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    • 专利摘要:
    SUMMARY An ectoparasiticidal composition is provided comprising a mixture of a carrier and an active moiety with an emulsifier. The bar comprises low viscosity non-volatile siloxane and the active moiety comprises a high viscosity non-volatile siloxane. The low viscosity siloxane and the high viscosity siloxane both have a flash point of at least 100 ° C when closed. Preferably, both the low viscosity siloxane and the high viscosity siloxane comprise a dimethicone or a dimethiconol or a mixture thereof, of which the low viscosity siloxane has a viscosity of the order of 5 to 1000 centistokes and the high viscosity siloxane has a viscosity of at least 1000 centistokes.
    公开号:SE537567C2
    申请号:SE1100883
    申请日:2010-05-12
    公开日:2015-06-16
    发明作者:Nigel Cooper
    申请人:Thornton & Ross Ltd；
    IPC主号:
    专利说明:

    The present invention relates to ectoparasiticidal additives and a method for controlling ectoparasites, in particular head lice and their agg.
    Compositions for controlling ectoparasites, especially head lice, have traditionally included conventional insecticides. However, many of these substances have an unpleasant odor and can cause allergic reactions. Recently, non-toxic products have been identified as being clinically effective. Particularly some silicone polymers, which are commonly found in personal care products, such as shampoos and conditioners, have been found to be very effective in eradicating both headaches and their aggregates when used in certain formulations.
    US4146619 discloses the use of linear alkyl or arylsiloxane polymers having a viscosity of less than about 20,000 centistokes for use as a pediculicide and / or ovicide. Such polymers are safe to use. however, it has later been found that compositions comprising siloxane polymers having viscosities in excess of 20,000 centistokes are clinically more effective.
    US6683065 discloses a composition for use as a pediculicide consisting of at least 40% of the polydimethylsiloxane in which the surface loading of the composition is below about 25 dynes / centimeter at 20 ° C and the viscosity of the composition is Over 200 centistokes at 20 ° C. This composition utilizes the effectiveness of dimethicones, but the high specified viscosity does not allow penetration of the composition through and over the surfaces of the hair. In addition, siloxanes with such high viscosity have been found to be responsible for washing out the hair after use with satisfactory results. This Or them answer and unpleasant to use.
    In contrast, EP1215965 discloses the use of a composition comprising at least one siloxane derivative as active ingredient, other than only one lin * alkyl or arylsiloxane having a viscosity of less than 20,000 centistokes, for controlling ectoparasites and, in particular, pediculous infestations. In particular, this patent discloses the use of head loss control compositions comprising a mixture of a volatile siloxane, such as a cyclomethicone, and a non-volatile siloxane, such as a dimethicone. During use, when the composition is applied to the hair, the volatile siloxane acts to disperse the non-volatile siloxane over the hair and the hair and then evaporates and leaves the non-volatile siloxane as an active deposit which bulges the hair and any loose and resentments present. A disadvantage of this product is that it has limited efficiency against the dgg of the head pilot. However, the main disadvantage of this composition and with other ectoparasiticidal compositions including volatile siloxanes, such as cyclomethicone, is that they are flammable or flammable and are therefore a fire hazard.
    It will again be appreciated that there is no absolute definition of the term "volatile" but in a scientific context it is a measure of the substance's tendency to want to evaporate. The term is most often used to describe a liquid's tendency to evaporate. One way to quantify data is to determine the heat of vaporization of a sink, which is the energy required to vaporize a given mass of liquid at a given temperature. At 25 ° C the heat of formation of water is 2257 kJ / kg while that of ethanol is 840 kJ / kg. In contrast, the heat of formation of cyclomethicones in the range is 157 kJ / kg, which makes them very volatile to the man as they do not show any cooling effect on the skin. It will be appreciated that in general it is said that the lower the heat of formation, the lower the flash point.
    It will be seen that viscosity can be expressed as absolute viscosity, as fed in poises or centipoises, or as kinematic viscosity. Kinematic viscosity is the ratio of a barar's absolute viscosity to density and is determined in stokes or centistokes. To underline this, viscosity will be expressed in centistokes savida unless otherwise indicated. The density of a bar substance is close to 1, as is the case with dimethicones which typically have specific gravities between 0.96 and 0.98 have absolute and kinematic viscosity almost the same numerical value.
