the raw data for Calsporin® but rather to use Calsporin® as an example of the type of data required by the European regulatory authorities. At the time of preparation of this manuscript Calsporin® has yet to be reviewed by the authorities. The regulatory system under the auspices of the EFSA FEEDAP Panel is clearly attempting to move in line with development of scientific opinion and is to be applauded for such efforts. Bacteria do need to be regulated, and the regulations clearly provide adequate and appropriate protection to human health and to environmental considerations. [source] Inhibition of human cytochrome p450 1b1 further clarifies its role in the activation of dibenzo[a,l]pyrene in cells in cultureJOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGY, Issue 3 2007Brinda Mahadevan Abstract Metabolic activation and DNA adduct formation of the carcinogenic aromatic hydrocarbon dibenzo{a,l}pyrene (DBP) was investigated in human mammary carcinoma MCF-7 cells and human cytochrome P450 (CYP) 1B1-expressing Chinese hamster V79 cells in culture. It has been shown that DBP is metabolically activated to DNA-binding diol epoxides both in vitro and in vivo. To further establish the role of human CYP1B1 in the activation of DBP, both cell lines were cotreated with DBP and a selective chemical inhibitor of CYP1B1, 2,4,3, ,5,-tetramethoxy-stilbene (TMS). Results from DBP,DNA adduct analyses revealed the complete inhibition of DNA binding when cells were cotreated with DBP and TMS in comparison to DBP alone. Inactivation of CYP1B1 by TMS was also demonstrated through a decrease in the 7-ethoxyresorufin O -deethylase (EROD) activity in microsomes isolated from these cells. Emodin, 3-methyl-1,6,8-trihydroxyanthraquinone, an active ingredient of an herb, has been recently shown of being able to induce CYP1 gene expression. Examination of human CYP1B1 induction and EROD activity confirmed an increase in protein levels upon cotreatment with emodin and DBP. Despite increases in protein levels and enzyme activity, there was no significant change in DBP,DNA binding levels at very low substrate concentrations (17 nM). The data obtained in this study emphasize the central role of CYP1B1 in the activation of DBP in human cells in culture. © 2007 Wiley Periodicals, Inc. J Biochem Mol Toxicol 21:101,109, 2007; Published online in Wiley InterScience (www.interscience.wiley.com). DOI 10.1002/jbt.20168 [source] Efficacy of Listerine® Antiseptic in reducing viral contamination of salivaJOURNAL OF CLINICAL PERIODONTOLOGY, Issue 4 2005Timothy F. Meiller Abstract Aim: The anti-viral efficacy of oral antimicrobial rinses has not been adequately studied in terms of potential clinical significance. As a follow-up to an in vitro study on the effect of oral antiseptics on Herpes simplex virus, Type 1, this study was undertaken to evaluate the in vivo effect of an essential oil containing oral antiseptic on the reduction of viral titer in saliva during active viral infection. Method: Patients were recruited and evaluated in a single visit protocol at the onset of a perioral outbreak, consistent historically and clinically with recurrent Herpes labialis. Direct immunofluorescence of cytological smears of the lesions/oral fluids was used to confirm Herpes simplex virus types I or II. Patients were randomly assigned to one of two treatment groups: (1) active ingredient and (2) sterile water control. The viral lesion was evaluated as to clinical stage according to standard protocol. Salivary fluid samples were taken: (1) at baseline; (2) immediately following a 30 s rinse; (3) 30 min. after the 30 s rinse; and (4) on the repeat trial, also at 60 min. after the 30 s rinse. All samples were evaluated for viral titer and results compared. Results: In Trial 1, the sample population consisted of 19 males and 21 females with an average age of 29.2 and in Trial 2, 21 males, 19 females with an average age of 28. In both Trials 1 and 2, recoverable infectious virions were reduced to zero after a 30 s experimental rinse; whereas, the control rinse resulted in a non-significant (p>0.05) reduction. The experimental group also demonstrated a continued significant (p<0.05) reduction 30 min. post rinse when compared with baseline while the control group returned to baseline levels. In Trial 2, the 60 min. post rinse follow-up demonstrated a 1,2 log residual reduction from baseline in the experimental group; however, this was not significant. Conclusions: There is clinical efficacy in utilizing an oral rinse with the antimicrobial agent Listerine® Antiseptic in reducing the presence of viral contamination in oral fluids for at least 30 min. after oral rinse. The risk of viral cross contamination generated from these oral fluids in person to person contact or during dental treatment may be reduced. [source] Evaluation of diquat against an acute experimental infection of Flavobacterium columnare in channel catfish, Ictalurus punctatus (Rafinesque)JOURNAL OF FISH DISEASES, Issue 5 2009A M Darwish Abstract A trial was performed to evaluate the efficacy of diquat (6,7-dihydrodipyrido[1,2-a:2,,1,-c]pyrazinediium dibromide) against an acute experimental infection of Flavobacterium columnare in channel catfish, Ictalurus punctatus. Diquat is an Environmental Protection Agency-approved herbicide and has the potential to be legally and practically used against columnaris. Channel catfish were