    WO 2007104345 also describes a composition Mr to combat ectoparasites, in particular head lice and their agg, the purpose of which is to avoid the use of cyclic 2 siloxanes which are considered to be potentially harmful. The composition described comprises a mixture of a line of low viscosity polysiloxane having a viscosity of less than 10 centistokes, a line of higher viscosity polysiloxane having a viscosity exceeding 90 centistokes, and at least one dispersant. In particular, the low viscosity polysiloxane is preferably dimethicone having a viscosity of 1 centistoke and the higher viscosity polysiloxane is preferably dimethicone having a viscosity of 100 centistokes. Dimethicones with a viscosity of around 1 centistoke carried a flash point of the order of 57 ° C and are volatile and therefore flammable. It will be appreciated that in its preferred embodiment, this composition is also flammable or combustible.
    In view of the foregoing, it will be appreciated that it is of the utmost importance for the recipient being treated to stay away from open flames, light cigarettes and the like when flammable or combustible products are used. Therefore, customers should be restrictive in using such products on children.
    Other commercially available pediculicidal products also suffer from the same disadvantages as those described above. Some include mixtures of alcohols with siloxanes and are flammable or flammable, while others use dimethicones that do not spread well and are responsible for rinsing off after use. It will be appreciated that a general compromise must be reached; either the same composition comprises non-volatile siloxanes and is responsive to rinsing or it comprises a large proportion of volatile siloxanes which make the whole composition flammable or flammable and dart & dangerous.
    It is an object of the present invention to provide an ectoparasiticidal composition which overcomes or substantially reduces the problems associated with flammability and at the same time provides an ectoparasiticidal composition which can be rinsed from the hair and removed from the skin after use with conventional shampoos and conditioners.
    The terms "flammable liquid" and "flammable liquid" are often used interchangeably to refer to water shoes that can actually catch fire. However, the terms "flammable" and "flammable" are used to refer to the exact definitions given to them by the National Fire Protection Association (NFPA), an international electoral body in the field of fire safety. These definitions are also used by US authorities, especially the US Department of Transportation, the US Environmental Protection Agency, the US Occupational Safety and Health Administration and others. These bodies use the term "flammable" for a liquid having a flash point below 100 ° F (37.8 ° C) and the term "flammable" for less flammable liquids having a flash point between 100 ° F (37.8 ° C) and 200 ° F (93.3 ° C). The flash point of a liquid is the lowest temperature at which it can form a flammable mixture in air. At this temperature, the angoma may cease to burn when the ignition source is removed. A slightly higher temperature, the flash point, is defined as the temperature at which the steam continues to burn after it is ignited. None of these parameters have anything to do with the ignition temperature of the cold or of the burning liquid, which is much higher.
    There are two basic types of flash point feeds: open cup (open cup) and closed cup (closed cup). Closed baking tests normally give a lower value at the flash point than open baking tests and are a better approximation to the temperature at which the pressure reaches a lower flammable limit. Therefore, in the appended claims, the term flash point is to be understood as being obtained by a Pensky-Martens closed baking method for which there are many international standards.
    The applicant has found that the use of a low viscosity non-volatile siloxane acts to disperse a high viscosity non-volatile siloxane and that the evaporation of the low viscosity siloxane is not required for the efficiency of the product.
    Therefore, according to a first aspect of the bile invention, there is provided an ectoparasiticidal composition comprising a mixture of a carrier and an active moiety with an emulsifier, the barrier comprising a low viscosity non-volatile siloxane and the active moiety comprising a high volatile siloxane viscosity, both the low viscosity siloxane and the high viscosity siloxane have a flash point of at least 100 ° C during a closed baking test. A flash point of at least 100 ° C means that the siloxane in question will not again form an antiridable mixture in air during normal use of the composition.
    Siloxanes can be either linear or cyclic. Non-volatile siloxanes are usually linear. Preferably, the low viscosity siloxanes and the high viscosity siloxanes comprise a dimethicone or a dimethiconol or a mixture thereof.
    Dimethicones are linear siloxanes of the general formula (C2H60Si). They are also 10 Uri & as polydimethylsiloxane (PDMS) and have recently been called idimethicone. They are viscoelastic and their viscosity relates to their molecular weight.
    Preferably, the low viscosity siloxane has a viscosity in the order of 10 to 1000 centistokes and the high viscosity siloxane has a viscosity of at least 1000 centistokes. More advantageously, low viscosity siloxanes have a viscosity of the order of up to 100 centistokes and siloxanes of the high viscosity have a viscosity of the order of 50,000 to 200,000 centistokes.
    Dimethicones with a viscosity of 10 centistokes having a steady state flash point of 211 ° C are available. Dimethicones with viscosities less than 10 centistokes which have a steady-state baking flash point higher than 200 ° C are currently not commercially available. Dimethicones with viscosities above 50,000 centistokes may have a closed baking flash point exceeding 300 ° C. The use of these dimethicones in a composition according to the invention means that the composition does not comprise a flammable or flammable liquid and therefore does not pose a health risk to the user. In particular, it is highly unlikely that the composition would allow a self-sufficient fire to arise in the hair or on the body when used if it is brought to change an Open Law. This composition of the invention is much safer to use compared to those used today and it is especially useful in children and infants.
    The composition preferably comprises at least 0.1% of the high viscosity non-volatile siloxane and may comprise up to 50%, but the actual proportion used depends on its viscosity. Preferably, the composition itself has a viscosity in excess of 30 centistokes so that it adheres to the ectoparasites and their aggregates. In general, the higher the viscosity of the siloxane with the high viscosity used, the lower the volume fraction required in the composition, otherwise the composition of the viscose to be used is satisfactory. In a composition comprising a high viscosity siloxane having a viscosity in the order of 50,000 to 200,000 centistokes, then only about 4% by volume of the composition need be high viscosity siloxane.
    In some formulations of the invention, a viscosity modifier may be added to the base composition to facilitate attachment to the ectoparasites and their dgg. Such a viscosity modifier preferably comprises a thixotropic additive to prepare the composition when used. It can also stabilize the composition if some physically incompatible materials are added, for example hydrophobic silicone derivatives.
    Lamp viscosity modifiers are known to those skilled in the art. One such is an additive in the form of nanoparticles consisting of silicon dioxide with a size of between 7 nm and 40 nm. Preferably, the composition comprises at least 0.1 and up to 0.5% by volume of the additive.
    In some already known compositions, dispersants are used to aid in the dispersibility of the composition Over skin and have. These dispersants reduce the surface tension of the composition. In bile invention, however, no dispersant is needed as siloxanes having a surface spar that eliminates their use can be used. More advantageously, the dad & siloxanes in the composition have a surface tension of the order of 20 mN / m.
    Preferably, the emulsifier comprises a copolymer of silicone. More advantageously, the composition comprises at least 1% and preferably between 1 and 10% by volume of an emulsifier comprising a copolymer of dimethicone, for example a 40% solution of a copolymer of dimethicone dissolved in cyclopentasiloxane. Such agents are already commercially available and are known to those skilled in the art as they are widely used in personal hygiene products such as antiperspirants, cosmetics, shampoos and hair conditioners. They act as stabilizing water-in-oil emulsifiers and provide scrubbing qualities which are high for a composition according to the golden invention and Mita for washing away skin and hair and for which it is more convenient to use. While the emulsifier itself may have a flash point of less than 200 ° C, the small amount of emulsifier needed in the composition does not affect its overall flammability.
    While mixtures of siloxanes are extremely effective in killing lice and fleas, their dgg is more likely to kill and they can survive and cause re-infection after treatment.
    Preferably, the composition is modified to improve its effectiveness against agg. Such a composition would have an enormous advantage that the number of treatments needed to treat a lice infestation could be reduced considerably, especially in the most effective compositions with a single treatment.
    Applicants have found that by adding a terpene or a phenylpropanoid derivative to siloxane compositions, without the presence of inherent insecticidal properties, the surface physicochemical properties of the composition are improved and a degree of hydrophilicity is added to the entire composition. This improves the penetrating properties of the composition and allows the siloxane with the high viscosity to penetrate the airflow air of the agen out over the spirals of the insects, thereby improving the overall efficiency of the composition as a whole.
    Preferably, therefore, the composition comprises an essential oil or essential oils.