challenged, by cutaneous abrasion, and waterborne exposure to F. columnare and treated once at 22-h post-challenge with 2.5, 5.0, 10.0 and 15 mg L,1 of diquat active ingredient for 6 h. At the conclusion of the trial, 21-day post-challenge, diquat at 5.0, 10.0 and 15 mg L,1 significantly (P < 0.05) reduced the mortality of infected fish from 95% in the challenged non-treated fish to 68%, 59% and 49%, respectively. In vitro, the minimum inhibitory concentration (MIC) of 23 isolates of F. columnare was assayed. The majority of the isolates had an MIC value of 5 ,g mL,1 (15 of the 23 isolates). Infected fish exhibited acute clinical signs similar to a natural infection. The skin had severe ulcerative necrotizing dermatitis and the muscles had severe necrotizing myositis. The gills had severe multifocal necrotizing branchitis. The results demonstrate that diquat would reduce mortalities caused by an acute columnaris infection. [source] Synergistic antioxidative activities of hydroxycinnamoyl-peptidesJOURNAL OF PEPTIDE SCIENCE, Issue 10 2009Seon-Yeong Kwak Abstract Antioxidants have become an important subject of study as an active ingredient for cosmetics and preservatives for food. We synthesized antioxidative peptide conjugates of hydroxycinnamic acids (HCAs) such as ferulic acid (FA), caffeic acid (CA), and sinapic acid (SA) by SPPS method. We measured their potential antioxidant properties by 2,2-diphenyl-1-picrylhydrazyl radical (DPPH) scavenging test and lipid autoxidation inhibition test. When the antioxidative peptides, such as glutathione analogue (GS(Bzl)H) and carnosine (CAR), were conjugated to HCAs, their antioxidative activities were enhanced significantly. CA-peptides exhibited the highest free radical scavenging activity by the DPPH test, and showed good antioxidative activity in the lipid autoxidation test. FA- and SA-peptides showed excellent antioxidative activity in the lipid autoxidation test. Furthermore, we demonstrated a synergistic antioxidative activity of HCA-peptide conjugates by comparing their antioxidative activity with that of a simple mixture of HCAs and the antioxidant peptides. Copyright © 2009 European Peptide Society and John Wiley & Sons, Ltd. [source] Assessment of diffuse transmission mode in near-infrared quantification,part I: The press effect on low-dose pharmaceutical tabletsJOURNAL OF PHARMACEUTICAL SCIENCES, Issue 12 2009M. Saeed Abstract Quantitative applications for pharmaceutical solid dosage forms using near-infrared (NIR) spectroscopy are central to process analytical technology (PAT) manufacturing designs. A series of studies were conducted to evaluate the use of NIR transmission mode under various pharmaceutical settings. The spectral variability in relation to tablet physical parameters were investigated using placebo tablets with different thickness and porosity steps and both variables showed an exponential relationship with the detected transmittance signal drop. The drug content of 2.5% m/m folic acid tablets produced under extremely different compaction conditions was predicted and found to agree with UV assay results after inclusion of extreme physical outliers to the training sets. NIR transmission was also shown to traverse a wide section of the tablet by comparing relative blocking intensities from different regions of the tablet surface and >90% of the signal was detected through a central area of 7 mm diameters of the tablet surface. NIR Quantification of both film thickness and active ingredient for film-coated tablets are examined in part II of this study. © 2009 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 98:4877,4886, 2009 [source] Design and evaluation of a dry coated drug delivery system with floating,pulsatile releaseJOURNAL OF PHARMACEUTICAL SCIENCES, Issue 1 2008Hao Zou Abstract The objective of this work was to develop and evaluate a floating,pulsatile drug delivery system intended for chronopharmacotherapy. Floating,pulsatile concept was applied to increase the gastric residence of the dosage form having lag phase followed by a burst release. To overcome limitations of various approaches for imparting buoyancy, we generated the system which consisted of three different parts, a core tablet, containing the active ingredient, an erodible outer shell and a top cover buoyant layer. The dry coated tablet consists in a drug-containing core, coated by a hydrophilic erodible polymer which is responsible for a lag phase in the onset of pulsatile release. The buoyant layer, prepared with Methocel® K4M, Carbopol® 934P and sodium bicarbonate, provides buoyancy to increase the retention of the oral dosage form in the stomach. The effect of the hydrophilic erodible polymer characteristics on the lag time and drug release was investigated. Developed formulations were evaluated for their buoyancy, dissolution and pharmacokinetic, as well gamma-scintigraphically. The results showed that a certain lag time before the drug released generally due to the erosion of the dry coated layer. Floating time was controlled by the quantity and composition of the buoyant layer. Both pharmacokinetic and gamma-scintigraphic data point out the capability of the system of prolonged residence of the tablets in the stomach and releasing drugs after a programmed lag time. © 2007 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 97:263,273, 2008 [source] | |||||||||||||||||||||||||||||||||||||