    Preferably, the composition also comprises at least 0.1% by volume of the essential oil and may comprise up to 2% by volume of the essential oil. More advantageously, the essential oil or oils comprise one or more terpenes, in particular the essential oil comprises nerolidol. In a second aspect, the bile invention provides the use of a composition in a method of treatment or for the purpose of prevention of a human or animal in which the composition is a mixture of a carrier and an active moiety with an emulsifier, the carrier comprising a non-volatile the low viscosity siloxane and the active moiety comprise a high viscosity non-volatile siloxane, both the low viscosity siloxane and the high viscosity siloxane have a flash point with a closed baker of at least 100 ° C.
    In a third aspect, the bile invention provides a method of controlling an ectoparasitic attack which comprises applying a composition consisting of a mixture of a carrier and an active moiety with an emulsifier, to said ectoparasite or its agg, the carrier comprising a non-volatile siloxane low viscosity and the active moiety comprises a high viscosity non-volatile siloxane, both the low viscosity siloxane and the high viscosity siloxane had a flash point with a closed baker of at least 100 ° C.
    Two examples of preparations of an ectoparasiticidal composition according to the present invention.
    Example 1 4% by volume of a dimethicone with a viscosity of 50,000 centistokes; between 1 and 4% by volume of an emulsifier comprising a copolymer of dimethicone; up to 2% by volume of nerolidol; an equilibrium of a dimethicone with a viscosity of between 10 and 100 centistokes.
    Example 2 1. 4% by volume of a dimethicone having a viscosity of 100,000 centistokes; between 1 and 4% by volume of an emulsifier comprising a copolymer of dimethicone; up to 2% by volume of nerolidol; up to 0.5% by volume of nanosize silicon dioxide particles; and 5. an equilibrium of a dimethicone having a viscosity of between 10 and 100 centistokes. In particular, ectoparasiticidal compositions according to the present invention have been developed which can be handled by special users as liquid gel preparations for application by holding the hair and as sprays or preparations for spraying on the hair with a pump-activated spray syringe.
    Separate examples of these preparations are as follows.
    Liquid gel formulation 1. 4% by volume of a dimethicone with a viscosity of 100,000 centistokes; 2. 2% by volume of a copolymer of dimethicone; 2% by volume of nerolidol; 0.5% by volume of nanosized silicon dioxide particles; and 91.5% the remainder of dimethicone with a viscosity of 50 centistokes.
    Spray gel formulation 4% by volume of a dimethicone with a viscosity of 100,000 centistokes; 2% by volume of a copolymer of dimethicone; 2% by volume of nerolidol; 0.5% by volume of nanosized silicon dioxide particles; and 5. 91.5% the remainder of a dimethicone with a viscosity of 10 centistokes.
    It will be appreciated that the only difference between these formulations is the viscosity of the dimethicone carrier, which in the spray gel formulation has a lower viscosity to facilitate application with a pump-activated spray syringe.
    When used for the treatment of head loss, the composition should be applied to dry hair and the hair should be belted from root to tip. The composition must then be left in place for at least one hour.
    Both examples proved to be very effective in the treatment of head loss and show 100% lice death within usually a few seconds of contact and 100% aggdod after one hour. After one hour, the composition can be thoroughly washed off with shampoo. The 9 dead lice are washed out at the same time and can also be easily combed out. All dead dgg or gnetar, which are empty aggholjen, can also be removed with the fingers or a fine-toothed comb. The treatment of other ectoparasites, such as fleas in animals, can be performed in the same way.
    The following research illustrates the invention.
    Experiment 1 This experiment compared the efficacy against head loss with a conventional siloxane-based product described in EP1215965 and comprising a mixture of 96.7% cyclopentasiloxane v / v and 3.3% dimethiconol v / v with a viscosity of less than 20%. 000 centistokes (Preparation A) and by the spray gel preparation described above (Preparation B) Materials and Methods Insects used in the experiments Head lice, Pediculus capitis, are obtained from volunteers from society. This resulted in the release used in the experiment being obtained from different sources. All samples were examined once daily during the course of the experiments. For each test performed on the same day, all detachments were obtained from the same individual patient, so there was an internal agreement with a batch of sample replicates. Since only one replicate trial is challenged by each preparation each day, there could have been some variation between the trials challenged on different days. However, this would have represented the normal variation of head loss that is likely to occur in society and each response response would be representative of the response variation that is likely to occur in consumers.
    Loss is collected using a plastic lice comb and transported to the laboratory within 2 hours. The pilot is included in batches such as Ors with boxes of gas dv, as a substrate to stand on, and each batch is assigned a market 55 mm Petri shell in plastic.
    For the experimental procedure, an aliquot of about 5-10 ml of a suitable preparation is poured into the bottom of a pure 55 mm plastic petri dish. The gas web carrying the unloader sank into the water tank for 10 seconds, at the same time as the gas web was turned at least twice to ensure the removal of air bubbles. After removing the liquid, the gauze is wiped and the insect is easily removed to remove excess liquid and salt back to a 5.5 mm filter paper in their marked petri dish. The same procedure is repeated for the other replicate gauze squares in that batch.
    The gauze boxes carrying the unloader are then incubated under normal maintenance conditions (0 ± 2 ° Celsius and 50% ± 15% relative humidity) for the remaining test period. At the end of the exposure period, the insects and gauze are washed with a mixed shampoo diluted with one shampoo and fourteen parts water (FWS 1:15) after which they are rinsed off by using 500 ml of warm (35 ° Celsius) tap water through and over the gas gauze windows. . They were wiped dry with medical wiping paper and incubated under normal maintenance conditions in clean petri dishes of plastic of suitable size until the results were documented.
    Results Activity against adult losers "Immobile" losers show no signs of movement.
    "Stagnant" describes looseness that maintains some mobility during the time as the pang-sans. Such movements can vary from complete physical immobility, with only slight abdominal movements noticeable, through minor twitches in the extremities, antennae or other appendages, for insects that have almost the ability to crawl but lack sufficient coordination so that they are not considered capable of surviving. LOs in the bare mortality category are generally classified as no longer living.
    "Living" describes loose that seems to go normally and should be expected, with the possibility of being fed, of being able to continue life in a normal way.
    The trials are challenged by using a lice replicate for the trial preparations and a lice replicate for the control. The experiments are challenged ex vivo, with an application time of 1 hour, 11 for all preparations and controls. The purpose of these rapids was to show the effectiveness of the three products tested against 18ss in the field.
    The test results are shown in Table 1 below. The effectiveness of the preparations is shown after a ten second dip and then an immediate dewatering and a further set of trials is shown with a ten minute application and then dewatering. These attempts are to show whether Wagon of the formulations have an immediate effect on the loss, and whether a ten-minute application is successful in immobilizing the loss.
    Table 1 Results 1 hour after dewatering Preparation Exposure Anxious Abnormal living Total Mortality% A minutes 14 0 0 14 100% B minutes 13 0 0 13 100% A 10 second dip / dewatering 0 0 100% B 10 second dip / dewatering 0 0 100% Control 1 hour 0 0 0% Results 2 hours after dehydration Preparation Exposure Immobile Abnormal live Total Mortality% A minutes 14 0 0 14 100% B minutes 13 0 0 13 100% A 10 second dip / dewatering 0 0 100% B second dip / dewatering 0 0 100% Control 1 hour 0 0 0% 12 Results 3 hours after dewatering Preparation Exposure Immobile Abnormal living Total Mortality% A minutes 14 0 0 14 100% B minutes 13 0 0 13 100% A second dip / dewatering 0 0 100% B second dip / dewatering 0 0 100% Control 1 hour 1 0 14 0% Results 17 hours after dewatering Preparation Exposure Diida Abnormal living Total Diability% B minutes 13 0 0 13 100% A 10 second dip / dewatering 0 0 100% B second dip / dewatering 0 0 100% Control 1 hour These experiments show that the composition of the biliary invention is successful in directly immobilizing immediately after both exposure times.
    Experiment 2 This compares the efficacy against head loosening of the liquid gel formulation and the spray gel formulation, both described above, at two different exposure times. The two preparations were tested with exposure times of 15 minutes and pH 30 minutes.
    Materials and Methods Insects Used in Experiments 13 Lice saws are obtained by providing actively laying adults loose on a small-mesh nylon gauze as an egg-laying substrate over a 48 hour period. After removal of the unloading, each large piece of gauze was cut into a series of smaller pieces of larval size and holding an appropriate number of aggregates. These panes were distributed on a random basis to marked 90 mm plastic petri dishes.
    For the experiment, an aliquot of about 5 ml of suitable liquid was taken and halided at the bottom of a 30 mm plastic petri dish. The gauze carrying the agge was dipped in the liquid for 10 seconds, the gauze being watered at least twice during the time to ensure the removal of air bubbles.
    After removal from the liquid, the gauze and the agar were lightly dried to remove any excess and returned to their marked petri dish. The same procedure was repeated for the other test products and the water control.
    The gauze squares bearing the agate were incubated under normal maintenance conditions (30 ° ± 2 ° Celsius and 50% ± 15% relative humidity) for the remaining period of the test period, during which the gauze was washed three times with 250 ml of warm (34 ° Celsius) tap water through and through. Over the gauze quadrants at the end. They were then wiped dry with medical wipes and incubated under normal maintenance conditions in clean, suitable plastic petri dishes until the results were documented. The test results against agg were documented after all control kits had completed the clacking, approximately 12 days later.
    Results Activity against eggs The activity of the treatment against lice requires classification of the effect according to the degree of penetration of the insecticide.
    "Heel" describes lice eggs in which the embryo inside develops normally and heel normally.
    "Half-heel" describes the eggs in which the lice die during the removal process so that it may only be able to lift the egg shell, or otherwise die partially out of the shell. 14 "YOU" describes the eggs in which the embryo appears to have completed its development but has not emerged from the eggshell. The young lice die or cloths before the removal process before lifting the lid from the eggshell.
    "Undeveloped" is a description used for all the agg that do not develop normally or not at all. This can be identified because at the time of the experiment, the young embryos appear amorphous inside the transparent eggshell. When the developing embryo is approximately 48 hours old, it begins to develop a small pigmented flake at the end of the eggshell.
    The flake will often develop into the lice's eye and be referred to as the lice's "Ogonflack". In some cases, the embryo develops only to the point that shows an uneven flake, but in these cases the flake is deformed or may even be in the wrong spirit of the egg oil. All such cases are classified as "Undeveloped".
    The results of the experiments are shown in Table 2.
    Table 2 Preparation Exposure time Total Heel Semi-heeled Killed Undeveloped Mortality Liquid gel 30 minutes 153 0 0 1 152 100% Spray gel 30 minutes 177 0 0 0 177 100% Liquid gel 15 minutes 10 0 14 116 100% Spray gel 15 minutes 136 0 0 0 136 100 % These results clearly show the effectiveness of both preparations against lice ashes at the different exposure times. Bathing produced 100% mortality with 15 and 30 minutes exposure time.
    The above experimental data will be shown above from the aforementioned liquid gel and spray gel formulations which have been found to exhibit 100% lice death on contact, usually within ten to fifteen seconds, and 100% agglomerate after as little as fifteen minutes. This is a dramatic improvement over kanda preparations that use siloxanes. WO2007 / 104345 discloses a composition comprising a mixture of a volatile dimethicone having a viscosity of less than 10 centistokes and a dimethicone having a viscosity of stone at 90 centistokes. However, by using the same procedure as described above in Experiment 2, this composition produces 82% aggdod during one hour of contact time.
    WO2010 / 018360 describes a siloxane preparation containing nerolidol which has the most effective exposure time for aggdOd overnight even if a four hour exposure period produced high levels of efficiency of 92.85% compared to overnight exposure which was 94.97%. In normal cases, darts & the line for users of such preparations to perform two one-hour treatments, with a week in between. The overriding unit in the bile invention, however, is that a cure is completed after a single hour of treatment. In fact, experimental data indicate that an effective treatment time of only around 15 minutes is needed.
    HuvudlOss in humans has a unique strategy of water management. They do not produce urine, but eliminate excess water through respiratory transpiration via the trachea and spiracles. Blockage of the spiracles counteracts or reduces water excretion, which often leads to clods causing the bowel to rupture.
    L6ss treated with the liquid gel preparation described above were scanned in a scanning electron microscope with X-ray spectroscopy and the chemical elements found in and around the LOss spirals were determined by cutting off the surrounding tissue using a focused ion beam and X-ray microanalysis. The result is shown in the accompanying drawings in which Fig. 1 is a photograph of an image produced by scanning electron microscope of a spiral of a head lice frail human after treatment with the liquid gel preparation described above; Fig. 2 is an X-ray spectrogram of the highlighted area of Fig. 1; Fig. 3 is a photograph of an image produced with a scanning electron microscope of a spiral in incision of a human head lice after treatment with the liquid gel preparation described above; and Fig. 4 is an X-ray spectrogram of the marked area in Fig. 3.
    X-ray analysis showed silicone present over the entire surface of a treated lice; silicone firms in dimethicone but not in lOss. As shown in Fig. 1, the silicone had formed a plug or a thin bulge on the inside of the spirals of the treated lice. Ion beam scanning in the scanning electron microscope created a scanning section of an abdominal spiral as shown in Fig. 3. X-ray spectral analysis shown in Figures 2 and 4 of the marked surfaces in Figures 1 and 3 showing the distribution of silicone from the dimethicone, respectively.
    It is an edge of ectoparasiticidal preparations containing siloxanes acting by blocking the spirals of the lice and thereby preventing water loss. Compositions of the bile invention operate by the same mechanism. However, the images and spectrographs attached hereto show that all significantly more silicone is deposited and soldered in the spirals and on the surface of the loose (after washing) than with conventional compositions. In Fig. 1, a thick coating on the surface of the lice can be seen with a physical plug which blocks the spiral. Fig. 2 shows that the plug is mainly silicone. Such plugs which coat the spiral can only be obtained with non-volatile siloxanes used in bile preparations because they are sufficiently adhesive to the outer head of the lice. In a similar manner, Fig. 3 shows a cross-section of a spiral showing penetration of the composition into the spiral as far down as in the trachea. Fig. 4 shows a significant amount of silicone present in the spiral. These images and spectrograms explain the superior performance of the compositions of the invention. In contrast, conventional siloxane compositions refer to siloxane formulations with very low viscosity, very low surface tension and which are thinly spread over the outer head of the lice. When it comes to the killing of head loosening as described in WO2010 / 018360, it is through aft terpenoids and phenylpropanoid derivatives, and especially linear terpenoids such as nerolidol, that the penetration character of siloxanes in the aerosol of the louse is improved. Lice saws need gas exchange of oxygen / carbon dioxide through their airway openings to develop. Blocking this structure will prevent the egg from developing. The research results described above show that the formulations of the liquid gel and the spray formulation, both of which contain nerolidol, are very effective in killing lice. While nerolidol is expected to improve the penetration of siloxanes in compositions of the bile invention into the air shark of the agen, it is also contemplated that the non-volatile siloxanes used in these compositions form plugs over the airway in the same manner as over the spirals, effectively blocking them. without necessarily having to penetrate deep into the airport. This explains why the egg is killed very quickly. 18
    权利要求:
    Claims (21)
    [1]
    A composition for use in the treatment or prophylaxis of ectoparasitic infestations on humans or animals, comprising a mixture of a carrier and an active moiety with an emulsifier, the carrier comprising a low viscosity non-volatile siloxane having a viscosity of the order of 10 to 1000 centistokes and the active moiety comprises a high viscosity non-volatile siloxane, where the viscosity is at least 1000 centistokes, and where the emulsifier comprises a copolymer of silicone, the low viscosity siloxane, the high viscosity siloxane and the mixture having a free point at least 100 ° C in a closed cup (closed cup).
    [2]
    A composition according to claim 1, wherein both the low viscosity siloxane and the high viscosity siloxane comprise a dimethicone or a dimethiconol or a mixture thereof.
    [3]
    A composition according to claim 1 or claim 2, in which the mixture has a viscosity exceeding 30 centistokes.
    [4]
    A composition according to any one of claims 1 to 3, in which both the low viscosity siloxane and the high viscosity siloxane have a surface tension of the order of 20 mN / m.
    [5]
    The composition of claim 1, comprising at least 1% by volume of the silicone copolymer.
    [6]
    A composition according to claim 1, comprising between 1 and 10% by volume of the copolymer of silicone.
    [7]
    A composition according to any one of claims 1 to 6, in which the emulsifier comprises a percent solution of a copolymer of dimethicone dissolved in cyclopentasiloxane. 19
    [8]
    A composition according to any one of claims 1 to 7, in which the low viscosity siloxane has a viscosity of the order of 10 to 100 centistokes.
    [9]
    A composition according to any one of claims 1 to 8, in which the high viscosity siloxane has a viscosity of the order of 50,000 to 200,000 centistokes.
    [10]
    A composition according to any one of claims 1 to 9, in which the high viscosity siloxane comprises at least 0.1% by volume of the composition.
    [11]
    A composition according to any one of claims 1 to 10, comprising an essential oil or essential oils.
    [12]
    A composition according to claim 11, in which the essential oil or oils comprise one or more terpenes.
    [13]
    A composition according to claim 11 or claim 12, in which the essential oil comprises nerolidol.
    [14]
    A composition according to any one of claims 11 to 13, in which the essential oil or oils comprise at least 0.1% by volume of the composition.
    [15]
    A composition according to any one of claims 11 to 14, in which the essential oil or oils comprise up to 2% by volume of the composition.
    [16]
    A composition according to any one of claims 1 to 15, comprising: 4% by volume of a dimethicone having a viscosity of 100,000 centistokes; between 1 and 4% by volume of an emulsifier comprising a copolymer of dimethicone; up to 2% by volume of nerolidol; and a residual portion of a dimethicone having a viscosity of between 10 and 100 centistokes.
    [17]
    The composition of claim 16, comprising a residual portion of a dimethicone having a viscosity of 50 centistokes.
    [18]
    A composition according to claim 16, comprising a residual part of a dimethicone having a viscosity of 10 centistokes.
    [19]
    A composition according to any one of claims 1 to 18, comprising a thixotropic additive for preparing the composition when used.
    [20]
    The composition of claim 19, wherein the thixotropic additive comprises nanosize silicon dioxide particles and constitutes at least 0.1% by volume of the composition.
    [21]
    A composition according to any one of the preceding claims for use in the treatment of or in the prevention of a headache infestation. 21 1/2
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    同族专利:
    公开号 | 公开日
    GB0908226D0|2009-06-24|
    CN102427820B|2014-05-21|
    AU2010247151A1|2011-12-01|
    CA2759546A1|2010-11-18|
    MY152966A|2014-12-15|
    MX2011012145A|2012-03-06|
    HRP20170764T1|2017-09-22|
    GB0912209D0|2009-08-26|
    PT2429284T|2017-07-18|
    FR2945447A1|2010-11-19|
    DK201170667A|2011-12-02|
    EP2429284B1|2017-04-12|
    GB2470208A|2010-11-17|
    HK1167813A1|2012-12-14|
    EA201171407A1|2012-05-30|
    JP5793492B2|2015-10-14|
    CN102427820A|2012-04-25|
    SE1100883A1|2012-02-09|
    WO2010130983A8|2011-12-22|
    EP2429284A1|2012-03-21|
    ES2380713B2|2013-12-10|
    PL2429284T3|2017-11-30|
    FR2945447B1|2011-06-03|
    TN2011000546A1|2013-05-24|
    DK2429284T3|2017-07-03|
    BRPI1007769A2|2015-09-01|
    AU2010247151B2|2015-10-22|
    HUE035165T2|2018-05-02|
    ES2628819T3|2017-08-04|
    ES2380713A1|2012-05-17|
    GB2470208B|2014-01-29|
    US8530451B2|2013-09-10|
    ZA201108348B|2013-01-30|
    DK177899B1|2014-12-01|
    JP2012526788A|2012-11-01|
    ECSP11011505A|2012-03-30|
    LT2429284T|2017-06-26|
    SI2429284T1|2017-07-31|
    CY1119274T1|2018-02-14|
    NI201100201A|2012-05-09|
    KR20120026543A|2012-03-19|
    CA2759546C|2015-02-03|
    KR101698624B1|2017-01-20|
    IL215837A|2015-01-29|
    CL2011002856A1|2012-06-01|
    PE20170204A1|2017-04-13|
    IL215837D0|2012-01-31|
    PE20120905A1|2012-08-02|
    DE112010001992T5|2013-08-22|
    EA020179B1|2014-09-30|
    SG175369A1|2011-11-28|
    US20120071444A1|2012-03-22|
    WO2010130983A1|2010-11-18|
    CO6470884A2|2012-06-29|
    UA107460C2|2015-01-12|
    CR20110597A|2012-03-09|
    NZ596526A|2013-06-28|
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    法律状态:
    优先权:
    申请号 | 申请日 | 专利标题
    GB0908226.4A|GB2470208B|2009-05-14|2009-05-14|A method and composition for the control of ectoparasites|
    GBGB0912209.4A|GB0912209D0|2009-05-14|2009-07-14|A method and composition for the control of ectoparasites|
    PCT/GB2010/000933|WO2010130983A1|2009-05-14|2010-05-12|A method and composition for the control of ectoparasites|
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